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Titolo:
PHARMACOLOGICAL CHARACTERIZATION OF NOVEL A(3) ADENOSINE RECEPTOR-SELECTIVE ANTAGONISTS
Autore:
JACOBSON KA; PARK KS; JIANG JL; KIM YC; OLAH ME; STILES GL; JI XD;
Indirizzi:
NIDDK,MOL RECOGNIT SECT,LBC,NIH BETHESDA MD 20892 DUKE UNIV,SCH MED,DEPT MED DURHAM NC 27710 DUKE UNIV,SCH MED,DEPT PHARMACOL DURHAM NC 27710
Titolo Testata:
Neuropharmacology
fascicolo: 9, volume: 36, anno: 1997,
pagine: 1157 - 1165
SICI:
0028-3908(1997)36:9<1157:PCONAA>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
TUMOR-NECROSIS-FACTOR; FACTOR-ALPHA; CEREBRAL-ISCHEMIA; MOLECULAR-CLONING; TNF-ALPHA; DERIVATIVES; CELLS; RAT; EXPRESSION; PROTEIN;
Keywords:
DIHYDROPYRIDINE; FLAVONOID; TRIAZOLOQUINAZOLINE; ADENYLATE CYCLASE; TUMOR NECROSIS FACTOR; GUANINE NUCLEOTIDES; ADENOSINE A(3) RECEPTOR; ADENOSINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
40
Recensione:
Indirizzi per estratti:
Citazione:
K.A. Jacobson et al., "PHARMACOLOGICAL CHARACTERIZATION OF NOVEL A(3) ADENOSINE RECEPTOR-SELECTIVE ANTAGONISTS", Neuropharmacology, 36(9), 1997, pp. 1157-1165

Abstract

The effects of putative A(3) adenosine receptor antagonists of three diverse chemical classes (the flavonoid MRS 1067, the 6-phenyl-1,4-dihydropyridines MRS 1097 and MRS 1191, and the triazoloquinazoline MRS 1220) were characterized in receptor binding and functional assays. MRS1067, MRS 1191 and MRS 1220 were found to be competitive in saturation binding studies using the agonist radioligand [I-125]AB-MECA amino-3-iodobenzyl)adenosine-5'-N-methyluronamide) at cloned human brain A(3)receptors expressed in HEK-293 cells. Antagonism was demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of [S-35]guanosine 5'-O-(3-thiotriphosphate) ([S-35]GTP-gamma-S) to the associated G-proteins. MRS 1220 and MRS 1191, with K-B values of 1.7 and 92 nM, respectively, proved to be highly selective for human A(3) receptor vs human A(1) receptor-mediated effects on adenylate cyclase. In addition, MRS 1220 reversed the effect of A(3) agonist-elicited inhibition of tumor necrosis factor-alpha formation in the human macrophage U-937 cell line, with anIC50 value of 0.3 mu M. Published by Elsevier Science Ltd.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/11/20 alle ore 02:00:50