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Titolo:
BINDING-AFFINITY OF ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS AT HUMAN CLONED A(3) ADENOSINE RECEPTORS
Autore:
VARANI K; CACCIARI B; BARALDI PG; DIONISOTTI S; ONGINI E; BOREA PA;
Indirizzi:
UNIV FERRARA,DEPT CLIN & EXPT MED,PHARMACOL UNIT,VIA FOSSATO MORTARA 17-19 I-44100 FERRARA ITALY UNIV FERRARA,DEPT CLIN & EXPT MED,PHARMACOL UNIT I-44100 FERRARA ITALY UNIV FERRARA,DEPT PHARMACEUT SCI I-44100 FERRARA ITALY CTR RIC SCHERING PLOUGH I-20132 MILAN ITALY
Titolo Testata:
Life sciences (1973)
fascicolo: 5, volume: 63, anno: 1998,
pagine: 81 - 87
SICI:
0024-3205(1998)63:5<81:BOARAA>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
SELECTIVE AGONISTS; POTENT; DERIVATIVES; NONXANTHINE;
Keywords:
ADENOSINE BINDING; HUMAN A(3) ADENOSINE RECEPTOR; A(2A) ADENOSINE RECEPTOR ANTAGONISTS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
20
Recensione:
Indirizzi per estratti:
Citazione:
K. Varani et al., "BINDING-AFFINITY OF ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS AT HUMAN CLONED A(3) ADENOSINE RECEPTORS", Life sciences (1973), 63(5), 1998, pp. 81-87

Abstract

The A(3) adenosine receptor is one of the four adenosine receptors which have thus far been identified. Cloning of the A(3) receptor from animal species such as rat, sheep and human has shown that there are interspecies differences in its peripheral distribution, and binding affinity for various adenosine receptor ligands. The adenosine derivative, 4-aminobenzyl-5'-N-methylcarboxamidoadenosine (AB-MECA), is a potentA(3) receptor agonist which is used as a reference drug. In this report we have characterized the binding of selected adenosine receptor agonists and antagonists to HEK 293 cells transfected with the human A(3) adenosine receptor using [I-125]AB-MECA as radioligand. HE-NECA and NECA were the most potent compounds showing K-i values in the low nanomolar range, while the recently discovered non-xanthine A(2A) receptorantagonists ZM 241385, SCH 58261 and SCH 63390 showed affinity valuesin the micromolar range. These data further indicate the need to examine the affinity of new adenosine receptor ligands directly in human A(3) receptors. (C) 1998 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/04/20 alle ore 22:58:30