BIMU 8

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。

CAS号

134296-40-5

分子式

C19H27ClN4O2

主要靶点

5-HT Receptor

仅限科研使用

Cat No : CM19342

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Synonyms



产品信息

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.

CAS号 134296-40-5
分子式 C19H27ClN4O2
主要靶点 5-HT Receptor
主要通路 神经科学|G蛋白偶联受体
分子量 378.9
纯度 99.36%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

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].

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].

溶解度

DMSO:45 mg/mL (118.76 mM)

参考文献

1.H Pan , et al. 5-HT1A and 5-HT4 receptors mediate inhibition and facilitation of fast synaptic transmission in enteric neurons. Am J Physiol. 1994 Feb;266(2 Pt 1):G230-8.
2.C Ghelardini, et al. Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8. Life Sci. 1996;58(25):2297-309.
3.Lucie P Pellissier, et al. Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors. Mol Pharmacol. 2009 Apr;75(4):982-90.

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