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Titolo:
Adenosine receptor ligands-recent developments part I. Agonists
Autore:
Muller, CE;
Indirizzi:
Univ Bonn, Inst Pharmaceut, D-5300 Bonn, Germany Univ Bonn Bonn Germany D-5300 onn, Inst Pharmaceut, D-5300 Bonn, Germany
Titolo Testata:
CURRENT MEDICINAL CHEMISTRY
fascicolo: 12, volume: 7, anno: 2000,
pagine: 1269 - 1288
SICI:
0929-8673(200012)7:12<1269:ARLDPI>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
POTENTIAL PARTIAL AGONISTS; A(1) RECEPTOR; BINDING-SITE; 2-CYCLOHEXYLMETHYLIDENEHYDRAZINOADENOSINE WRC-0470; BIOLOGICAL EVALUATION; ENDOGENOUS ADENOSINE; SELECTIVE AGONISTS; KINASE INHIBITORS; A(2A) RECEPTORS; A(2B) RECEPTOR;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
111
Recensione:
Indirizzi per estratti:
Indirizzo: Muller, CE Univ Bonn, Inst Pharmaceut, D-5300 Bonn, Germany Univ Bonn Bonn Germany D-5300 harmaceut, D-5300 Bonn, Germany
Citazione:
C.E. Muller, "Adenosine receptor ligands-recent developments part I. Agonists", CURR MED CH, 7(12), 2000, pp. 1269-1288

Abstract

Developments in the field of adenosine receptor (AR) agonists of the past years are presented and discussed. Four different AR subtypes, A(1), A(2A),A(2B), and Ag, have been cloned from different species including the humanreceptors. Recombinant ARs expressed in permanent mammalian cell lines have found wide application in the screening of new ligands. Considerable differences are observed among data from different laboratories, using recombinant receptors for the assays. Reevaluation of compounds at all four receptor subtypes has shown that agonists that were believed to be selective for either A(1) or A(2A) ARs may be potent Ag agonists and thus, nonselective. Potent and selective agonists for two of the AR subtypes, A(1) and A(3), have been developed. Truly selective A(2A) AR agonists, however, are presentlynot available. Potent or selective A(2B) agonists are still lacking. Sincethe treatment with AR agonists may lead to fast desensitization of the receptors, partial agonists, and indirect AR agonists, such as adenosine kinase inhibitors, or allosteric enhancers of adenosine binding, are being developed as site- and event-specific agents.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 08:56:00