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Product Name:BIMU 8
CAS:134296-40-5
Purity:98% HPLC Package:5mg;10mg;25mg;50mg;100mg;250mg;500mg;1g
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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 Basic information |
| Product 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: | (endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide;BIMU-8;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;BIMU8 hydrate;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;N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-3-propan-2-ylbenzimidazole-1-carboxamide,hydrochloride;inhibit,5-hydroxytryptamine Receptor,Inhibitor,5-HT Receptor,antidepressant,BIMU-8,Serotonin Receptor,BIMU8,antinociception,BIMU 8,5-HT4,EPSP | | CAS: | 134296-40-5 | | MF: | C19H26N4O2.HCl | | MW: | 0 | | EINECS: | | | Product Categories: | | | Mol File: | 134296-40-5.mol |  |
| | (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 |
| storage temp. | 2-8°C | | solubility | H2O: ≥5mg/mL | | form | solid | | color | off-white to light tan |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26 | | WGK Germany | 3 |
| | (endo-N-8-methyl-8-azabicyclo-(3.2.1)oct-3-yl)-2,3-dihydro-3-isopropyl-2-oxo-1H-benzimidazol-1-carboxamide Usage And Synthesis |
| 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 |
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