货号 | 2214/50 |
别名 | 2-[[4-(2-Pyridinyl)-1-piperazinyl]m |
供应商 | Tocris |
生物活性 | Potent dopamine D4 receptor partial agonist (EC50 = 12.4 nM; 61% efficacy vs. dopamine). Has no agonist activity at D2 receptors (EC50 > 10 μM). Selective in rats in vivo; produces penile erection following i.c.v. administration; increases intracavernosal pressure and potentiates the proerectile effects of sildenafil following s.c. administration. Displays minimal side effects. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 402.75 |
分子式 | C17H19N5.3HCl |
可溶性/溶解性 | Soluble to 100 mM in water |
CAS号 | 70006-24-5 |
参考文献 | Brioniet al (2004) Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats. Proc.Natl.Acad.Sci.USA 1016758. Cowartet al (2004) Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction. J.Med.Chem. 47 3853. PMID: 15239663. Stewartet al (2004) Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning. J.Med.Chem. 47 2348. PMID: 15084133. |