Overview
- Bolden, C. et al. (1992) J. Pharmacol. Exp. Ther. 260, 576.
- Sudo, Y. et al. (1999) Life Sci. 64, PL99.
- Brocks, D.R. (1999) J. Pharm. Pharmaceut. Sci. 2, 39.
Alomone Labs Biperiden hydrochloride inhibits carbachol’s effect on M1 mAChR expressed in C6 cells.Cells were loaded with Fluo-3 AM and changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following application. A. Normalized fluorescence following application (arrow) of 10 μM Carbachol without (control) and with 10 or 100 μM Biperiden hydrochloride (#B-115), as indicated. B. Inhibition of 10 μM Carbachol effect, plotted against Biperiden hydrochloride concentrations.
Muscarinic acetylcholine receptors (mAChR) regulate a number of important basic physiologic functions including heart rate, motor and sensory control and more complex behaviors including arousal, memory, and learning. Loss of muscarinic receptor number or function has been implicated in the etiology of several neurological disorders including Alzheimer's dementia, Down's syndrome, and Parkinson's disease. Five subtypes of muscarinic receptors (m1-m5) have been identified by molecular cloning1 and much has been learned about their distribution, pharmacology, and structure2.
Biperiden hydrochloride is a non-selective muscarinic receptor antagonist that displays selectivity for the M1 subtype (Ki values are 0.48, 2.4, 3.9, 6.3 and 6.3 nM for M1, M4, M3, M2 and M5 receptors respectively)3-4. It is antiparkinsonian5 and therefore used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arteriosclerotic), also commonly used to improve parkinsonian signs and symptoms related to antipsychotic drug therapy6.
