Name | 2-butyl-9-methyl-8-(triazol-2-yl)purin-6-amine |
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Synonyms | st-1535 |
Description | 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]. |
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Related Catalog | |
Target |
A2a adenosine receptor |
In Vitro | 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]。 |
In Vivo | 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. |
References |
Molecular Formula | C12H16N8 |
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Molecular Weight | 272.30900 |
Exact Mass | 272.15000 |
PSA | 100.33000 |
LogP | 1.45000 |