BIMU 8 |
| Catalog No.GC14925 |
BIMU 8은 야생형 5HT4 수용체, T3.36A 및 W6.48A 돌연변이 5-HT4 수용체에 대해 EC50이 18 nM, 77 nM 및 540 nM인 강력하고 선택적인 5-HT4 작용제입니다.
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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 | |
| Chemical Name | 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 | ||
| Formula | C19H26N4O2.HCl | M.Wt | 378.9 |
| Solubility | <37.89mg/ml in DMSO; <28.42mg/ml in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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