Bethanechol-d6 is intended for use as an internal standard for the quantification of bethanechol by GC- or LC-MS. Bethanechol is an agonist of muscarinic acetylcholine receptors with IC50 values of 1,837, 25, 631, 317, and 393 µM for M1-5, respectively, in a radioligand binding assay using CHO cells expressing the human receptors.1 It inhibits M2-mediated increases in cyclic AMP induced by isoproterenol in isolated guinea pig small intestine (IC50 = 127 µM).2 Bethanechol increases basal tone of isolated porcine intravesical ureter (EC50 = 4.27 µM).3 It also induces fluid secretion in the ileum, duodenum, and jejunum of anesthetized rats when administered at a dose of 60 µg/kg.4 Formulations containing bethanechol have been used to increase urination and improve smooth muscle tone in the gastrointestinal tract.
1.Richards, M.H., and van Giersbergen, P.L.Human muscarinic receptors expressed in A9L and CHO cells: Activation by full and partial agonistsBr. J. Pharmacol.114(6)1241-1249(1995) 2.Okamoto, H., Prestwich, S.A., Asai, S., et al.Muscarinic agonist potencies at three different effector systems linked to the M2 or M3 receptor in longitudinal smooth muscle of guinea-pig small intestineBr. J. Pharmacol.135(7)1765-1775(2002) 3.HernÁndez, M., SÍmonsen, U., Prieto, D., et al.Different muscarinic receptor subtypes mediating the phasic activity and basal tone of pig isolated intravesical ureterBr. J. Pharmacol.110(4)1413-1420(1993) 4.Young, A., and Levin, R.J.Intestinal hypersecretion of the refed starved rat: A model for alimentary diarrhoeaGut33(8)1050-1056(1992)