M4 Muscarinic Acetylcholine Receptors Antibodies
Functionally, M4-muscarinic receptors are able to couple to the pertusiss toxin-sensitive Gi/o proteins. M4-muscarinic receptor knockout animals show locomotor phenotypes. In fact, M4 receptors are thought to mediate an inhibitory affect on striatal dopamine-mediated locomotor activity. M4 agonists might be beneficial in schizophrenia and antagonists are likely to be of benefit in Parkinson's disease. M4 receptor activity is regulated by phosphorylation of serine296/serine297 and threonine311/serine314 in the 3rd intracellular loop. This nomenclature refers to the human M4 but is highly conserved in mice and rats. For more information on M4 receptor pharmacology please refer to the IUPHAR database. For further reading refer to:
Caulfield MP, Birdsall NJ. International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors. Pharmacol Rev. 1998 Jun;50(2):279-90. PMID: 9647869.
Wess J, Eglen RM, Gautam D. Muscarinic acetylcholine receptors: mutant mice provide new insights for drug development. Nat Rev Drug Discov. 2007 Sep;6(9):721-33. doi: 10.1038/nrd2379. PMID: 17762886.
Birdsall NJM, Bradley S, Brown DA, Buckley NJ, Challiss RJ, Christopoulos A, Eglen RM, Ehlert F, Felder CC, Hammer R, Kilbinger HJ, Lambrecht G, Langmead C, Mitchelson F, Mutschler E, Nathanson NM, Schwarz RD, Thal D, Tobin AB, Valant C, Wess J. Acetylcholine receptors (muscarinic) in GtoPdb v.2021.3. IUPHAR/BPS Guide to Pharmacology CITE. 2021; 2021(3).