Denise G. Denter, Nicolas Heck, Therese Riedemann, Robin White, Werner Kilb, Heiko J. Luhmann,
... gated channels. To examine the functional role of GABAC receptors in radial migration we analyzed the effects of specific GABAA and GABAC receptor antagonists on the migration of BrdU-labeled neurons ... antagonist picrotoxin both impeded migration, suggesting that the GABAC receptor mediated effects dominate. Addition of the specific GABAC receptor agonist cis-4-aminocrotonic acid (CACA) also hampered ... function. RT-PCR experiments using specific probes for GABAC receptor mRNA and Western blot assays using an antibody ...
Tópico(s): Neuroscience and Neural Engineering
2010 - Elsevier BV | Neuroscience
Neil J. Harrison, Sarah C. R. Lummis,
... acid, type A (GABAA) receptors, of which the GABAC receptor family is a subgroup, are members of the ... or close to the binding site of the GABAC receptor (Arg-104, Arg-170, Arg-158, and Arg- ... acid, type A (GABAA) receptors, of which the GABAC receptor family is a subgroup, are members of the ... or close to the binding site of the GABAC receptor (Arg-104, Arg-170, Arg-158, and Arg- ... via both ionotropic (GABAA) and metabotropic (GABAB) receptors. GABAC receptors are a subfamily of GABAA receptors and are ... GABAA receptors because of their distinct pharmacological properties; GABAC receptor-mediated responses are not inhibited by bicuculline (the ...
Tópico(s): Phenothiazines and Benzothiazines Synthesis and Activities
2006 - Elsevier BV | Journal of Biological Chemistry
Graham A.R. Johnston, Mary Chebib, Jane R. Hanrahan, Kenneth N. Mewett,
GABAC receptors are the least studied of the three major classes of GABA receptors. The physiological roles of GABAC receptors are still being unravelled and the pharmacology of ... of agents has been described that act on GABAC receptors with varying degrees of specificity as agonists, partial ... are known to exist between subtypes of cloned GABAC receptors that have been cloned from mammalian sources. There is evidence for functional GABAC receptors in the retina, spinal cord, superior colliculus, pituitary ...
Tópico(s): Nicotinic Acetylcholine
2003 - Bentham Science Publishers | Current Drug Targets - CNS & Neurological Disorders
... 11: 112– 116. Bormann J, Feigenspan A. 1995. GABAC receptors. Trends Neurosci 18: 515– 519. Bormann J, Rundström ... Enz R, Cutting GR. 1998. Molecular composition of GABAC receptors. Vision Res 38: 1431– 1441. Enz R, Brandstätter ... H, Bormann J. 1996. Immunocytochemical localization of the GABAC receptor ρ subunits in the mammalian retina. J Neurosci ... Wässle H. 1998. Different contributions of GABAA and GABAc receptors to rod and cone bipolar cells in a ... cells are presynaptic to rod bipolar cells through GABAC receptors. J Comp Neurol 413: 155– 167. Fletcher EL, ...
Tópico(s): Photoreceptor and optogenetics research
2000 - Wiley | Microscopy Research and Technique
Davide Ragozzino, Richard M. Woodward, Y. Murata, Fabrizio Eusebi, Larry E. Overman, Ricardo Miledi,
... classes, which are denoted GABAA, GABAB, and GABAC. GABAC receptors are defined by their insensitivity to the GABAA ... antagonist bicuculline and the GABAB receptor agonist (-)-baclofen. GABAC receptors probably are a heterogeneous group of proteins. The most extensively studied mammalian GABAC receptors are those found in neurons of the outer ... are two subtypes. The physiological functions served by GABAC receptors are largely unknown; to determine the functions, it ... a GABAB-selective agonist, show affinity for retinal GABAC receptors. In particular, 3-APMPA is an antagonist with ...
Tópico(s): Nicotinic Acetylcholine
1996 - American Society for Pharmacology and Experimental Therapeutics | Molecular Pharmacology
Mélanie Rose, Eva Dütting, Nadja Schröder, Heinrich Sticht, Johann Helmut Brandstätter, Ralf Enz,
... 1 (PP1) as a new binding partner of GABAC receptors. In the mammalian retina, PNUTS is co-expressed with GABAC receptors and PP1 in bipolar cells. PNUTS and PP1 ... protein preparations of the retina and precipitate with GABAC receptor specific antibodies. Furthermore, PNUTS shuttles from the nucleus to the membrane in cells co-expressing GABAC receptors. We show simultaneous binding of PP1 and GABAC receptors to different domains of PNUTS, demonstrating that PNUTS cross-links PP1 and GABAC receptors. Finally, modeling studies showed that the PP1 docking ...
Tópico(s): Neuroscience and Neuropharmacology Research
2008 - Elsevier BV | Molecular and Cellular Neuroscience
Jahanshah Αmin, David S. Weiss,
... effects of the ginkgolides at recombinant human ρ1 GABAC receptors, Neuropharmacology, 10.1016/j.neuropharm.2012.06.067, ... 2011) Subunit-specific polyclonal antibody targeting human ρ1 GABAC receptor, Experimental Eye Research, 10.1016/j.exer.2011. ... D and Chang Y (2005) Mapping the ρ1 GABAC Receptor Agonist Binding Pocket, Journal of Biological Chemistry, 10. ... Online publication date: 1-Nov-2002. Enz R GABAC Receptors: A Molecular View, Biological Chemistry, 10.1515/BC. ... is a determinant of the response kinetics of GABAC receptors, Journal of Neurobiology, 10.1002/(SICI)1097-4695( ...
Tópico(s): Neuroscience and Neuropharmacology Research
1996 - Royal Society | Proceedings of the Royal Society B Biological Sciences
Katja Schlicker, Mathias Boller, M. Schmidt,
In the dorsal lateral geniculate nucleus (dLGN), GABAC receptors seems to be specifically expressed by local GABAergic interneurons. Although the presence of GABAC receptors has been demonstrated, a quantitative estimation of their ... blocked by co-application of TPMPA, a specific GABAC receptor antagonist, or picrotoxin, an unspecific GABAA and GABAC receptor blocker. The latter neurons were also sensitive to the selective GABAC receptor agonist cis-aminocrotonic acid. These results indicate that in those dLGN neurons that express GABAC receptors, these receptors contribute considerably to GABAergic inhibitory inputs.
Tópico(s): Neuroendocrine regulation and behavior
2004 - Elsevier BV | Brain Research Bulletin
Peter D. Lukasiewicz, Erika D. Eggers, Botir T. Sagdullaev, Maureen A. McCall,
... ganglion cells and is mediated, in part, by GABAC receptors. We investigated GABAC receptor-mediated inhibition using pharmacological approaches and genetically altered mice that lack GABAC receptors. Responses to applied GABA showed distinct time courses ... classes, attributable to different proportions of GABAA and GABAC receptors. The elimination of GABAC receptors in GABAC null mice reduced and shortened GABA- ... in GABAC null mice. These data suggest that GABAC receptors determine the time course and extent of inhibition ...
Tópico(s): Photoreceptor and optogenetics research
2004 - Elsevier BV | Vision Research
Byung-Hwan Lee, Sun-Hye Choi, Sung-Hee Hwang, Hyeon-Joong Kim, Joon‐Hee Lee, Seung-Yeol Nah,
... of 5-HT3A receptors. The γ-aminobutyric acidC (GABAC) receptor is mainly expressed in retinal bipolar cells and ... of resveratrol on the channel activity of homomeric GABAC receptor expressed in Xenopus oocytes injected with cRNA encoding ... peak current (IGABA ) in oocytes that express the GABAC receptor. Resveratrol treatment had no effect on oocytes injected with H2O or with GABAC receptor cRNA. Co-treatment with resveratrol and GABA inhibited IGABA in oocytes with GABAC receptors. The inhibition of IGABA by resveratrol was in ...
Tópico(s): Photoreceptor and optogenetics research
2013 - The Korean Society of Pharmacology | Korean Journal of Physiology and Pharmacology
Shifeng Li, Yunbin Zhang, Haixiong Liu, Yuanchang Yan, Yiping Li,
... or GABA. Here, we report the presence of GABAC receptor in rat testis and spermatozoa. Full-length complementary ... encoding the ρ1, ρ2 and ρ3 subunits of GABAC receptor were cloned from rat testis; their sequences are identical to those of rat GABAC receptor in retina. Reverse transcription-polymerase chain reaction analysis ... analysis using an anti-ρl antibody revealed that GABAC receptor exists on the elongated spermatid and sperm. Using ... we found that N(4)-chloroacetylcytosine arabinoside, a GABAC receptor agonist, triggered rat sperm acrosome reaction; whereas (1, ...
Tópico(s): RNA Interference and Gene Delivery
2008 - Oxford University Press | Acta Biochimica et Biophysica Sinica
S.E. Clark, Maurice Garret, Bettina Platt,
... GABAB receptor (R1a and R1b splice variants), and GABAC receptor ρ1 subunit expression and distribution in the superficial, ... GABAB receptors (R1a and R1b splice variants) and GABAC receptors (ρ1 subunit) showed similar patterns. Both receptors could ... after birth. When slices were double labelled for GABAC receptors and neurofilament, some overlap was observed. Double labelling for the presynaptic protein synaptophysin and GABAC receptors showed proximity in some places, indicative of a partly synaptic location of GABAC receptors. When GABAC and GABAA receptors were labelled simultaneously, ...
Tópico(s): Nicotinic Acetylcholine
2001 - Elsevier BV | Neuroscience
Produção Nacional
Revisado por pares
Gláucia Maria Lopes Reis, Igor Dimitri Gama Duarte,
... potassium channel blockers on the antinociception induced by GABAC receptor agonist CACA (cis-4-aminocrotonic acid) using the ... effect when injected in the contralateral paw. The GABAC receptor antagonist (1,2,5,6 tetrahydropyridin-4-yl) ... CACA. This study provides evidence that activation of GABAC receptors in the periphery induces antinociception, that this effect results from the activation of chloride channel coupled GABAC receptors and that potassium channels appear not to be ...
Tópico(s): Botulinum Toxin and Related Neurological Disorders
2007 - Elsevier BV | Life Sciences
... receptors, defined as baclofen-sensitive, bicuculline-insensitive receptors. GABAC receptors that are bicuculline-insensitive, baclofen-insensitive, linked to ... CAMP) may represent one such class of receptors. GABAC receptors may be more widespread in insects and bacteria ... of the nervous system, such as the retina. GABAC receptors may represent receptors that subsequently evolved into GABAA ... but not all of the pharmacological properties of GABAC receptors as deduced from electrophysiological and neurochemical studies on ...
Tópico(s): Neuroscience and Neuropharmacology Research
1994 - Elsevier BV | Progress in brain research
Andreas Feigenspan, Joachim Bormann,
GABAA and GABAC receptors were studied on cultured or freshly isolated rat retinal bipolar cells. The cells displayed GABA-induced whole-cell ... was ∼ 2 for both receptors. The bicuculline-insensitive GABAC receptors were markedly blocked by 100 μM picrotoxinin, 2-( ... GABAA receptors, respectively. The pore diameter of open GABAC receptor channels was 5.1 Å, i.e. close ... pharmacologically distinct GABA receptors, GABAA and novel-type GABAC receptors, which might subserve different physiological functions in controlling ...
Tópico(s): Ion channel regulation and function
1994 - Elsevier BV | European Journal of Pharmacology Molecular Pharmacology
Gurpreet S. Ratra, Brian E. Erkkila, David S. Weiss, John E. Casida,
... brain on binding to the GABAA receptor. The GABAC receptor, important in retina and present in brain, is ... radioligand binding and electrophysiological experiments. Human homomeric ρ1 GABAC receptor expressed in human embryonic kidney cells (HEK293) undergoes ... does not consider ρ2 homomeric and ρ1ρ2 heteromeric GABAC receptors which are known to be more sensitive than ... The inhibitor sensitivity and specificity of this ρ1 GABAC receptor differ greatly from those of human homomeric β3 ...
Tópico(s): Ion channel regulation and function
2002 - Elsevier BV | Toxicology Letters
... Based on their homology to nicotinic acetylcholine receptors, GABAC receptors are believed to be oligomeric protein complexes composed ... pentameric arrangement. To date up to five different GABAC receptors subunits have been identified in various species. Recent ... shed new light on the biological characteristics of GABAC receptors, including the chromosomal localization of its subunit genes ... data in view of the molecular structure of GABAC receptors and presents new insights into the biological function ...
Tópico(s):
2001 - De Gruyter | Biological Chemistry
Ming‐Hu Han, Ying Li, Xiong-Li Yang,
BICUCULLINE and baclofen-insensitive GABA receptors (GABAC receptors) on bipolar cells acutely dissociated from carp retina were investigated with using the whole-cell patch-clamp recording technique. The currents of these cells mediated by GABAC receptors showed striking desensitization, even at low concentrations of ... of desensitization were significantly different from that of GABAC receptors previously observed in other retinas and elsewhere in the CNS, suggesting that the GABAC receptors of carp bipolar cells might be distinct in ...
Tópico(s): Ion channel regulation and function
1997 - Lippincott Williams & Wilkins | Neuroreport
... the release of several hormones via different receptors. GABAC receptors are heterooligomers that differ from GABAA receptors in ... molecular and functional evidence for the presence of GABAC receptors outside the retina has yet to be established. ... In contrast to the Cl− current generated by GABAC receptors in the retina, the bicuculline-insensitive Cl− currents ... quickly desensitized. These results suggest that a novel GABAC receptor may regulate TSH secretion and that the structure ...
Tópico(s): Neuroscience and Neuropharmacology Research
2000 - Oxford University Press | Endocrinology
... any native GABA receptor, it is thought that GABAC receptors are homomeric assemblies of ρ–subunits. However, we ... perch retina did not resemble those of the GABAC receptors on perch bipolar cells. Because both GABAA and GABAC receptors are present on retinal bipolar cells, we attempted ... closely approximated the values obtained from the native GABAC receptors on bipolar cells. These results provide the first ... ρ–subunits contributes to the molecular organization of GABAC receptors in the retina and perhaps throughout the nervous ...
Tópico(s): Photoreceptor and optogenetics research
1999 - Royal Society | Proceedings of the Royal Society B Biological Sciences
... subunits are very similar to those exhibited by GABAC receptors and ρ subunits and GABAC responses have been ... that ρ subunits are the sole components of GABAC receptors. In contrast, the propensity of GABAA receptor and ... and their coexistence in retinal cells suggests that GABAC receptors might be heterooligomers of ρ and GABAA receptor ... our current understanding of the molecular composition of GABAC receptors based upon studies of ρ subunit assembly.
Tópico(s):
1998 - Elsevier BV | Vision Research
Jian Zhang, Malcolm M. Slaughter,
... selective agonist. This pharmacology is indicative of the GABAC receptor. 4. In voltage-clamp recordings of ganglion cells ... indicates that ganglion cells possess both GABAA and GABAC receptors. 5. The GABAC receptor current was relatively nondesensitized. Consequently, whereas the peak ... current was more than fivefold larger than the GABAC receptor current, after desensitization the latter current was larger. ...
Tópico(s): Photoreceptor and optogenetics research
1995 - American Physiological Society | Journal of Neurophysiology
Ataúlfo Martínez‐Torres, Ricardo Miledi,
GABAC receptors are part of the ligand-gated ion channel family of receptors that share some functional and ... segment is presumed to form the ion-channel. GABAC receptors open chloride channels and do not desensitize even ... a role in the process of desensitization of GABAC receptors, we used site-directed mutagenesis to produce several ... receptor that was antagonized by TPMPA, a specific GABAC receptor antagonist. Moreover, in contrast with wild-type rho1 ... study mechanisms involved in gating and desensitization of GABAC receptors in particular, and of neurotransmitter receptors in general.
Tópico(s): Nicotinic Acetylcholine
2004 - Elsevier BV | Archives of Medical Research
Virginia E. Wotring, Yongchang Chang, David S. Weiss,
1. Homomeric human rho1 GABAC receptors were expressed in Xenopus oocytes and in human embryonic kidney cells (HEK293) in order to examine their conductance and permeability. ... NO3-, Br- and HCO3- were higher for rho1 GABAC receptors than alpha1beta2gamma2L GABAA receptors. 4. Expression of rho1 GABAC receptors in Xenopus oocytes and in HEK293 cells gave ... 5. The pore diameter of the homomeric rho1 GABAC receptor expressed in oocytes was estimated to be 0. ... homomeric receptor may not be the native retinal GABAC receptor reported previously.
Tópico(s):
1999 - Wiley | The Journal of Physiology
... a decrease in Ca2+ concentrations. The role of GABAC receptors in retinotectal responses was also evaluated. GABAC receptor antagonists did not block the effects of melatonin ... studies have shown that in Xenopus tectal cells, GABAC receptors mediate inhibition, in retinotectal axons, the opposite appears ... calcium rises in retinotectal axons were inhibited by GABAC receptor blockade. This result suggests that activation of GABAC receptors produces an increase in the synaptic excitability of ...
Tópico(s): Neuroscience and Neuropharmacology Research
2005 - Elsevier BV | Brain Research
Mary Chebib, Robert J. Vandenberg, Wolfgang Froestl, Graham A.R. Johnston,
... analogues of γ-aminobutyric acid (GABA) are potent GABAC receptor antagonists but are even more potent as GABAB ... GABAB receptor phosphonoamino acid antagonists were tested on GABAC receptors in Xenopus oocytes expressing human retinal ϱ1 mRNA. ... antagonist, was found to be a moderately potent GABAC receptor antagonist (IC50 = 62 μM). The unsaturated methylphosphinic and ... analogues of GABA were competitive antagonists of the GABAC receptors, the order of potency being [(E)-3-aminopropen- ...
Tópico(s): Organophosphorus compounds synthesis
1997 - Elsevier BV | European Journal of Pharmacology
Kristin Hartmann, Frank Stief, Andreas Draguhn, Christiane Frahm,
... yl)methylphosphinic acid (TPMPA), a specific antagonist of GABAC receptors. This sensitivity was enhanced when we evoked the currents by the GABAC receptor agonist cis-4-aminocrotonic acid (CACA). However, both ... bicuculline and thus lack the defining feature of GABAC receptors, which are insensitive towards this antagonist. Spontaneous miniature ... with mixed pharmacological properties of both, GABAA and GABAC receptors.
Tópico(s): Ion channel regulation and function
2004 - Elsevier BV | European Journal of Pharmacology
Maria Grazia Zizzo, Flavia Mulè, Rosa Serio,
... Tetrahydropyridin-4-yl)methylphosphinic acid hydrate (TPMPA), a GABAC-receptor antagonist and it was not affected by phaclofen, ... atropine. Cis-4-aminocrotonic acid (CACA), a specific GABAC receptor agonist, induced an inhibitory effect, consisting in the ... and muscular relaxation, which was antagonised by TPMPA, GABAC-receptor antagonist, TTX or Nω-nitro-l-arginine methyl ... release of ACh from excitatory cholinergic neurons, and GABAC receptors increasing the release of NO from non-adrenergic, ...
Tópico(s): Ion Channels and
2007 - Elsevier BV | Neuropharmacology
... of zinc on the gamma-aminobutyric acid-C (GABAC) receptor in acutely isolated catfish cone horizontal cells using ... cell patch-clamp technique. 2. GABA activates the GABAC receptor with a half-activation concentration (EC50) of 2. ... concentration is > 3 microM. 3. Zinc downmodulates the GABAc receptor current, elicited by 30 microM GABA, with a ... voltage independent. 6. These results suggest that the GABAC receptor of horizontal cells can be modulated by endogenous ...
Tópico(s): Neuroscience and Neuropharmacology Research
1995 - American Physiological Society | Journal of Neurophysiology
Tadashi Kusama, Kouji Hatama, Kiyoshige Saito, Yasuo Kizawa, Hajime Murakami,
... gated currents in Xenopus oocytes expressing human ρ1 GABAC receptors. To investigate whether the inhibition of currents was ... in efficacy or in the potency of ρ1 GABAC receptor, concentration-response curves for GABA were compared before ... for GABA. To allow histochemical detection of ρ1 GABAC receptors, we constructed a receptor tagged at the C- ... and PMA as those of wild-type ρ1 GABAC receptors. Immunohistochemistry with anti-myc antibody detected a dense ... protein kinase C leads to internalization of ρ1 GABAC receptors expressed in Xenopus oocytes.
Tópico(s): Nicotinic Acetylcholine
2000 - Physiological Society of Japan | The Japanese Journal of Physiology