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Titolo:
CP-154,526 - A POTENT AND SELECTIVE NONPEPTIDE ANTAGONIST OF CORTICOTROPIN-RELEASING FACTOR RECEPTORS
Autore:
SCHULZ DW; MANSBACH RS; SPROUSE J; BRASELTON JP; COLLINS J; CORMAN M; DUNAISKIS A; FARACI S; SCHMIDT AW; SEEGER T; SEYMOUR P; TINGLEY FD; WINSTON EN; CHEN YL; HEYM J;
Indirizzi:
PFIZER INC,DEPT NEUROSCI GROTON CT 06340
Titolo Testata:
Proceedings of the National Academy of Sciences of the United Statesof America
fascicolo: 19, volume: 93, anno: 1996,
pagine: 10477 - 10482
SICI:
0027-8424(1996)93:19<10477:C-APAS>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
CENTRAL NERVOUS-SYSTEM; ADENYLATE-CYCLASE ACTIVITY; CEREBROSPINAL-FLUID; MAJOR DEPRESSION; BETA-ENDORPHIN; LOCUS-CERULEUS; NORADRENERGIC NEURONS; HEMODYNAMIC STRESS; ACOUSTIC STARTLE; CUSHINGS-DISEASE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
48
Recensione:
Indirizzi per estratti:
Citazione:
D.W. Schulz et al., "CP-154,526 - A POTENT AND SELECTIVE NONPEPTIDE ANTAGONIST OF CORTICOTROPIN-RELEASING FACTOR RECEPTORS", Proceedings of the National Academy of Sciences of the United Statesof America, 93(19), 1996, pp. 10477-10482

Abstract

Here we describe the properties of CP-154,526, a potent and selectivenonpeptide antagonist of corticotropin (ACTH) releasing factor (CRF) receptors. CP-154,526 binds with high affinity to CRF receptors (K-i <10 nM) and blocks CRF-stimulated adenylate cyclase activity in membranes prepared from rat cortex and pituitary. Systemically administered CP-154,526 antagonizes the stimulatory effects of exogenous CRF on plasma ACTH, locus coeruleus neuronal firing and startle response amplitude. Potential anxiolytic activity of CP-154,526 was revealed in a fear-potentiated startle paradigm. These data are presented in the contextof clinical findings, which suggest that CRF is hypersecreted in certain pathological states. We propose that a CRF antagonist such as CP-154,526 could affirm the role of CRF in certain psychiatric diseases and may be of significant value in the treatment of these disorders.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 12:41:44