CL 316243 disodium salt 是一种高选择性的 β3-肾上腺素能受体激动剂和抗肥胖剂。 CL 316243 二钠盐的选择性超过 β1 和β2 的 10,000 倍以上。 CL 316243 二钠盐导致小鼠血糖水平快速下降,并已用于研究棕色脂肪细胞的诱导和增加膳食肥胖小鼠模型的产热作用。
Nakamura Y, Sato T, Shiimura Y, Miura Y, Kojima M Biochem Biophys Res Commun, 2013;441(1):42-6. Efficacy of the β3-adrenergic receptor agonist CL-316243 on experimental bladder hyperflexia and detrusor instability in the rat. Woods et al. ...
There was an increase of MAO activity in WAT and BAT, but not in liver, of CL-treated rats while no change was detected in guinea pigs. These findings show that only rat adipocytes, which are β 3 -adrenergic-responsive, respond to chronic β 3 -AR agonist by an increase of GLUT4 ...
1.1第一代BETA3肾上腺素受体激动剂 该类药物中最常见的就是BRL26830A和CL316243，这两种化合物都可作用于啮齿类动物，进入啮齿类动物体内之后，可有效降低体重和脂肪含量，然而在临床试验中效果并不理想。在之后的研究中发现，虽然大鼠和人体的BETA3肾上腺素受体的氨基酸序列同源性在80%-90%，但是受体功能却有很大的...
Prolonged treatment with the β3-adrenergic agonist CL 316243 induces adipose tissue remodeling in rat but not in guinea pig: 1) fat store depletion and desensitization of β-adrenergic responses (2006). Prolonged treatment with the beta3-adrenergic agonist CL 316243 induces adipose tissue remodeling...