(endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide
- CAS No.
- 134296-40-5
- Chemical Name:
- (endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide
- Synonyms
- BIMU-8;BIMU8 hydrate;(endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide;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;inhibit,5-hydroxytryptamine Receptor,Inhibitor,5-HT Receptor,antidepressant,BIMU-8,Serotonin Receptor,BIMU8,antinociception,BIMU 8,5-HT4,EPSP;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 (1:1) hydrate
- CBNumber:
- CB31383684
- Molecular Formula:
- C19H26N4O2.HCl
- Molecular Weight:
- 0
- MDL Number:
- MFCD00903899
- MOL File:
- 134296-40-5.mol
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H315-H319-H335 | |||||||||
Precautionary statements | P261-P264-P271-P280-P302+P352-P305+P351+P338 | |||||||||
Hazard Codes | Xi | |||||||||
Risk Statements | 36/37/38 | |||||||||
Safety Statements | 26 | |||||||||
WGK Germany | 3 | |||||||||
NFPA 704 |
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(endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide price More Price(9)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | B4063 | BIMU8 hydrate ≥98% (HPLC) | 134296-40-5 | 5mg | $241 | 2024-03-01 | Buy |
Sigma-Aldrich | B4063 | BIMU8 hydrate ≥98% (HPLC) | 134296-40-5 | 25mg | $784 | 2021-12-16 | Buy |
Tocris | 4374 | BIMU8 ≥98%(HPLC) | 134296-40-5 | 5 | $115 | 2021-12-16 | Buy |
Tocris | 4374 | BIMU8 ≥98%(HPLC) | 134296-40-5 | 25 | $432 | 2021-12-16 | Buy |
Usbiological | 254766 | BIMU 8 | 134296-40-5 | 10mg | $460 | 2021-12-16 | Buy |
(endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide Chemical Properties,Uses,Production
Uses
BIMU 8 is a potent full agonist of SR-4.
Biological Activity
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].
storage
Store at +4°C
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.
(endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
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Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
EMMX Biotechnology LLC | 888-539-0666 | info@emmx.com | United States | 8449 | 60 |
BOC Sciences | -- | info@bocsci.com | USA | 0 | 65 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |
Energy Chemical | 021-58432009 400-005-6266 | marketing1@energy-chemical.com | China | 44843 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24018 | 58 |
Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 4164 | 58 |