Solabegron(GW427353)是β3肾上腺素能受体(β3-AR)的选择性激动剂,在中国仓鼠卵巢细胞中测得的EC50值为22nM。目前正在被用于开发治疗膀胱过度活跃和肠易激综合征。
CAS：252920-94-8
分子式：C23H23ClN2O3
分子量：410.89
纯度：98%
存储：Store at -20°C

Background:

Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM[1]. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome[1]. EC50: 22 nM (β3-AR in cells)[1].

Solabegron (GW427353) at 3 mg/kg i.v. evokes an increase in micturition volume threshold that prevented the acetic acid-evoked decreases in dogs. The low dose (1 mg/kg) shows no significant activity[1]. Animal Model: Adult female beagle dogs (6-10 kg)[1].

[1]. Hicks A, et al. GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. J Pharmacol Exp Ther. 2007 Oct;323(1):202-9. [2]. Andersson KE, et al. Selective β3-adrenoceptor agonists for the treatment of overactive bladder. J Urol. 2013 Oct;190(4):1173-80.