Biperiden hydrochloride. Selective Antagonist of M1 Muscarinic Acetylcholine Receptors (mAChRs).
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 cloning and much has been learned about their distribution, pharmacology, and structure.
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).
It is antiparkinsonian 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 therapy.
G-Protein Coupled Receptor Ligands; Muscarinic Acetylcholine Receptor Ligands