BIMU 8

Names

[ Name ]:
BIMU 8

[Synonym ]:
BIMU8
N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-3-propan-2-ylbenzimidazole-1-carboxamide hydrochloride

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT4 Receptor:18 nM (EC50)

T3.36A-5-HT4:77 nM (EC50)

W6.48A-5-HT4:540 nM (EC50)

[In Vitro]

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 Vivo]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₂₇ClN₄O₂

[ Molecular Weight ]:
378.89600

[ Exact Mass ]:
378.18200

[ PSA ]:
62.76000

[ LogP ]:
3.51110

MSDS

Click to get detail MSDS

Related Compounds

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