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ST1535 is an adenosine A2A receptor antagonist.1 It is selective for adenosine A2A over A1 receptors (Kis = 2.3 and 107 nM, respectively, in radioligand binding assays). ST1535 inhibits agonist-induced production of cAMP in CHO cells expressing adenosine A2A receptors (IC50 = 353 nM). In vivo, ST1535 (10 and 20 mg/kg) reduces haloperidol-induced catalepsy in mice. It reduces the number of jaw tremors in a rat model of Parkinsonian jaw tremors induced by tacrine (Item No. 70240).2 ST1535 (20 and 40 mg/kg) increases locomotor activity and reverses motor disabilities in a marmoset model of MPTP-induced Parkinson’s disease.3
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1. ST 1535: a preferential A2A adenosine receptor antagonist. Int. J. Neuropsychopharmacol. 9(5), 575-584 (2006).
2. Characterization of the antiparkinsonian effects of the new adenosine A2A receptor antagonist ST1535: acute and subchronic studies in rats. Eur. J. Pharmacol. 566(1-3), 94-102 (2007).
3. The novel adenosine A2a receptor antagonist ST1535 potentiates the effects of a threshold dose of L-