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Titolo:
THE UNUSUAL BINDING-PROPERTIES OF THE ENDOTHELIN RECEPTOR ANTAGONIST CGS-27830 DISTINGUISHES RECEPTOR AGONIST INTERACTIONS/
Autore:
CHIN MH; CIOFFI CL; GARAY M; NEALE RF; SHETTY SS; DELGRANDE D; MUGRAGE B; SILLS MA; LIPSON KE;
Indirizzi:
CIBA GEIGY CORP,RES DEPT,DIV PHARMACEUT,556 MORRIS AVE SUMMIT NJ 07901 CIBA GEIGY CORP,RES DEPT,DIV PHARMACEUT SUMMIT NJ 07901
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 1, volume: 276, anno: 1996,
pagine: 74 - 83
SICI:
0022-3565(1996)276:1<74:TUBOTE>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT-BRAIN; LIGAND; MEMBRANES; SUBTYPES; AGONIST; SITES; RADIOLIGAND; IRL-1620; POTENT; ACID;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
46
Recensione:
Indirizzi per estratti:
Citazione:
M.H. Chin et al., "THE UNUSUAL BINDING-PROPERTIES OF THE ENDOTHELIN RECEPTOR ANTAGONIST CGS-27830 DISTINGUISHES RECEPTOR AGONIST INTERACTIONS/", The Journal of pharmacology and experimental therapeutics, 276(1), 1996, pp. 74-83

Abstract

CGS 27830 ycarbonyl-2,6-dimethyl-4-(3-nitrophenyl)3-pyridine carboxylic acid anhydride] is a nonpeptidic, insurmountable, endothelin (ET) receptor antagonist with approximately 10- to 20-fold selectivity for ET(A) receptors. CGS 27830 exhibits unusual binding properties which depend on the receptor and ligand: standard saturation binding experiments (coincubation of membranes with ligand in the absence or presence of antagonist) suggest that CGS 27830 is a competitive inhibitor of [I-125]IRL 1620 binding to ET(B) receptors in rat cerebellar membranes (i.e., there was a change of apparent K-d with no change of maximum binding), but a noncompetitive inhibitor of [I-125]IRL 1620 binding to ET(B) receptors in rat lung membranes (i.e., significant loss of total binding was observed). Although the antagonist appears to be a noncompetitive inhibitor of [I-125]IRL 1620 binding to ET(B) receptors in rat lung membranes, CGS 27830 appears to be a competitive inhibitor of [I-125]ET-1 binding to the same receptors as well as to ET(A) receptors inA7r5 cell membranes. Thus, CGS 27830 can distinguish [I-125]IRL 1620 binding to ET(B) receptors in rat cerebellar and lung membranes, but not ET-1 binding to ET(B) receptors in these tissues. These unusual binding properties demonstrate that rat lung and cerebellum ET(B) receptors interact differently with IRL 1620 or ET-1.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 11/07/20 alle ore 13:40:08