BIMU 8
目录号 : GC14925
A 5-HT4 receptor agonist
Cas No.:134296-40-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 134296-40-5 | SDF | |
| 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 SMILES | O=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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6392 mL | 13.1961 mL | 26.3922 mL |
| 5 mM | 0.5278 mL | 2.6392 mL | 5.2784 mL |
| 10 mM | 0.2639 mL | 1.3196 mL | 2.6392 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet