An adenosine A2A receptor antagonist
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 .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
1.Stasi, M.A., Borsini, F., Varani, K., et al.ST 1535: a preferential A2A adenosine receptor antagonistInt. J. Neuropsychopharmacol.9(5)575-584(2006) 2.Tronci, E., Simola, N., Borsini, F., et al.Characterization of the antiparkinsonian effects of the new adenosine A2A receptor antagonist ST1535: acute and subchronic studies in ratsEur. J. Pharmacol.566(1-3)94-102(2007) 3.Rose, S., Jackson, M.J., Smith, L.A., et al.The novel adenosine A2a receptor antagonist ST1535 potentiates the effects of a threshold dose of L-DOPA in MPTP treated common marmosetsEur. J. Pharmacol.546(1-3)82-87(2006)
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