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Titolo:
THE ANXIOLYTIC SEROTONIN 5-HT1A RECEPTOR AGONISTS BUSPIRONE, IPSAPIRONE AND GEPIRONE ARE INHIBITORS OF TYROSINE HYDROXYLATION IN RAT STRIATUM
Autore:
JOHNSON EA; FOX JL; AZZARO AJ;
Indirizzi:
W VIRGINIA UNIV,ROBERT C BYRD HLTH SCI CTR W VIRGINIA,DEPT BEHAV MED & PSYCHIAT,POB 9137 MORGANTOWN WV 26506 W VIRGINIA UNIV,ROBERT C BYRD HLTH SCI CTR W VIRGINIA,DEPT NEUROL MORGANTOWN WV 26506 W VIRGINIA UNIV,ROBERT C BYRD HLTH SCI CTR W VIRGINIA,DEPT PHARMACOL & TOXICOL MORGANTOWN WV 26506
Titolo Testata:
Behavioural brain research
fascicolo: 1-2, volume: 73, anno: 1995,
pagine: 331 - 335
SICI:
0166-4328(1995)73:1-2<331:TAS5RA>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
DOPAMINE; SITES; BRAIN; BINDING;
Keywords:
TYROSINE HYDROXYLATION; BUSPIRONE; IPSAPIRONE; GEPIRONE; ANXIOLYTICS; STRIATUM; 5-HT1A RECEPTOR; SYNAPTOSOME;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Science Citation Index Expanded
Citazioni:
14
Recensione:
Indirizzi per estratti:
Citazione:
E.A. Johnson et al., "THE ANXIOLYTIC SEROTONIN 5-HT1A RECEPTOR AGONISTS BUSPIRONE, IPSAPIRONE AND GEPIRONE ARE INHIBITORS OF TYROSINE HYDROXYLATION IN RAT STRIATUM", Behavioural brain research, 73(1-2), 1995, pp. 331-335

Abstract

The anxiolytics buspirone (BUS), ipsapirone (IPSAP) and gepirone (GEP) were investigated as 5-HT1A receptor-mediated inhibitors of tyrosinehydroxylation (TH) in a synaptosome-rich preparation of rat striatum. BUS, IPSAP and GEP were moderately potent inhibitors of TH with EC(50) values of 48.4 mu M, 50 mu M and 836 mu M, respectively. By comparison, 8-OH-DPAT, a 5-HT1A receptor selective agonist, has been previously shown to be more potent with an EC(50) value of 7.0 mu M. Each of these agents demonstrated full agonist activity at the striatal 5-HT1A receptors regulating TH. The inhibitory effects of each agent were attenuated by prior exposure to the 5-HT1A antagonist NAN-190, (10 mu M) (P<0.05), but not by the dopamine D-2 antagonist (-)-sulpiride (10 mu M). The potencies of 8-OH-DPAT, BUS, IPSAP and GEP were correlated withtheir reported affinities for the 5-HT1A receptor (P<0.01) but not the dopamine D-2 receptor. These results support the hypothesis that BUS, IPSAP and GEP inhibit TH through activation of a striatal 5-HT1A heteroreceptor on dopamine nerve terminals.

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Documento generato il 30/03/20 alle ore 17:57:44