BIMU 8

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 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].