BIMU 8

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.(In Vitro):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.(In Vivo):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.

In myenteric neurons of guinea pig ileum, BIMU 8 (0.003-0.1 μM) increases excitatory postsynaptic potentials (EPSPs) mplitude but does not change the membrane potential of any neuron.

In mice and rats, 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. Intracerebroventricular injection in mice of BIMU 8 (10 μg/mouse), doses which are largely ineffective by parenteral routes, induces an antinociception whose intensity equaled that obtainable s.c., i.p. or p.o.

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Endocrinology/Hormones

5-HT Receptor

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134296-40-5

378.9

C19H27ClN4O2

>98% (HPLC)

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C(N[C@H]1C[C@@H]2N(C)[C@H](C1)CC2)(=O)N3C=4C(N(C(C)C)C3=O)=CC=CC4.Cl

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(-20℃)

With Ice Pack

≥ 2 years