GABA ρ2 receptor pharmacological profile: GABA recognition site similarities to ρ1

Kusama, Tadashi; Wang, Tien Li; Guggino, William B.; Cutting, Garry R.; Uhl, George R.

doi:10.1016/0922-4106(93)90174-8

Cited by 79 publications

(57 citation statements)

References 4 publications

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“…; Kusama et al . ) while 3.0 mM toluene clustered with 20 μM CI‐966 (1‐[2‐[bis[4‐trifluoromethyl)phenyl]methoxy]ethyl]‐1,2,5,6‐tetrahydropyridine‐3‐carboxylic acid hydrochloride), a very potent and selective inhibitor of the GABA transporter 1 (GAT1) (Borden et al . ) and with 100 μM CACA (Fig.…”

Section: Resultsmentioning

confidence: 99%

Toluene inhalation in adolescent rats reduces flexible behaviour in adulthood and alters glutamatergic and GABAergic signalling

Furlong

Duncan

Corbit

et al. 2016

Journal of Neurochemistry

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Toluene is a commonly abused inhalant that is easily accessible to adolescents. Despite the increasing incidence of use, our understanding of its long-term impact remains limited. Here, we used a range of techniques to examine the acute and chronic effects of toluene exposure on glutameteric and GABAergic function, and on indices of psychological function in adult rats after adolescent exposure. Metabolomics conducted on cortical tissue established that acute exposure to toluene produces alterations in cellular metabolism indicative of a glutamatergic and GABAergic profile. Similarly, in vitro electrophysiology in Xenopus oocytes found that acute toluene exposure reduced NMDA receptor signalling. Finally, in an adolescent rodent model of chronic intermittent exposure to toluene (10 000 ppm), we found that, while toluene exposure did not affect initial learning, it induced a deficit in updating that learning when response-outcome relationships were reversed or degraded in an instrumental conditioning paradigm. There were also group differences when more effort was required to obtain the reward; toluene-exposed animals were less sensitive to progressive ratio schedules and to delayed discounting. These behavioural deficits were accompanied by changes in subunit expression of both NMDA and GABA receptors in adulthood, up to 10 weeks after the final exposure to toluene in the hippocampus, prefrontal cortex and ventromedial striatum; regions with recognized roles in behavioural flexibility and decision-making. Collectively, our data suggest that exposure to toluene is sufficient to induce adaptive changes in glutamatergic and GABAergic systems and in adaptive behaviour that may underlie the deficits observed following adolescent inhalant abuse, including susceptibility to further drug-use.

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Section: Resultsmentioning

confidence: 99%

Toluene inhalation in adolescent rats reduces flexible behaviour in adulthood and alters glutamatergic and GABAergic signalling

Furlong

Duncan

Corbit

et al. 2016

Journal of Neurochemistry

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“…Modulation of the GABA response by Zn 2+ has been extensively reported in various GABA receptor preparations (Smart and Constanti, 1990;Legendre and Westbrook, 1991;Smart et al, 1991;Smart, 1992;Kusama et al, 1993b;Calvo et al, 1994;Wang et al, 1994). Zinc strongly inhibits the GABA C responses in hybrid bass retinal bipolar cells without any effect on GABA A responses (Quian and Dowling, 1995) and in cone horizontal cells (Dong and Werblin, 1995).…”

Section: Pharmacological Characterization Of Gabainduced Responsementioning

confidence: 97%

A picrotoxin-resistant GABA-gated chloride channel receptor subtype in the cockroach central nervous system

Hue

1998

Arch. Insect Biochem. Physiol.

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γ‐Aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the cockroach central nervous system (CNS). Electrophysiological assays performed at cercal‐afferent giant‐interneuron (GI) synapses demonstrated that a biphasic (transient and stable phases) increase in membrane conductance, in response to long‐lasting (30‐s) neuropilar pressure microapplication of GABA, could be explained by the presence of two GABA‐operated chloride channel receptor subtypes in the postsynaptic membrane. The low stable membrane conductance increase, representing less than 30% of the maximum response, reached during the early transient phase, was not desensitized quickly. It was reproduced by neuropilar pressure microapplication of cis‐4‐aminocrotonic acid (CACA) and was not, as the fast phase, antagonized by bath application of 10μM picrotoxin (PTX). Imidazole‐4‐acetic acid (I‐4AA) and Zn2+ did not modulate GABA and CACA‐induced responses. Furthermore, a presynaptic target site for CACA, that modulates Ach release, was identified. Arch. Insect Biochem. Physiol. 37:231–238, 1998. © 1998 Wiley‐Liss, Inc.

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“…Recent studies have also examined ethanol effects on "ρ-type" (presumed GABAC) GABA receptors, Wick et al 1996). The GABA ρ receptor resembles the GABAA receptor in structure, but lacks many of the modulatory sites traditionally associated with GABA-gated chloride channels (Feiganspan et al 1993;Harrison et al 1993;Kusama et al 1993;Shimada et al 1992). It is beyond the scope of this review to discuss all of the studies that have examined alcohol-GABA A receptor interactions.…”

Section: Alcohol Effects On Ligand-gated Ion Channels: Pharmacologicamentioning

confidence: 99%

Alcohols and neurotransmitter gated ion channels: past, present and future

Lovinger

1997

Naunyn-Schmiedeberg's Arch Pharmacol

163

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The neurotransmitter-gated ion channels form a superfamily of neurotransmitter receptors specialized for recognizing transmitters and rapidly gating ion channels that are contained within the same holoprotein complex. A large body of research indicates that alcohols alter the function of this class of receptor at concentrations relevant to the intoxicating and anesthetic effects of the alcohols. In addition, studies have implicated several types of neurotransmitter-gated channels in intoxicating and anesthetic alcohol actions. All of the neurotransmitter-gated ion channels contain conserved features such as N-terminal ligand binding domains, hydrophobic membrane spanning domains and charged pore-lining domains. However, at least two, and possibly three families of receptors have been identified within the superfamily, including the nicotinic ACh-like receptors, the ionotropic glutamate receptors and the ATP-gated ion channels. This review will begin with a brief overview of the structural features of the different receptors, with an emphasis on comparing and contrasting features of the different families of neurotransmitter-gated channels. The emphasis will be mostly on the nicotinic-like receptors and the iGluRs, since more is known about these receptors than about other types of ligand-activated cation channels. The remainder of the review focuses on the latest studies aimed at determining the mechanism of alcohol actions on this superfamily of receptor-channels as well as the relationship between the molecular structure of these channels and the effects of alcohols on channel function. In addition, emerging directions for future study of these effects of alcohols and possible regions of the protein that may be altered during alcohol exposure are discussed.

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GABA ρ2 receptor pharmacological profile: GABA recognition site similarities to ρ1

Cited by 79 publications

References 4 publications

Toluene inhalation in adolescent rats reduces flexible behaviour in adulthood and alters glutamatergic and GABAergic signalling

Toluene inhalation in adolescent rats reduces flexible behaviour in adulthood and alters glutamatergic and GABAergic signalling

A picrotoxin-resistant GABA-gated chloride channel receptor subtype in the cockroach central nervous system

Alcohols and neurotransmitter gated ion channels: past, present and future

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