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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . C Ghelardini, et al. Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8. Life Sci. 1996;58(25):2297-309.  [Content Brief]

  . 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.  [Content Brief]

  . 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.  [Content Brief]