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Distribution of two GABA receptor-like subunits in the Drosophila CNS. Paper-1244306.
GABAA receptor RDL inhibits Drosophila olfactory associative learning. Paper-12650047.
A point mutation in a Drosophila GABA receptor confers insecticide resistance. Paper-7889711.
However, its potency ( IC50 500 microM) was much reduced when compared to GABAA receptors. Paper-929109.
Drosophila gamma-aminobutyric acid receptor gene Rdl shows extensive alternative splicing. Paper-7587127.
The GABAA receptor RDL suppresses the conditioned stimulus pathway for olfactory learning. Paper-13603452.
In contrast, Rdl receptor subunits appear confined to the neuropil in all developmental stages. Paper-1244306.
Cloning of the Drosophila cyclodiene insecticide resistance gene: a novel GABAA receptor subtype? Paper-88585.
GABA receptor minigene rescues insecticide resistance phenotypes in Drosophila. Paper-384830.
7. The GABA-evoked responses reversed close to the Nernst equilibrium potential for chloride ions. Paper-12649656.
The effect of a transmembrane amino acid on etomidate sensitivity of an invertebrate GABA receptor. Paper-1497085.
This is the first demonstration of alternative splicing in a GABA receptor gene from invertebrates. Paper-7587127.
The ILGICs, including GABAA, Gly, and GluCl receptors, conduct Cl- when the ligand is bound. Paper-1643783.
GABAA receptors in vertebrates assemble as heteromultimers to form an integral chloride ion channel. Paper-7889711.
Stable expression of a functional homo-oligomeric Drosophila GABA receptor in a Drosophila cell line. Paper-8231156.
GABAA receptors are composed of a number of different subunits that assemble to form a chloride ionophore. Paper-88585.
Transcriptional analysis of the Drosophila GABA receptor gene resistance to dieldrin. Paper-1628929.
Previously we have described the distribution of the Rdl GABA receptor subunit in the Drosophila CNS. Paper-1244306.
Splice-variant- and stage-specific RNA editing of the Drosophila GABA receptor modulates agonist potency. Paper-13698737.
1. The Drosophila gene Rdl (resistance to dieldrin) encodes a GABA receptor. Paper-7976751.
By correcting the pH shift induced by these acid salts, responses more typical of GABA agonists were seen. Paper-928901.
Cross-resistance with dieldrin of a novel tricyclic dinitrile GABA receptor antagonist. Paper-2011748.
Expression of functional GABA receptors in the cell lines was demonstrated by whole-cell patch clamp recordings. Paper-12649656.
Relative agonist potencies of the expressed receptor were found to be in the order GABA = TACA > CACA. Paper-8231156.
The potency of fipronil was dependent on the GABA concentration but was unaffected by membrane potential. Paper-410970.
Cation permeability and cation-anion interactions in a mutant GABA-gated chloride channel from Drosophila. Paper-1955455.
Alternative splicing of a Drosophila GABA receptor subunit gene identifies determinants of agonist potency. Paper-8732495.
Four observations establish that alpha-thujone is a modulator of the gamma-aminobutyric acid ( GABA) type A receptor. Paper-2200635.
In both oocytes and S2 cells, the three convulsants suppressed the amplitude of responses to GABA. Paper-979182.
In this paper we address submolecular mechanisms for gamma-aminobutyric acid ( GABA) receptor modulation by isoflurane. Paper-1254046.
Allosteric modulation of an expressed homo-oligomeric GABA-gated chloride channel of Drosophila melanogaster. Paper-754934.
An order of potency of GABA approximately muscimol approximately TACA > CACA > glycine was observed. Paper-8118970.
Glutamate, GABA and acetylcholine signaling components in the lamina of the Drosophila visual system. Paper-14318099.
Effects of [3H]-BIDN, a novel bicyclic dinitrile radioligand for GABA-gated chloride channels of insects and vertebrates. Paper-1153259.
Thus, BIDN probes a novel site on GABA-gated Cl- channels to which a number of insecticidally-active molecules bind. Paper-1153259.
GABA receptors containing Rdl subunits mediate fast inhibitory synaptic transmission in Drosophila neurons. Paper-9715295.
Ionotropic gamma-aminobutyric acid ( GABA) receptors are distributed throughout the nervous systems of many insect species. Paper-1290864.
pH-dependent actions of THIP and ZAPA on an ionotropic Drosophila melanogaster GABA receptor. Paper-928901.
Expression of functional GABA-gated ion channels in these cell lines was demonstrated by electrophysiological recording. Paper-8231156.
The first six introns in Rdl show positions similar to those in vertebrate GABAA receptors, whereas the last two differ. Paper-7530926.
A missense mutation has been found in the gene encoding the GABA- A beta 3 subunit in a patient with chronic insomnia. Paper-12232574.
Actions of picrodendrin antagonists on dieldrin-sensitive and -resistant Drosophila GABA receptors. Paper-929108.
Referred to as picrodendrins, they inhibit the binding of [35S]-tert-butylbicyclophosphorothionate ( TBPS) to rat GABAA receptors. Paper-929108.
Alternative splicing of the Drosophila melanogaster Rdl gene yields four ionotropic GABA receptor subunits. Paper-8732495.
Resistance to fipronil in Drosophila simulans: influence of two point mutations in the RDL GABA receptor subunit. Paper-11282392.
Recombinant baculoviruses containing two alternative splice forms of the Drosophila Rdl GABA receptor gene were constructed. Paper-7740807.
Drosophila sleep has recently been shown to be controlled by GABA, which acts on unknown cells expressing the Rdl GABAA receptor. Paper-14342855.
When either 1 microM fipronil or 1 microM BIDN was present in the external saline, the GABA-gated channels were completely blocked. Paper-8505369.
The channel activators avermectin and moxidectin usually retain their inhibitory potency in the Rdl subunit mutants. Paper-176344.
Stably-transfected clonal cell lines which expressed high levels of GABA receptor were identified by specific [3H]-muscimol binding. Paper-8231156.
The most potent agonists of these receptors were GABA, muscimol and trans-aminocrotonic acid (TACA), which were approximately equipotent. Paper-929109.
These include Resistance to dieldrin, or Rdl, and a homologue of the vertebrate GABAA receptor beta subunit. Paper-413675.
2. In cultured neurons from both wild type and mutant strains, GABA activated a channel that reversed near 0 mV in symmetrical chloride. Paper-7976751.
Of the four receptor variants tested, the double mutant showed the highest resistance to fipronil, following repeated GABA applications. Paper-11282392.
Clonal cell lines stably expressing homo-oligomeric L. striatella GABA receptors were generated by transfecting the vector into D.mel-2 cells. Paper-12649656.
Thus both BIDN and fipronil shorten the duration of wild-type RDL(ac) GABA receptor channel openings but appear to act at distinct sites. Paper-8505369.
Actions of picrotoxinin analogues on an expressed, homo-oligomeric GABA receptor of Drosophila melanogaster. Paper-283437.
Thus, alpha-thujone in absinthe and herbal medicines is a rapid-acting and readily detoxified modulator of the GABA-gated chloride channel. Paper-2200635.
We identify here the relevant Rdl-containing cells as PDF-expressing small and large ventral lateral neurons (LNvs) of the circadian clock. Paper-14342855.
3. Utilizing the appropriate GABA EC10, etomidate (300 microM) had little effect on the agonist-evoked current of the wild type Rdl receptor. Paper-1497085.
Wild-type and insecticide-resistant homo-oligomeric GABA receptors of Drosophila melanogaster stably expressed in a Drosophila cell line. Paper-979182.
3-Aminopropane sulphonic acid (3-APS), a partial agonist of RDLac homo-oligomers, was the weakest agonist tested and 100 fold less potent than GABA. Paper-929109.
Drosophila GABA-gated chloride channel: modified [3H]EBOB binding site associated with Ala-->Ser or Gly mutants of Rdl subunit. Paper-176344.
Interestingly, despite the use of GABA in both the peripheral and CNS of insects, Rdl GABA receptor subunits appear to be confined to the CNS. Paper-1244284.
We conclude that the model and docking procedures yield a good model of the insect GABA receptor binding site and the location of agonists within it. Paper-14686844.
2. The actions of GABA, isoguvacine and isonipecotic acid on RDLac and DRC 17-1-2 homo-oligomers were compared, by use of two-electrode voltage-clamp. Paper-929109.
Actions of the insecticide fipronil, on dieldrin-sensitive and- resistant GABA receptors of Drosophila melanogaster. Paper-410970.
Patch-clamp electrophysiology reveals GABA- activated picrotoxin-sensitive chloride currents on PDF+ neurons. Paper-13660697.
Similarly, etomidate acting at RdlM314S receptors produced an enhancement of GABA but the magnitude of the effect was reduced compared to RdlM314N receptors. Paper-1497085.
Prior studies have shown that the GABA receptor RDL inhibits aversive olfactory learning via its role in the Drosophila mushroom bodies (MBs). Paper-13603452.
In Drosophila melanogaster resistance is associated with a single base pair substitution in the GABA receptor/ chloride ion channel gene Rdl. Paper-7886183.
GABA-evoked currents are highly sensitive to antagonism by picrotoxin but are insensitive to bicuculline, RU 5135, or zinc. Paper-124672.
GABA is the likely transmitter of centrifugal neurons C2 and C3 and GABA(B) receptor immunoreactivity is seen on these neurons as well as the Cha-Tan neurons. Paper-14318099.
Cloning of a putative GABAA receptor from cyclodiene-resistant Drosophila: a case study in the use of insecticide-resistant mutants to isolate neuroreceptors. Paper-11720187.
3. The sodium salts of pentobarbitone (10 microM to 1 mM) and phenobarbitone (50 microM to 1 mM) dose-dependently enhanced submaximal GABA responses. Paper-754934.
DmRdl antibodies also immunoprecipitated all solubilized nodulisporic receptors, but only approximately 70% of the ivermectin receptors. Paper-9459653.
RDL is an ionotropic GABA receptor subunit, a product of the Rdl gene, originally identified in the Maryland strain of Drosophila melanogaster. Paper-979182.
Actions of agonists and convulsant antagonists on a Drosophila melanogaster GABA receptor ( Rdl) homo-oligomer expressed in Xenopus oocytes. Paper-8118970.
Immunocytochemical mapping of a C-terminus anti-peptide antibody to the GABA receptor subunit, RDL in the nervous system in Drosophila melanogaster. Paper-539908.
Results are compared with the distribution of staining observed in the insect CNS with antibodies against GABA itself and synaptotagmin, a synaptic vesicle protein. Paper-1244284.
The large variation in mIPSC frequency, amplitude, and kinetics properties between neurons suggests heterogeneity in GABA receptor number, location, and/or subtype. Paper-9715295.
4. At 10 microM, the steroids 5 alpha-pregnan-3 alpha-ol-20-one and alphaxalone (5 alpha-pregnan-3 alpha-ol-11,20-dione), potentiated submaximal GABA responses. Paper-754934.
Thus, the RDL homo-oligomer exhibits a pharmacological profile for picrotoxinin analogues resembling that of native GABA receptors. Paper-283437.
The properties of this dieldrin-resistant, homo-oligomeric receptor have been compared with those of the stably expressed, wild-type form (S2- RDL). Paper-979182.
When expressed in Xenopus laevis oocytes, the subunit functions efficiently, presumably as a homooligomeric complex and is activated by GABA or muscimol. Paper-124672.
This receptor is picrotoxin (PTX) sensitive but bicuculline (BIC) insensitive and cannot be readily classified within the known GABAA receptor subtypes. Paper-413675.
A cloned Drosophila gamma-aminobutyric acid GABA receptor subunit ( Rdl) has been stably expressed as a functional homo-oligomeric ion channel in a Drosophila cell line. Paper-8231156.
The differences in the benzodiazepine pharmacology of RDL homo-oligomers and native GABA receptors, may reflect roles of other subunits in native insect receptors. Paper-754934.
A single point mutation in the insect gamma-aminobutyric acid receptor (GABAR)-encoding gene ( Rdl) confers high levels of resistance to cyclodienes in Drosophila and other insects. Paper-567179.
The stereoselectivity of steroid action seen on vertebrate GABAA receptors was observed on RDL homo-oligomers as 5 alpha-pregnan-3 beta-ol-20-one (10 microM) was without effect. Paper-754934.
Following analysis of two dissimilar cDNAs isolated from the locus, we report that Rdl undergoes extensive alternative splicing at two locations in the putative extracellular domain. Paper-7587127.
A single point mutation within the GABA receptor gene Resistance to dieldrin ( Rdl) confers a high level of resistance to cyclodiene insecticides in a wide range of insects. Paper-384830.
We report that coinfection of cells with recombinant baculoviruses containing Rdl plus beta subunits induces GABA receptors with distinct pharmacological and kinetic properties. Paper-413675.
Resistance to the cyclodiene insecticide dieldrin maps to a single gene ( Rdl) on the left arm of chromosome III in Drosophila melanogaster (Meigen). Paper-6889971.
In wild-type receptors, the inhibition of GABA (EC(30))-induced currents by fipronil and picrotoxin was enhanced by repeated GABA applications. Paper-11282392.
3-Hydroxymethyl-beta-carboline (1 microM) and ethyl-beta-carboline-3-carboxylate (both 1 and 100 microM) had no effect on currents induced by 30 microM (approximately EC50) GABA. Paper-754934.
Molecular cloning of a GABA receptor subunit from Laodelphax striatella (Fallén) and patch clamp analysis of the homo-oligomeric receptors expressed in a Drosophila cell line. Paper-12649656.
Ionotropic GABA receptors are widely distributed throughout the vertebrate and invertebrate central nervous system ( CNS) where they mediate inhibitory neurotransmission. Paper-14686844.
One of the most widely studied insect GABA receptors is constructed from RDL (resistance to dieldrin) subunits from Drosophila melanogaster. Paper-14686844.
Western blotting of cell membrane extracts and immunoprecipitation experiments with an anti- Rdl antiserum recognized a protein of the expected size of approximately 65 kDa. Paper-7740807.
Injections of GABA and Mas-allatotropin into the vicinity of the accessory medulla resulted in stable phase-dependent resetting of the circadian locomotor activity of the cockroach. Paper-9327717.
Two-electrode voltage-clamp was used to investigate allosteric modulation of GABA-induced currents recorded from the expressed, bicuculline-insensitive, RDL homo-oligomers. Paper-754934.
To our knowledge, this represents the first cloning of an invertebrate GABA receptor and also allows us to manipulate the resistance status of an insect via germ-line transformation. Paper-6882565.
The GABAA receptor, resistance to dieldrin ( Rdl), is highly expressed in the Drosophila mushroom bodies (MBs), a group of neurons playing essential roles in insect olfactory learning. Paper-12650047.
Single channel analysis of the blocking actions of BIDN and fipronil on a Drosophila melanogaster GABA receptor ( RDL) stably expressed in a Drosophila cell line. Paper-8505369.
The Ala-->Ser replacement with both melanogaster and simulans almost always reduces the potency in inhibiting [3H]EBOB binding of each of eight channel blockers and of muscimol and GABA. Paper-176344.
4. Functional GABA-gated chloride channels of rootworm nervous system and of cockroach nerve and muscle were blocked by BIDN, whereas cockroach neuronal GABA(B) receptors were unaffected. Paper-1153259.
4. SR95531, an antagonist of vertebrate GABAA receptors, competitively inhibited the GABA responses of RDLac homo-oligomers, which have previously been found to insensitive to bicuculline. Paper-929109.
The Ala-->Gly replacement in D. simulans is generally less effective than the Ala-->Ser modification in reducing sensitivity to the channel blockers and to muscimol and GABA. Paper-176344.
Here, we report the generation of a Drosophila melanogaster cell line (S2-RDLA302S) stably expressing a mutated, dieldrin-resistant (A302S) form of RDL. Paper-979182.
Thus, in accord with earlier work on agonist and allosteric sites, the S2- RDL cell line is found to yield similar pharmacological results to those obtained in transient expression studies. Paper-979182.
Stable expression of insect GABA receptors in insect cell lines. Promoters for efficient expression of Drosophila and mosquito Rdl GABA receptors in stably transformed mosquito cell lines. Paper-517171.
Resistance is due to insensitivity of the cyclodiene/ picrotoxinin binding site on the gamma-aminobutyric acid subtype A (GABAA) receptor-chloride ionophore complex. Paper-6882565.
Here, we report the identification of the region containing the rdl promoter, via transient expression of a luc reporter gene following micro-injection into embryos of the mosquito Aedes aegypti. Paper-567179.
3. GABA responses in neurons from the mutant strains showed reduced sensitivity to the GABA antagonists picrotoxin, lindane and t-butyl-bicyclophosphorothionate. Paper-7976751.
The differences in the potency of agonists on RDLac and DRC 17-1-2 homo-oligomers observed in the present study may assist in identification of further molecular determinants of GABA receptor function. Paper-929109.
1. A series of terpenoid compounds, recently isolated from Picrodendron baccatum, share a picrotoxane skeleton with picrotoxinin, an antagonist of ionotropic GABA receptors. Paper-929108.
9. The depression of GABA response at high isoflurane concentrations, in WT receptors, (typical of a variety of anaesthetic agents) may reflect low affinity channel block via the PTX site. Paper-1254046.
5. Isoflurane, 195-389 microM, enhanced GABA conductance in both receptor variants by significantly increasing the affinity of the agonist for its receptor without changing Hill slope or maximal response. Paper-1254046.
Branch IIIA, composed of vertebrate Gly receptors, is loosely clustered with Branch IIIB, composed of invertebrate GluCl receptors, to form Branch III, which is designated NA for being non- GABA responsive. Paper-1643783.
Picrotoxinin ( PTX) and cyclodiene insecticides are GABAA receptor antagonists which competitively displace each other from the same binding site. Paper-7889711.
Using RDL, a Drosophila melanogaster GABA-gated ion channel, we examined the functional impact of RNA editing at several sites along with alternative splicing of more than one exon. Paper-13698737.
A rapid increase in spontaneous firing in response to bath application of picrotoxin demonstrates that these GABA receptors mediate inhibition in the neuronal networks formed in culture. Paper-9715295.
The developmental GABA switch is mediated primarily by KCC2, a neuronal K+/Cl- cotransporter that determines the intracellular concentration of Cl- and, hence, the reversal potential for GABA. Paper-12088487.
To investigate the structural basis of anion selectivity of Drosophila GABA-gated Cl(-) channels, the permeation properties of wild-type and mutant channels were studied in Xenopus oocytes. Paper-1955455.
The gene product appears to code for a subunit of a receptor highly similar to vertebrate GABAA receptor/ chloride ion channels, and functional expression studies are described which will elucidate its pharmacology. Paper-11720187.
The significance of the expression of an insect GABA receptor in an insect cell line and the similarity of the results from these functional expression studies to recordings from cultured neurons is discussed. Paper-7740807.
These results suggest possible roles for an RDL-like GABA receptor subunit in the processing of olfactory, visual and mechanosensory information in the nervous system of D. melanogaster. Paper-539908.
7. Etomidate acting at human alpha6beta3gamma2L receptors is known to produce a large enhancement of GABA-evoked currents and at higher concentrations this anaesthetic directly activates the GABA(A) receptor complex. Paper-1497085.
In situ hybridization using Rdl cDNA probes and the anti- Rdl antibody shows that Rdl message and protein are highly expressed in the developing central nervous system ( CNS) of 15-17 h embryos. Paper-1244284.
Expression of a Drosophila GABA receptor in a baculovirus insect cell system. Functional expression of insecticide susceptible and resistant GABA receptors from the cyclodiene resistance gene Rdl. Paper-7740807.
Previously, we used a field-isolated Drosophila mutant Rdl (Resistant to dieldrin) insensitive to PTX and cyclodienes to clone a putative GABA receptor. Paper-7889711.
The cyclodiene resistance gene Rdl (resistance to dieldrin) was cloned from a mutant of the model insect Drosophila resistant to cyclodienes and picrotoxinin. Paper-8066059.
Antagonists such as fipronil (100 nM), 4'-ethynyl-4-n-propylbicycloorthobenzoate ( EBOB) (100 nM), dieldrin (100 nM) and SR95531 (gabazine) (1 microM) suppressed GABA-induced currents. Paper-12649656.
1. The Drosophila melanogaster gamma-aminobutyric acid ( GABA) receptor subunits, RDLac and DRC 17-1-2, form functional homo-oligomeric receptors when heterologously expressed in Xenopus laevis oocytes. Paper-929109.
Partial atomic charges and dipole separation distances of a range of GABA analogues were calculated, and the potency of the analogues was determined using RDL receptors expressed in Xenopus oocytes. Paper-14686844.
We are interested in establishing stably transformed insect cell lines efficiently expressing the insect gamma-aminobutyric acid ( GABA) receptor subunit gene Resistance to dieldrin or Rdl. Paper-517171.
1. Functional GABA-gated chloride channels are formed when cRNA encoding the Drosophila melanogaster GABA receptor subunit RDL is injected into the cytoplasm of Xenopus oocytes. Paper-754934.
By contrast, at RdlM314N receptors, etomidate produced a clear concentration-dependent enhancement of GABA-evoked currents with a calculated EC50 of 64+/-3 microM and an Emax of 68+/-2% (of the maximum response to GABA). Paper-1497085.
By combining fluorescent in situ hybridization and immunolabeling against GFP expressed with cell-type-specific GAL4 driver strains, we quantified the percentage of the cells that produce or receive GABA for each cell type. Paper-13656740.
Rdl codes for a subunit of a novel class of GABA gated chloride ion channels and resistance is correlated with replacement of the same amino acid residue in a wide range of species from different insect orders. Paper-8066059.
Sensitivity to the block by KN244 of the response to 30 microM GABA (IC50=41.6 nM, wild-type RDLac) was reduced abut 100 fold (IC50=4.5 microM) in the dieldrin-resistant (RDLacA302S) form of RDL. Paper-2011748.
Using these stable lines, a striking reduction in sensitivity to both picrotoxinin and dieldrin was observed for responses to GABA of S2-RDLA302S compared to S2- RDL. Paper-979182.
2. In the case of the wild type receptor, fipronil blocked GABA-induced currents inducing both a shift to the right in the GABA dose-response curve and depressing the maximum amplitude of responses to GABA. Paper-410970.
In order to examine the conservation of the mechanism of cyclodiene insecticide resistance between species we cloned a cDNA from the yellow fever mosquito Aedes aegypti homologous to the resistance gene Rdl in Drosophila. Paper-7891072.
Ivermectin and nodulisporic acid receptors in Drosophila melanogaster contain both gamma-aminobutyric acid-gated Rdl and glutamate-gated GluCl alpha chloride channel subunits. Paper-9459653.
Whole cell patch clamp analysis of cells infected with either splice form revealed functional expression of GABA gated chloride ion channels which were blocked by application of 1 microM picrotoxinin. Paper-7740807.
BIDN blocked the wild-type form of the receptor in a neither purely competitive, nor purely non-competitive manner, being dependent on the GABA concentration yet insurmountable, and block was independent of the membrane potential. Paper-571979.
The Drosophila gamma-aminobutyric acid ( GABA) receptor subunit gene Rdl was isolated on the basis of a mutant phenotype showing high levels of insensitivity to picrotoxinin and cyclodiene insecticides. Paper-7587127.
2. Flunitrazepam (0.1 microM to 100 microM) had no effect on the amplitude of responses to 10 microM GABA (approximately EC10), whereas 4'chlorodiazepam (100 microM) enhanced the amplitude of submaximal responses to GABA. Paper-754934.
In conclusion, the present study emphasizes new aspects of the pharmacological alterations induced by the Rdl mutation and shows that resistance to GABA receptor-directed insecticides may implicate a mutation distinct from Rdl. Paper-11282392.
6. The potencies of barbiturates and steroids on RDL homo-oligomers resemble those observed for several in situ insect GABA receptors, whereas those of benzodiazepine binding-site ligands are considerably reduced. Paper-754934.
The actions of THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) and ZAPA (Z-3-[(aminoiminomethyl)thio]prop-2-enoic acid) were tested on an ionotropic homo-oligomeric GABA receptor of Drosophila melanogaster. Paper-928901.
Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes. Paper-571979.
4. As previously shown, the point mutation in the M2 domain conferred a profound resistance to the blocking action of 10 microM picrotoxinin ( PTX): circa 7 fold reduction at the GABA EC20. Paper-1254046.
Rdl knock down failed to enhance learning in animals carrying mutations in genes of the cAMP signaling pathway, such as rutabaga and NF1, suggesting that RDL works up stream of these functions in CS/US integration. Paper-13603452.
The EC(so) values for GABA and its analogues isoguvacine, muscimol, isonipecotic acid and 3-amino sulphonic acid on the RDL(ad) homomeric receptor differed from those previously described for RDL(ac) and DRC17-1-2 receptors. Paper-8732495.
Molecular cloning of the cDNA encoding the RDL GABA receptor subunit of this strain revealed the presence of two mutations: the Rdl mutation (A301G) and an additional mutation in the third transmembrane domain (T350M). Paper-11282392.
The amplitudes of agonist-induced currents were found to be in the order muscimol (100 microM) >/= GABA (100 microM) > isoguvacine (100 microM) > cis-4-aminocrotonic acid (CACA) (100 microM) > 5-(4-piperidyl)-3-isoxazolol (4-PIOL) (1 mM). Paper-12649656.
A variety of gamma-aminobutyric acid ( GABA) receptor convulsants, including the insecticides heptachlor ( IC50, 35 +/- 3 nM) and dieldrin ( IC50, 93 +/- 7 nM), displaced [3H]-BIDN from rootworm membranes. Paper-1153259.
Cytoplasmic injection of Xenopus oocytes with cDNA-derived RNA (cRNA) encoding a wild-type Drosophila melanogaster GABA receptor subunit ( Rdl) resulted in functional expression of a GABA receptor homo-oligomer. Paper-8118970.
5. The effects of this mutation were selective for etomidate as the GABA-modulatory actions of 1 mM pentobarbitone at wild type Rdl (49+/-4% of the GABA maximum) and RdlM314N receptors (53+/-2% of the GABA maximum) were similar. Paper-1497085.
The high potency and efficacy of isoguvacine and ZAPA distinguishes RDLac homo-oligomers from bicuculline-insensitive vertebrate GABAC receptors, while the low potency of SR95531 and 3-APS distinguishes them from GABAA receptors. Paper-929109.
4. Analysis of the predicted amino acid sequence and gene structure shows that Rdl codes for a receptor subunit similar to vertebrate GABAA receptors, but sufficiently different that it may represent a novel class of GABAA receptor subtype. Paper-88585.
Under two-electrode voltage-clamp, the actions of picrodendrins and related terpenoids have been assayed on homooligomeric GABA receptors formed by the expression of a Drosophila GABA receptor subunit (RDLac) in Xenopus oocytes. Paper-929108.
Oocytes injected with in vitro transcribed RNA, encoding either HisCl1 or HisCl2, produced substantial chloride currents in response to histamine but not in response to GABA, glycine, and glutamate. Paper-9154401.
The L. striatella GABA receptor subunit was found to have high amino acid sequence similarity to the bd-type splice variant of the Drosophila GABA receptor Rdl subunit and several other GABA receptor subunits, with identities of over 70%. Paper-12649656.
Branch II, named NB for non-benzodiazepine binding, and consisting of GABAA receptor beta, delta, pi, and rho subunits, is further subdivided into IIA, containing beta subunits; IIB, containing delta, and pi subunits; and IIC, containing rho subunits. Paper-1643783.
2. Complementary RNA-injected oocytes expressing the wild type Rdl GABA receptor and voltage-clamped at -60 mV responded to bath applied GABA with a concentration-dependent inward current response and a calculated EC50 for GABA of 20+/-0.4 microM. Paper-1497085.
Here we report the production of stable mosquito cell lines carrying high copy numbers of Rdl genes from both Drosophila and Aedes aegypti mosquitoes and the subsequent high efficiency expression of functional GABA gated chlorine ion channels. Paper-517171.
Cyclodiene resistance in D. melanogaster has been attributed to a mutation resulting in an Ala302-->Ser replacement in the Rdl GABA receptor subunit and in D. simulans to an homologous Ala-->Ser or Gly replacement. Paper-176344.
Finally, neurons from the GABA receptor subunit mutant Rdl exhibit reduced sensitivity to picrotoxin blockade of the mIPSCs and resistance to picrotoxin-induced increases in spontaneous firing frequency. Paper-9715295.
Therefore a Drosophila mutant ( Rdl), resistant to cyclodienes and the GABAA receptor ligand picrotoxin ( PTX), was used to clone the gene responsible for resistance as a putative invertebrate GABAA receptor. Paper-88585.
In order to assess the individual and combined roles of the two mutations in fipronil resistance, the functional properties of wild-type, A301G, T350M and A301G/T350M homomultimeric RDL receptors were compared by expression in Xenopus oocytes. Paper-11282392.
Genomic clones from the Rdl locus of Drosophila, whose mutant phenotype is resistant to cyclodiene insecticides and picrotoxin, were characterized by restriction mapping and partial sequencing to determine intron/exon structure. Paper-7530926.
Branch I, called BZ, for the majority of the members are known to be related to benzodiazepine binding, is subdivided into IA, composed of all GABAA receptor alpha subunits, and IB, composed of the gamma and epsilon subunits, which are shown to be tightly linked. Paper-1643783.
The receptor antagonist actions are described for a novel bicyclic dinitrile compound (BIDN, 3,3-bis-(trifluoromethyl)-bicyclo [2.2.1] heptane-2,2-dicarbonitrile) on a Drosophila melanogaster homo-oligomeric GABA receptor expressed in Xenopus oocytes. Paper-571979.
This approach yielded three discrete amplified sequence elements (designated LCCH1, LCCH2, and LCCH3) that contained open reading frames and > 40% amino acid sequence identity to the corresponding regions of vertebrate ligand-gated chloride channel genes. Paper-8066061.
As the mutation A302-->S reduces the potency of both fipronil and picrotoxinin, homooligomeric RDL receptors should facilitate detailed studies of the molecular basis of convulsant/insecticide antagonist actions on GABA receptors. Paper-410970.
By making use of transgenic tools and immunohistochemistry, our results suggest that HS and VS cells of Drosophila express gamma-aminobutyric acid ( GABA) receptors in their dendritic region within the lobula plate, thus being postsynaptic to inhibitory input there. Paper-13192783.
Pentobarbitone greatly enhances GABA-evoked currents, whereas the neurosteroid 5 alpha-pregnan-3 alpha-ol-20-one demonstrates a large reduction in both the potency and maximal effect when compared with its actions upon vertebrate GABA type A receptors. Paper-124672.
Rapid and pronounced rundown of responses to GABA during whole-cell patch clamp recordings was overcome by the inclusion of EGTA in the pipette solution, indicating a possible role for calcium-dependent processes in the functional regulation of this GABA receptor. Paper-8231156.
Response of the expressed Drosophila Rdl receptor to GABA was reduced by t-butylbicyclophosphorothionate (TBPS), 4-n-propyl-4'-ethynylbicycloorthobenzoate ( EBOB), picrotoxinin and the novel insecticide, fipronil (all at 1.0 x 10(-5) M). Paper-8118970.
8. The location of alanine 302 in the sequence of the Rdl gene product supports a mechanism of action in which convulsants such as picrotoxin bind within the channel lumen, where they induce a rapid conformational change to the desensitized state. Paper-7976751.
Mutation of the human beta3 subunit asparagine to methionine (beta3 N289M found in the equivalent position in Rdl completely inhibited both the GABA-modulatory and GABA-mimetic action of etomidate (10-300 microM) acting at alpha6beta3 N289Mgamma2L receptors. Paper-1497085.
4. The actions of etomidate at RdlM314N receptors exhibited an enantioselectivity common to that found for mammalian receptors, with 100 microM R-(+)-etomidate and S-(-)-etomidate enhancing the current induced by GABA (EC10) to 52+/-6% and 12+/-1% of the GABA maximum respectively. Paper-1497085.
These results are examined in relation to the proposal, based on amino acid identities, that Rdl codes for a novel class of GABAA receptor subunit more closely related to glycine receptors, and the possible place of Rdl in the lineage of the receptor superfamily is discussed. Paper-7530926.
A polymerase chain reaction (PCR)-based homology probing strategy was employed to screen Drosophila melanogaster genomic DNA for sequences encoding a conserved amino acid 'signature motif' known to be present in vertebrate GABA receptor and glycine receptor subunit genes. Paper-8066061.
Receptors in which the transmembrane methionine residue ( M314) had been exchanged for an asparagine (RdlM314N) or a serine (RdlM314S) also exhibited a concentration-dependent inward current response to GABA, but in both cases with a reduced EC50 of 4.8+/-0.2 microM. Paper-1497085.
This mutation not only identifies a single amino acid conferring high levels of resistance to the important GABA receptor antagonist PTX but also, by conferring resistance to cyclodienes, may account for over 60% of reported cases of insecticide resistance. Paper-7889711.
The non-competitive blocker site of the GABA-gated chloride ion channel in normal susceptible strains of Drosophila melanogaster and simulans binds 4-n-[3H]propyl-4'-ethynylbicycloorthobenzoate ([3H]EBOB) at specific sites with KdS of 1.6-1.9 nM and BmaxS of 171-181 fmol/mg protein. Paper-176344.
2. Wild-type Drosophila melanogaster homo-oligomeric GABA receptors were characterized and compared with an ion-channel mutant ( alanine substituted to a serine in M2) by means of two-electrode voltage-clamp in membrane-invariant Xenopus oocytes. Paper-1254046.
Following our recent cloning of a novel gamma-aminobutyric acid ( GABA) receptor subunit gene Resistance to dieldrin or Rdl form cyclodiene resistance locus in Drosophila melanogaster, we were interested in defining its pattern of expression during development. Paper-1244284.
5. The novel anticonvulsant, loreclezole (100 microM), potentiated the response to 10 microM GABA, but not that of saturating concentrations of GABA. delta-Hexachlorocyclohexane (0.1 microM to 30 microM) was a potent enhancer of submaximal responses to GABA of RDL. Paper-754934.
5. Expression in Xenopus oocytes of either rat brain mRNA, or cDNA-derived RNA encoding a GABA receptor subunit ( Rdl) that is expressed widely in the nervous system of Drosophila melanogaster resulted in functional, homo-oligomeric GABA receptors that were blocked by BIDN. Paper-1153259.
RDLac homo-oligomers were fully activated by a range of GABA analogues, with the order of potency: GABA > ZAPA ((Z)-3-[(aminoiminomethyl)thio]prop-2-enoic acid) > isoguvacine > imidazole-4-acetic acid > or = isonipecotic acid > or = cis-aminocrotonic acid (CACA) > beta-alanine. Paper-929109.
Thus, using expression in Xenopus oocytes, we have demonstrated differences in agonist potency for the neurotransmitter GABA (and four analogues) between splice variant products of the Drosophila melanogaster Rdl gene encoding homomer-forming GABA receptor subunits. Paper-8732495.
We show that alternative splicing and RNA editing have a combined influence on the potency of the neurotransmitter GABA, and the editing isoforms detected in vivo span the entire functional range of potencies seen for all possible edit variants expressed in Xenopus laevis oocytes. Paper-13698737.
This single amino acid replacement Ala302 > Ser, within the proposed lining of the chloride ion channel, also confers insensitivity to the blocking action of cyclodienes and picrotoxinin on GABA gated chloride ion channels expressed in Xenopus oocytes. Paper-8066059.
These data suggest that both DmGluCl alpha and DmRdl are components of nodulisporic acid and ivermectin receptors, and that there also exists a distinct class of ivermectin receptors that contains the DmGluCl alpha subunit but not the DmRdl subunit. Paper-9459653.
The global association of a single amino acid replacement with cyclodiene resistance suggests that the resistance phenotype depends on changes in both of these properties, and that insecticides have selected residue 302 of Rdl for replacement because of its unique ability to influence both of these functions. Paper-7976751.
LCCH1 was identical to the Rdl gene, a known GABA receptor subunit gene from D. melanogaster, whereas LCCH2 and LCCH3 were novel D. melanogaster sequences that exhibited structural similarity to other members of the ligand-gated chloride channel gene family. Paper-8066061.
Here we report the functional expression and novel pharmacology of this GABA receptor and examine the functionality of a resistance-associated point mutation ( alanine to serine) within the second membrane-spanning domain, the region thought to line the chloride ion channel pore. Paper-7889711.
The actions of picrotoxinin and four of its analogues were tested on a Drosophila melanogaster homo-oligomeric GABA (gamma-aminobutyric acid) receptor formed when RDL (resistance to dieldrin) subunits were expressed in Xenopus oocytes. Paper-283437.
An antibody raised against a peptide based on the C-terminal derived amino acid sequence from a cloned Drosophila melanogaster (fruit fly) gene, Rdl (resistant to dieldrin), was used to investigate localization of a GABA receptor subunit in adult male D. melanogaster. Paper-539908.
3. Mutant RDL GABA-receptors, which have a naturally occurring amino acid substitution (A302-->S) in the putative ion-channel lining region, conferring resistance to dieldrin and picrotoxinin, were markedly less sensitive to fipronil than the wild-type receptors. Paper-410970.
Here, we have utilized the Xenopus laevis oocyte expression system in conjunction with the two-point voltage clamp technique to determine the influence of the equivalent amino acid ( M314) on the actions of this anaesthetic at an etomidate-insensitive invertebrate GABA receptor ( Rdl) of Drosophila melanogaster. Paper-1497085.
In addition to providing a possible physiological role for the alternative splicing of Rdl, these data delineate a hitherto functionally unassigned region of the N-terminal domain of GABA receptor subunits, which affects agonist potency and aligns closely with known determinants of potency in nicotinic acetylcholine receptors. Paper-8732495.
Knowing that Rdl can coassemble with LCCH3 (a Drosophila GABA receptor-like subunit showing sequence similarity to vertebrate beta subunit GABAA receptors) in baculovirus infected insect cells, we compared the localization of these two receptor subunits in order to identify any potential overlap in their spatial or temporal distribution. Paper-1244306.
To determine if these stable insect cell lines generate results similar to those obtained by transient expression in Xenopus laevis oocytes, we have examined the actions of two widely used convulsants, EBOB and TBPS, and a recently developed convulsant BIDN, on RDL-mediated GABA responses in the two expression systems. Paper-979182.
In agreement with previously reported studies on native insect GABA receptors and native expressed vertebrate GABA receptors, acetylation of the bridgehead hydroxyl group ( picrotoxinin acetate) greatly reduced the activity of the molecule, but surprisingly, substitution with flourine at the same position also reduced the activity. Paper-283437.
1. Blocking actions of the novel insecticide, fipronil, were examined on GABA responses recorded from Xenopus oocytes expressing either wild type ( dieldrin-sensitive) or mutant ( dieldrin-resistant) forms of the Drosophila melanogaster GABA-gated chloride channel homo-oligomer, RDL (the product of the resistance to dieldrin locus: Rdl). Paper-410970.
These synonyms are used for gene Rdl (Resistant to dieldrin): RDL, rdl, Rd1, Protein cyclodiene resistance, LCCH1, Gamma-aminobutyric acid receptor subunit beta, GABAr, GABA[[A]] receptor, GABA[[A]], GABA(A) receptor subunit beta, GABA, gaba, DmRDL, DmRdl, Dmel\CG10537, CG10537.
These accession numbers are used for gene Rdl: Q8IQB5 (UNIPROT__AC), Q7JPX8 (UNIPROT__AC), AAN11988 (NCBI_GENBANK__AC), AAA28556 (NCBI_GENBANK__AC).
Rdl is a homologue of lgc-38 (Ligand-Gated ion Channel) from Caenorhabditis elegans.
Rdl is a homologue of glra4a (glycine receptor, alpha 4a) from Danio rerio.
Rdl is a homologue of GLRA4 (glycine receptor, alpha 4) from Homo sapiens.
Rdl is a homologue of GLRA4 (glycine receptor, alpha 4) from Pan troglodytes.
Rdl is a homologue of GLRA4 (glycine receptor, alpha 4) from Canis lupus familiaris.
Rdl is a homologue of GLRA4 (glycine receptor, alpha 4) from Gallus gallus.
Rdl is a homologue of Glra4 (glycine receptor, alpha 4 subunit) from Mus musculus.
Rdl is a homologue of Glra4 (glycine receptor, alpha 4) from Rattus norvegicus.
Rdl is a homologue of AgaP_AGAP006028 (AGAP006028-PA) from Anopheles gambiae str. PEST.
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