BIMU 8|134296-40-5|-陌孚医药/Medlife

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BIMU 8

目录号: PC11391 纯度: ≥98%

CAS No. :134296-40-5

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中文名称	BIMU 8
英文名称	BIMU 8
英文别名	1H-Benzimidazole-1-carboxamide,2,3-dihydro-N-[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]-3-(1-methylethyl)-2-oxo-,hydrochloride (1:1);(endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide;1H-Benzimidazole-1-carboxamide,2,3-dihydro-N-[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]-3-(1-methylethyl)-2-oxo-,hydroch;1H-Benzimidazole-1-carboxamide,2,3-dihydro-N-[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]-3...;BIMU 8;N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-3-propan-2-ylbenzimidazole-1-carboxamide,hydrochloride;1H-Benzimidazole-1-carboxamide, 2,3-dihydro-N-(8-methyl-8-azabicyclo(3.2.1)oct-3-yl)-3-(1-methylethyl)-2-oxo-, monohydrochloride, endo-;N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-3-(propan-2-yl)-2,3-dihydro-1H-benzimidazole-1-carboxamide hydrochloride (1:1);N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]-3-(1-methyl;BIMU8;BIMU-8;N-[(1R,5S)-8-Methyl-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-3-propan-2-ylbenzimidazole-1-carboxamide;hydrochloride;2,3-Dihydro-N-[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]-3-(1-methylethyl)-2-oxo-1H-benzimidazole-1-carboxamide hydrochloride;B7660;Q4835690;1H-Benzimidazole-1-carboxamide, 2,
Cas No.	134296-40-5
分子式	C₁₉H₂₇ClN₄O₂
分子量	378.90
包装储存	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

BIMU 8 is a potent and selective 5-HT4 agonist with EC₅₀s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors.

性状

Solid

IC50 & Target[1][2]

5-HT₄ Receptor

18 nM (EC₅₀)

T3.36A-5-HT4

77 nM (EC₅₀)

W6.48A-5-HT4

540 nM (EC₅₀)

体外研究(In Vitro)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[1]. C Ghelardini, et al. Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8. Life Sci. 1996;58(25):2297-309. [Information]

[2]. 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. [Information]

[3]. 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. [Information]

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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