For research use only. Not for therapeutic Use.
BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors[1][2].
In myenteric neurons of guinea pig ileum, BIMU 8 (0.003-0.1 µM) increases excitatory postsynaptic potentials (EPSPs) mplitude but does not change the membrane potential of any neuron[3].
In mice and rats, BIMU 8 (20-30 mg/kg s.c. and 60 mg/kg p.o. in mice; 20 mg/kg i.p. in rats), produces significant antinociception.
Intracerebroventricular injection in mice of BIMU 8 (10 μg/mouse), doses which are largely ineffective by parenteral routes, induces an antinociception whose intensity equaled that obtainable s.c., i.p. or p.o[1].
| Catalog Number | M106984 |
| CAS Number | 134296-40-5 |
| Synonyms | N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-3-propan-2-ylbenzimidazole-1-carboxamide;chloride |
| Molecular Formula | C19H26ClN4O2- |
| Purity | ≥95% |
| 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/p-1/t13?,14-,15+; |
| InChIKey | NQYXXIUVFVOJCX-XZPOUAKSSA-M |
| SMILES | CC(C)N1C2=CC=CC=C2N(C1=O)C(=O)NC3CC4CCC(C3)N4C.[Cl-] |
| Reference | [1]. C Ghelardini, et al. Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8. Life Sci. 1996;58(25):2297-309. [2]. Lucie P Pellissier, et al. Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors. Mol Pharmacol. 2009 Apr;75(4):982-90. [3]. H Pan , et al. 5-HT1A and 5-HT4 receptors mediate inhibition and facilitation of fast synaptic transmission in enteric neurons. Am J Physiol. 1994 Feb;266(2 Pt 1):G230-8. |
