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Titolo:
DEVELOPMENT OF 5-HT1A RECEPTOR ANTAGONISTS
Autore:
ROUTLEDGE C;
Indirizzi:
SMITHKLINE BEECHAM PHARMACEUT,DEPT PSYCHIAT RES,NEW FRONTIERS SCI PK N,3RD AVE HARLOW CM19 5AD ESSEX ENGLAND
Titolo Testata:
Behavioural brain research
fascicolo: 1-2, volume: 73, anno: 1995,
pagine: 153 - 156
SICI:
0166-4328(1995)73:1-2<153:DO5RA>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSTSYNAPTIC 5-HT(1A) RECEPTORS; SELECTIVE ANTAGONIST; BRAIN MICRODIALYSIS; RAT HIPPOCAMPUS; AGONIST; NAN-190; INVIVO; (S)-5-FLUORO-8-HYDROXY-2-(DIPROPYLAMINO)TETRALIN; 8-HYDROXY-2-(DI-NORMAL-PROPYLAMINO)TETRALIN; 8-HYDROXY-2-(DI-N-PROPYLAMINO)TETRALIN;
Keywords:
5HT(1A) RECEPTOR ANTAGONISTS; SOMATODENDRITIC 5HT(1A) RECEPTOR; WAY100635;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
C. Routledge, "DEVELOPMENT OF 5-HT1A RECEPTOR ANTAGONISTS", Behavioural brain research, 73(1-2), 1995, pp. 153-156

Abstract

The discovery that non-benzodiazepine anxiolytic agents such as buspirone bind with high affinity to the 5-HT1A receptor has stimulated thedevelopment of selective 5-HT1A receptor ligands as potential drug candidates. However, the lack of selective 5-HT1A receptor antagonists has hampered the elucidation of the mechanism of action of these agents, indeed, it is still unclear whether buspirone exerts its anxiolytic effects via an agonist action at presynaptic (somatodendritic) or an antagonist action at postsynaptic 5-HT1A receptors. Ligands that have been used previously to define the 5-HT1A receptor are either son-selective or have agonist activity at the presynaptic 5-HT1A receptor. It is only in the past three years that selective and silent 5-HT1A receptor antagonists have emerged. This overview compares the profiles of the first selective 5-HT1A receptor antagonists in models of pre- and postsynaptic 5-HT1A receptor function. In addition, it highlights some of the problems associated with the development of selective 5-HT1A receptor antagonists.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/04/20 alle ore 17:47:19