An adenosine A2A receptor antagonist
货号:ajcx23520
CAS:496955-42-1
分子式:C12H16N8
分子量：272.3
溶解度:DMF: 5mg/mL,DMSO: 5mg/mL,DMSO:PBS (pH 7.2) (1:9): 0.1mg/mL
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ST1535 is an adenosine A_2Areceptor antagonist.¹It is selective for adenosine A_2Aover A₁receptors (K_is = 2.3 and 107 nM, respectively, in radioligand binding assays). ST1535 inhibits agonist-induced production of cAMP in CHO cells expressing adenosine A_2Areceptors (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 .²ST1535 (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)