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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.
WARNING This product is not for human or veterinary use.
1. Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells. J. Pharmacol. Exp. Ther. 260(2), 576-580 (1992).
2. Effects of the antiparkinsonian drug budipine on neurotransmitter release in central nervous system tissue in vitro. J. Pharmacol. Exp. Ther. 264(2), 889-898 (1993).
3. The antiparkinsonian drugs budipine and biperiden are use-
4. Drugs for Parkinson’s disease reduce tremor induced by physostigmine. Naunyn Schmiedebergs Arch. Pharmacol. 323(3), 205-210 (1983).