| CAS NO: | 134296-40-5 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 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 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℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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: |
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