Biperiden-d5 is intended for use as an internal standard for the quantification of biperiden by GC- or LC-MS. Biperiden is an antagonist of muscarinic acetylcholine receptors (mAChRs; IC50s = 0.48, 6.3, 3.9, 2.4, and 6.3 nM for M1-5 receptors, respectively).1 It increases spontaneous and electrically evoked dopamine release and electrically evoked acetylcholine (ACh) release from rabbit caudate nucleus slices preincubated with dopamine.2 Biperiden (10 µM) also inhibits NMDA-induced ACh release in rabbit caudate nucleus slices.3 Biperiden (0.01-1.0 mg/kg) reduces physostigmine-induced tremor in rats.4 Formulations containing biperiden have been used as an adjuvant treatment for Parkinson’s disease.
1.Bolden, C., Cusack, B., and Richelson, E.Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cellsJ. Pharmacol. Exp. Ther.260(2)576-580(1992) 2.Jackisch, R., Huang, H.Y., Reimann, W., et al.Effects of the antiparkinsonian drug budipine on neurotransmitter release in central nervous system tissue in vitroJ. Pharmacol. Exp. Ther.264(2)889-898(1993) 3.Jackisch, R., Kruchen, A., Sauermann, W., et al.The antiparkinsonian drugs budipine and biperiden are use-dependent (uncompetitive) NMDA receptor antagonistsEur. J. Pharmacol.264(2)207-211(1994) 4.GothÓni, P., Lehtinen, M., and Fincke, M.Drugs for Parkinson’s disease reduce tremor induced by physostigmineNaunyn Schmiedebergs Arch. Pharmacol.323(3)205-210(1983)