2-butyl-9-methyl-8-(triazol-2-yl)purin-6-amine

ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease[1][2].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

A2a adenosine receptor

ST 1535 (0-1000 nM) 抑制 CHO 细胞中 forskolin (HY-15371) 诱导的 cAMP 的形成，对 hA1, hA2A, hA2B, hA3 的 IC50 值分别为 510, 353, 950, >1000 nM[1]。

ST 1535 (0, 5, 10 mg/kg; 口服) 拮抗 A2A 腺苷激动剂 CGS 21680 (HY-13201) (i.c.v.) 诱发的僵直症[1]。 ST 1535 (10、20、40 mg/kg；腹腔注射) 增加在大鼠中 l-DOPA (HY-N0304) 引起的对侧转动次数[2]。 Animal Model: 5-6 weeks CD1 male mice[1] Dosage: 0, 5, 10 mg/kg Administration: P.o. Result: Antagonized catalepsy induced by i.c.v. administration with the A2A adenosine agonist CGS 21680. Animal Model: Male Sprague Dawley rats[2] Dosage: 10, 20, 40 mg/kg Administration: I.p. Result: Significantly increased the number of contralateral turns induced by l-DOPA (3 mg/kg i.p.) at 20 and 40 mg/kg.

[1]. Stasi MA, et al. ST 1535: a preferential A2A adenosine receptor antagonist. Int J Neuropsychopharmacol. 2006 Oct;9(5):575-84.  

[2]. Tronci E, et al. Characterization of the antiparkinsonian effects of the new adenosine A2A receptor antagonist ST1535: acute and subchronic studies in rats. Eur J Pharmacol. 2007 Jul 2;566(1-3):94-102.