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Titolo:
A NON PEPTIDIC CORTICOTROPIN-RELEASING FACTOR-RECEPTOR ANTAGONIST ATTENUATES FEVER AND EXHIBITS ANXIOLYTIC-LIKE ACTIVITY
Autore:
LUNDKVIST J; CHAI Z; TEHERANIAN R; HASANVAN H; BARTFAI T; JENCK F; WIDMER U; MOREAU JL;
Indirizzi:
UNIV STOCKHOLM,DEPT NEUROCHEM & NEUROTOXICOL,SVANTE ARRHENIUS VAG 21AS-10691 STOCKHOLM SWEDEN UNIV STOCKHOLM,DEPT NEUROCHEM & NEUROTOXICOL S-10691 STOCKHOLM SWEDEN F HOFFMANN LA ROCHE & CO LTD,PRECLIN CNS RES,DIV PHARMA CH-4002 BASELSWITZERLAND
Titolo Testata:
European journal of pharmacology
fascicolo: 2, volume: 309, anno: 1996,
pagine: 195 - 200
SICI:
0014-2999(1996)309:2<195:ANPCFA>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT-BRAIN; NERVOUS-SYSTEM; FACTOR CRF; SECRETION; IDENTIFICATION; LOCALIZATION; CLONING; STRESS;
Keywords:
CRF (CORTICOTROPIN-RELEASING FACTOR); ANXIETY; INTERLEUKIN-1-BETA; FEVER; CRF RECEPTOR ANTAGONIST;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
23
Recensione:
Indirizzi per estratti:
Citazione:
J. Lundkvist et al., "A NON PEPTIDIC CORTICOTROPIN-RELEASING FACTOR-RECEPTOR ANTAGONIST ATTENUATES FEVER AND EXHIBITS ANXIOLYTIC-LIKE ACTIVITY", European journal of pharmacology, 309(2), 1996, pp. 195-200

Abstract

The multiple actions of corticotropin-releasing factor (CRF) on neuroendocrine and behavioural functions can now be examined using new, high affinity, non peptidic antagonists which exhibit central activity upon systemic application. We have shown that compound CP 154,526 thylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amine) displaces [I-125][Tyr(0)]CRF from rat hippocampal CRF receptors (IC50 = 0.5 nM) and from pituitary CRF receptors (IC50 = 0.04 nM). The same compound inhibits in a concentration-dependent manner the ovine CRF (0.1 mu M)-stimulated adenylate cyclase activity in membranes of a mouse pituitary adenoma cell line, AtT20, with an IC50 value of 50 nM. Systemic application of the CRF receptor antagonist (0.16 mg/kg i.p.) blocked recombinant human interleukin-1 beta (5 mu g/kg i.p.) induced fever in rats. The CRF receptor antagonist CP 154,526 (1 mg/kg i.p.) also exhibited signs of anxiolytic-like activity in the elevated plus-maze test in rats.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 15:57:38