BIMU 8

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

inhibit|EPSP|5-HT Receptor|5HT Receptor|5-hydroxytryptamine Receptor|5-HT4|5HTReceptor|antidepressant|antinociception|BIMU 8|BIMU8|BIMU-8|Serotonin Receptor|Inhibitor



产品信息

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 | Shipping with blue ice.
别名 inhibit|EPSP|5-HT Receptor|5HT Receptor|5-hydroxytryptamine Receptor|5-HT4|5HTReceptor|antidepressant|antinociception|BIMU 8|BIMU8|BIMU-8|Serotonin Receptor|Inhibitor

体内活性

BIMU 8(小鼠经皮下给药20-30 mg/kg,经口给药60 mg/kg;大鼠经腹腔给药20 mg/kg)能显著产生镇痛效果。在小鼠中,通过脑室内给药10 μg的BIMU 8,尽管经肠道给药效果不明显,但依然能诱发镇痛作用[2]。

体外活性

BIMU 8(0.003-0.1 μM)在豚鼠回肠的肠神经元中增加兴奋性突触后电位的幅度,但不改变任何神经元的膜电位[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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The dilution calculator equation

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