BIMU 8

BIMU 8 is an agonist of the serotonin (5-HT) receptor subtype 5-HT₄ (K_i = 69 nM).¹ It also binds 5-HT₃ receptors (K_i = 0.36 nM). It stimulates cAMP formation in primary mouse embryonic colliculi neurons with an EC₅₀ value of 72 nM.² BIMU 8 (30, 40, and 60 nmol/animal, i.c.v.) induces acetylcholine release in the rat frontal cortex.³ It increases postprandial antral and colonic motility in conscious dogs when administered at doses of 0.1, 0.3, and 1 mg/kg.⁴ BIMU 8 (20 mg/kg, i.p.) also increases the latency to withdraw in the paw pressure test in rats.⁵

WARNING This product is not for human or veterinary use.

1. Schiavi, G.B., Brunet, S., Rizzi, C.A., et al. Identification of serotonin 5-HT₄ recognition sites in the porcine caudate nucleus by radioligand binding. Neuropharmacology 33(3-4), 543-549 (1994).

2. Dumuis, A., Sebben, M., Monferini, E., et al. Azabicycloalkyl benzimidazolone derivatives as a novel class of potent agonists at the 5-HT₄ receptor positively coupled to adenylate cyclase in brain. Naunyn Schmiedebergs Arch. Pharmacol. 343(3), 245-251 (1991).

3. Consolo, S., Arnaboldi, S., Giorgi, S., et al. 5-HT₄ receptor stimulation facilitates acetylcholine release in rat frontal cortex. Neuroreport 5(10), 1230-1232 (1994).

4. Mine, Y., Yoshikawa, T., Oku, S., et al. Comparison of effect of mosapride citrate and existing 5-HT₄ receptor agonists on gastrointestinal motility in vivo and in vitro. J. Pharmacol. Exp. Ther. 283(3), 1000-1008 (1997).

5. Ghelardini, C., Galeotti, N., Casamenti, F., et al. Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8. Life Sci. 58(25), 2297-2309 (1996).