BIMU 8 是 5-HT4 的选择性激动剂,对野生型 5HT4 受体、T3.36A 和 W6.48A 突变体 5-HT4 的 EC50 分别为 18 nM、77 nM 和 540 nM。
产品描述
BIMU 8 is a selective agonist of 5-HT4 with EC50s of 18 nM, 77 nM, and 540 nM for wild-type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4.
体外活性
BIMU 8 (0.003-0.1 μM) increases excitatory postsynaptic potentials amplitude without changing the membrane potential of any neuron in myenteric neurons of guinea pig ileum[1].
体内活性
BIMU 8 (20-30 mg/kg s.c. and 60 mg/kg p.o. in mice; 20 mg/kg i.p. in rats), produces significant antinociception. In mice, BIMU 8 (10 μg; i.c.v) which is largely ineffective by parenteral routes induces antinociception[2].
Cas No.
134296-40-5
分子式
C19H27ClN4O2
分子量
378.9
别名
BIMU 8
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years