ST 1535: a preferential A2A adenosine receptor antagonist.
作者： Maria Antonietta Stasi , Franco Borsini , Katia Varani , Fabrizio Vincenzi , Maria Assunta Di Cesare
DOI: 10.1017/S1461145705006188
关键词:
摘要: Antagonism of the A2A adenosine function has proved beneficial in treatment Parkinson's disease, that it increases L-dopa therapeutical effects without concomitant worsening its side-effects. In this paper we describe a preferential antagonist, ST 1535, with long-lasting pharmacodynamic effects. It competitively antagonizes agonist NECA on cAMP cells cloned human receptor (IC50=353+/-30 nM), and A1 CHA (IC50=510+/-38 nM). at oral doses 5 10 mg/kg, catalepsy induced by intracerebroventricular administration CGS 21680 (10 microg/5 microl) mice. At ranging between 20 1535 induces hypermotility haloperidol-induced mice up to 7 h. Oral 1.25 2.5 potentiates reducing catalepsy. represents potential new compound, activity, for disease.
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