Muscarinic Acetylcholine Family Related Drug Discovery Products
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
Acetylcholine (ACh), the first neurotransmitter to be discovered, binds to and activates two physically and functionally distinct groups of cell-surface receptors to produce its extensive range of physiological effects. These receptors are the nicotinic ACh receptors (nAChRs) and the muscarinic ACh receptors (mAChRs). The Brain has high concentrations of mAChRs, which regulate a wide range of neuronal activities. mAChRs have long been a focus of the drug discovery industry due to their roles in numerous CNS processes; nevertheless, the only mAChR ligands that have been licensed for use in the clinic are non-selective antagonists for the treatment of Parkinson's disease.
Fig.1 Overall structure of the M2 and M3 receptors. (Kruse, 2014)
To meet the needs of our customers, Creative Biolabs can offer muscarinic acetylcholine family in vitro assays and products to contribute to the success of muscarinic acetylcholine family drug discovery:
Muscarinic Acetylcholine GPCR Assays 
GPCR Assay Kits 
GPCR Cell Lines 
GPCR Membranes 
Membrane Protein Tools
Overview of Muscarinic Acetylcholine Family
The muscarinic acetylcholine receptors (mAChRs) are a family of class A G protein-coupled receptors (GPCRs). There are five different subtypes of the mAChR family, designated M1 to M5 (and encoded by the genes CHRM1 to CHRM5). The Gq/11 family of G proteins have been demonstrated to couple to three of these receptor subtypes (M1, M3, and M5), whilst the Gi/o family of G proteins have been shown to couple to the remaining two subtypes (M2 and M4). The major role of the mAChRs in human physiology includes controlling the heart rate, smooth muscle contraction, glandular secretion, and numerous other essential central nervous system processes. Whereas the M2 and M3 receptor subtypes are broadly distributed both in the Brain and in peripheral organs, the M1, M4, and M5 receptors are primarily expressed in the CNS. Typically, at least two or more mAChR subtypes are expressed by the majority of tissues and cell types.
Fig.2 Subclassification of mAChRs. (Wess, 2007)
Muscarinic Acetylcholine Family Drug Discovery
One of the most well-studied subfamilies of G protein-coupled receptors, the mAChRs are abundantly expressed in the central nervous system. Their various functions in regulating neuronal function make them appealing therapeutic targets for a variety of CNS diseases. While the literature has long documented the significance of mAChRs in AD, Parkinson's disease, and—to a lesser extent—schizophrenia, more recent research has indicated that blocking the M5 mAChR may be an effective strategy for treating drug addiction and dependence. Again, the ability to build antagonists that exhibit appropriate subtype selectivity will likely determine how far therapeutic development for this subtype advances.
References
- Kruse, A.C.; et al. Muscarinic acetylcholine receptors: novel opportunities for drug development. Nature reviews Drug discovery. 2014, 13(7): 549-560.
- Wess, J.; et al. Muscarinic acetylcholine receptors: mutant mice provide new insights for drug development. Nature reviews Drug discovery. 2007, 6(9): 721-733.
