Description
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 . BIMU 8 significantly decreased the K+ current in colliculi neurons. This suggested a 5-HT4 receptor-mediated effect . 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 . 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 .
Product information
CAS Number: 134296-40-5
Molecular Weight: 378.90
Formula: C19H27ClN4O2
Chemical Name: N-[(1R,3S,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-3-(propan-2-yl)-2,3-dihydro-1H-1,3-benzodiazole-1-carboxamide hydrochloride
Smiles: Cl.CN1[C@@H]2C[C@H](C[C@H]1CC2)NC(=O)N1C2=CC=CC=C2N(C(C)C)C1=O
InChiKey: NQYXXIUVFVOJCX-NFWSUKNGSA-N
InChi: InChI=1S/C19H26N4O2.ClH/c1-12(2)22-16-6-4-5-7-17(16)23(19(22)25)18(24)20-13-10-14-8-9-15(11-13)21(14)3;/h4-7,12-15H,8-11H2,1-3H3,(H,20,24);1H/t13-,14+,15-;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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