货号 | 1363/50 |
别名 | (2-Amino-4,5-dimethyl-3-thienyl)-[3 |
供应商 | Tocris |
生物活性 | Allosteric potentiator at the adenosine A1 receptor; acts via agonist-dependent and -independent mechanisms. Enhances agonist affinity for, and increased t½ of dissociation from, the receptor. Also inhibits basal and forskolin-stimulated adenylyl cyclase (AC) activity in A1 receptors expressed in CHO cells, possibly via direct potentiation of constitutive receptor activity or by direct inhibition of AC. Active in vivo. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >99 % |
计算分子量 | 299.31 |
分子式 | C14H12F3NOS |
可溶性/溶解性 | Soluble to 100 mM in ethanol and to 100 mM in DMSO |
CAS号 | 132861-87-1 |
参考文献 | Musseret al (1999) Adenosine A1 receptor-dependent and -independent effects of the allosteric enhancer PD 81,723. J.Pharmacol.Exp.Ther. 288 446. PMID: 9918544. Kollias-Bakeret al (1997) Agonist-independent effect of an allosteric enhancer of the A1 adenosine receptor in CHO cells stably expressing the recombinant human A1 receptor. J.Pharmacol.Exp.Ther. 281 761. PMID: 9152383. Mizumuraet al (1996) PD 81,723, an allosteric enhancer of the A1 adenosine receptor, lowers the threshold for ischemic preconditioning in dogs. Circ.Res. 79 415. PMID: 8781475. Brunset al (1990) Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes. Mol.Pharmacol. 38 950. PMID: 2250667. |