Document Detail


Discriminative stimulus effects of zolpidem in squirrel monkeys: role of GABA(A)/alpha1 receptors.
MedLine Citation:
PMID:  12420154     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
RATIONALE: The discriminative stimulus effects of zolpidem in squirrel monkeys trained at doses greater than or equal to 3.0 mg/kg differ from those of conventional benzodiazepines (BZs), but the extent to which these effects reflect the selectivity of zolpidem for GABA(A)/alpha(1) receptors is not known. OBJECTIVES: The present study investigated the ability of GABA(A)/alpha(1)-preferring agonists to substitute for training doses of zolpidem greater than or equal to 3.0 mg/kg and the ability of GABA(A)/alpha(1)-preferring antagonists to block zolpidem's discriminative stimulus effects. METHODS: Squirrel monkeys were trained to discriminate intravenous injections of zolpidem (3.0 or 5.6 mg/kg) from saline and tested with BZ agonists differing in selectivity and efficacy at GABA(A)/alpha(1) receptors. Antagonism of the effects of zolpidem was studied using the GABA(A)/alpha(1)-preferring antagonists beta-carboline-3-carboxylate-t-butyl ester (beta-CCT) and 3-propyloxy-beta-carboline (3-PBC). RESULTS: Zolpidem and quazepam (GABA(A)/alpha(1)-preferring agonist) engendered full substitution for zolpidem, whereas CL 218,872 (GABA(A)/alpha(1)-preferring partial agonist) and the non-selective BZ agonists alprazolam and flunitrazepam engendered low and variable levels of zolpidem-lever responding (35-58%). Both beta-CCT and 3-PBC antagonized the discriminative stimulus effects of zolpidem in a surmountable fashion. CONCLUSIONS: Our findings provide evidence for a key role of GABA(A)/alpha(1) receptors in the discriminative stimulus effects of zolpidem at relatively high training doses, and suggest that selectivity and relatively high efficacy at GABA(A)/alpha(1) receptors is required for BZ agonists to reproduce these discriminative stimulus effects.
Authors:
James K Rowlett; Roger D Spealman; Snjezana Lelas; James M Cook; Wenyuan Yin
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, U.S. Gov't, P.H.S.     Date:  2002-11-06
Journal Detail:
Title:  Psychopharmacology     Volume:  165     ISSN:  0033-3158     ISO Abbreviation:  Psychopharmacology (Berl.)     Publication Date:  2003 Jan 
Date Detail:
Created Date:  2003-01-23     Completed Date:  2003-05-07     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  7608025     Medline TA:  Psychopharmacology (Berl)     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  209-15     Citation Subset:  IM    
Affiliation:
Harvard Medical School, New England Regional Primate Research Center, One Pine Hill Drive, Box 9102, Southborough, MA 01772-9102, USA. james_rowlett@hms.harvard.edu
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MeSH Terms
Descriptor/Qualifier:
Alprazolam / pharmacology
Animals
Anti-Anxiety Agents / pharmacology
Benzodiazepines*
Carbolines / pharmacology
Discrimination Learning / drug effects*,  physiology
Dose-Response Relationship, Drug
Flunitrazepam / pharmacology
GABA Agonists / pharmacology*
GABA Antagonists / pharmacology
Injections, Intravenous
Male
Pyridazines / pharmacology
Pyridines / pharmacology*
Receptors, GABA-A / agonists,  physiology*
Saimiri
Grant Support
ID/Acronym/Agency:
DA11792/DA/NIDA NIH HHS; DA13591/DA/NIDA NIH HHS; MH46851/MH/NIMH NIH HHS; RR00168/RR/NCRR NIH HHS
Chemical
Reg. No./Substance:
0/3-propoxy-beta-carboline; 0/Anti-Anxiety Agents; 0/Carbolines; 0/GABA Agonists; 0/GABA Antagonists; 0/Pyridazines; 0/Pyridines; 0/Receptors, GABA-A; 0/alpha1 subunit, GABA-A receptor; 12794-10-4/Benzodiazepines; 1622-62-4/Flunitrazepam; 28981-97-7/Alprazolam; 36735-22-5/quazepam; 66548-69-4/CL 218872; 82626-48-0/zolpidem; 93835-05-3/tert-butyl beta-carboline-3-carboxylate

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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