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Titolo:
INHIBITION BY 5-HT OF FORSKOLIN-INDUCED CAMP FORMATION IN THE RENAL OPOSSUM EPITHELIAL-CELL LINE OK - MEDIATION OF A 5-HT1B LIKE RECEPTOR AND ANTAGONISM BY METHIOTHEPIN
Autore:
PAUWELS PJ; PALMIER C;
Indirizzi:
CTR RECH PIERRE FABRE,CELLULAR NEUROBIOL LAB,17 AVE JEAN MOULIN F-81106 CASTRES FRANCE
Titolo Testata:
Neuropharmacology
fascicolo: 1, volume: 33, anno: 1994,
pagine: 67 - 75
SICI:
0028-3908(1994)33:1<67:IB5OFC>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
ADENYLATE-CYCLASE; 5-HYDROXYTRYPTAMINE1B RECEPTOR; SEROTONIN RECEPTOR; MOLECULAR-CLONING; HUMAN-BRAIN; SUBTYPE; AUTORECEPTORS;
Keywords:
5-HYDROXYTRYPTAMINE RECEPTOR AGONISTS/ANTAGONISTS; BETA-ADRENERGIC RECEPTOR ANTAGONISTS; ADENYLATE CYCLASE; RENAL OK CELLS; 5-HT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
33
Recensione:
Indirizzi per estratti:
Citazione:
P.J. Pauwels e C. Palmier, "INHIBITION BY 5-HT OF FORSKOLIN-INDUCED CAMP FORMATION IN THE RENAL OPOSSUM EPITHELIAL-CELL LINE OK - MEDIATION OF A 5-HT1B LIKE RECEPTOR AND ANTAGONISM BY METHIOTHEPIN", Neuropharmacology, 33(1), 1994, pp. 67-75

Abstract

The functional activity of various 5-HT receptor agonists, including 5-CT, sumatriptan, CP 93, 129 and 1-naphtylpiperazine, and of drugs known to bind with high affinity to 5-HT1B (pindolol, propranolol, cyanopindolol, SDZ 21,009 and isamoltane) or 5-HT1D binding sites (yohimbine and rauwolscine) was measured at 5-HT receptors that are negatively coupled to adenylate cyclase in cultures of the renal epithelial cell line OK. 5-HT receptor-mediated inhibition of adenylate cyclase was studied by measuring inhibition of cAMP formation, induced by 100 mu M forskolin. Besides 5-HT, various other compounds with affinity for 5-HTreceptors behaved as agonists with the following rank order of potency: RU 24,969 > 5-CT > dihydroergotamine = 5-HT > CP 93,129 > d-LSD > 1-naphtylpiperazine > sumatriptan > TFMPP = mCPP > CGS 12066B = metergoline > methysergide. The beta-adrenergic receptor blockers cyanopindolol, SDZ 21,009 (-)-pindolol and (-)-propranolol, and the alpha(2)-adrenergic blockers yohimbine and rauwolscine yielded agonist. Methiothepin was the only compound that antagonised the OK cell 5-HT receptor hasproperties consistent with a 5-HT1B receptor, although differences are apparent with regard to potencies of some compounds. Methiothepin isprobably the only effective antagonist at 5-HT1B receptor sites, whereas the described putative 5-HT1B receptor antagonists have to be considered as partial agonists, yielding agonist or antagonist activity depending on the system that is studied.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 31/03/20 alle ore 05:09:27