您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > BIMU 8
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
BIMU 8
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BIMU 8图片
CAS NO:134296-40-5
包装与价格：
包装价格(元)
5mg电议
25mg电议

产品介绍
BIMU 8 是一种有效的选择性 5-HT4 激动剂，对野生型 5HT4 受体、T3.36A 和 W6.48A 突变型 5-HT4 受体的 EC50 分别为 18 nM、77 nM 和 540 nM。
Cas No.134296-40-5
化学名3-isopropyl-N-((1R,3r,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazole-1-carboxamide hydrochloride
Canonical SMILESO=C(N1C2=CC=CC=C2N(C(C)C)C1=O)N[C@H]3C[C@@H]4N(C)[C@H](C3)CC4.Cl
分子式C19H26N4O2.HCl
分子量378.9
溶解度<37.89mg/ml in DMSO;<28.42mg/ml in Water
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BIMU 8 is an agonist of 5-HT4 with Ki values of 33.9 ± 8.0 nM and 12.6 ± 0.9 nM in guinea pig ileum and striatum, respectively [1, 2].

As a member of the seven transmembrane spanning G-protein-coupled family of receptors, the 5-HT4 receptor is positively coupled to adenylate cyclase. It exists in two isoforms (5-HT4S and 5-HT4L). These two isoforms differ in the sequence and length of their carboxy termini [3].

BIMU 8 significantly decreased the K+ current in colliculi neurons. This suggested a 5-HT4 receptor-mediated effect [4]. In neurons, BIMU 8 at concentrations ranging from 0.003-0.1 μM increased EPSP amplitude but did not change membrane potential. The EPSP potentiation induced by BIMU 8 was blocked by tropisetron (1 μM), a 5-HT3/5-HT4 receptor antagonist. But ondansetron (1 μM), a 5-HT3 receptor antagonist did not blocked the EPSP potentiation induced by BIMU 8 [5].

In the hot-plate test, BIMU 8 injected i.p. in the range of doses of 20-30 mg/kg significantly induced an increase in the pain threshold. 15 min after administration, the antinociceptive effect reached a maximum and hence diminished. This effect disappeared within 45 min. Choline uptake blocker HC-3 (1 μg per mouse i.c.v.), antimuscarinic drug atropine (5 mg/kg i.p.), 5-HT4 antagonists SDZ 205-557 (10 mg/kg i.p.) and GR 125487 (20 mg/kg i.p.) completely prevented the antinociception of BIMU 8 [1].

References:
[1].  Ghelardini C, Galeotti N, Casamenti F, et al. Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8. Life sciences, 1996, 58(25): 2297-2309.
[2].  Yoshikawa T, Yoshida N, Mine Y, et al. Affinity of mosapride citrate, a new gastroprokinetic agent, for 5-HT4 receptors in guinea pig ileum. The Japanese Journal of Pharmacology, 1998, 77(1): 53-59.
[3].  Hegde SS, Eglen RM. Peripheral 5-HT4 receptors. The FASEB journal, 1996, 10(12): 1398-1407.
[4].  Fagni L, Dumuis A, Sebben M, et al. The 5-HT4 receptor subtype inhibits K+ current in colliculi neurones via activation of a cyclic AMP-dependent protein kinase. British journal of pharmacology, 1992, 105(4): 973-979.
[5].  Pan H, Galligan JJ. 5-HT1A and 5-HT4 receptors mediate inhibition and facilitation of fast synaptic transmission in enteric neurons. American Journal of Physiology-Gastrointestinal and Liver Physiology, 1994, 266(2): G230-G238.