Acetylcholine Receptors
Cambridge Bioscience, through our collaboration with ChanTest, offers access to GPCR screening and profiling services to the following acetylcholine receptor targets:
m1
Synonym: CHRM1
Validated Assay/Platform: Binding & Calcium
Description: Muscarinic acetylcholine receptors are members of the superfamily of G protein-coupled receptors (GPCRs). They are relatively abundant and mediate many of the diverse actions of acetylcholine in the CNS as well as throughout non-nervous tissues innervated by the parasympathetic nervous system. At present, five receptor subtypes (M1 - M5) have been identified. The odd-numbered receptors (M1, M3, and M5) are preferentially coupled to G(q/11). The even-numbered receptors (M2 and M4) are coupled to G(i/o). They also activate G protein-gated potassium channels, which leads to hyperpolarization of the plasma membrane in different excitable cells. Among the five subtypes, M1 receptor is important in excitatory postsynaptic potential in autonomic ganglia, secretion from salivary glands and stomach, memory and Alzheimers disease.
m2
Validated Assay/Platform: Binding & cAMP
Description: The five muscarinic receptor subtypes all mediate the action of acetylcholine. The odd-numbered receptors (m1, m3, and m5) couple efficiently through Gq/11 to activate phospholipase C and lead to elevation of intracellular calcium, whereas the even-numbered receptors (m2, M4) are efficiently coupled to Gi and lead to inhibition of intracellular cAMP along with several other signal transduction pathways.
m3
Synonym: CHRM3
Validated Assay/Platform: Binding & Calcium
Description: Muscarinic acetylcholine receptors are members of the superfamily of G protein-coupled receptors (GPCRs). They are relatively abundant and mediate many of the diverse actions of acetylcholine in the CNS as well as throughout non-nervous tissues innervated by the parasympathetic nervous system. At present, five receptor subtypes (M1 - M5) have been identified. The odd-numbered receptors (M1, M3, and M5) are preferentially coupled to G(q/11). The even-numbered receptors (M2 and M4) are coupled to G(i/o). They also activate G protein-gated potassium channels, which leads to hyperpolarization of the plasma membrane in different excitable cells. Among the five subtypes, M3 receptor is important in smooth muscle contraction, increased endocrine and exocrine gland secretion, vasodilation, eye accommodation, emesis and other CNS effects.
m4
Validated Assay/Platform: Binding & cAMP
Description: The five muscarinic receptor subtypes all mediate the action of acetylcholine. The odd-numbered receptors (m1, m3, and m5) couple efficiently through Gq/11 to activate phospholipase C and lead to elevation of intracellular calcium, whereas the even-numbered receptors (m2, M4) are efficiently coupled to Gi and lead to inhibition of intracellular cAMP along with several other signal transduction pathways.
m4 (Rat)
Synonym: M4
Validated Assay/Platform: Binding & cAMP
Description: Muscarinic acetylcholine receptors are relatively abundant and mediate many of the diverse actions of acetylcholine in the CNS, as well as throughout non-nervous tissues innervated by the parasympathetic nervous system. There are five muscarinic receptor subtypes referred to as M1, M2, M3, M4 and M5 which belong to GPCR superfamily. The odd-numbered muscarinic receptors (M1, M3, M5) couple efficiently through Gq/11, to activate of phospholipase C, that initiates the phosphatidylinositol turnover response. The even-numbered muscarinic receptors (M2, M4) inhibit adenylyl caclase activity via activation of the Gi class of G proteins. M2 and M4 receptors also activate G protein-coupled potassium channel, which leads to hyperpolarization of the plasma membrane of excitable cells.
m5
Synonym: CHRM5
Validated Assay/Platform: Binding & Calcium
Description: Muscarinic acetylcholine receptors are members of the superfamily of G protein-coupled receptors (GPCRs). They are relatively abundant and mediate many of the diverse actions of acetylcholine in the CNS as well as throughout non-nervous tissues innervated by the parasympathetic nervous system. At present, five receptor subtypes (M1 - M5) have been identified. The odd-numbered receptors (M1, M3, and M5) are preferentially coupled to G(q/11). The even-numbered receptors (M2 and M4) are coupled to G(i/o). They also activate G protein-gated potassium channels, which leads to hyperpolarization of the plasma membrane in different excitable cells. Among the five subtypes, M5 receptors are mainly expressed in brain and involved in muscarinic induced dopamine release and Parkinson’s disease.
Platforms Available
Cambridge Bioscience, through our collaboration with ChanTest, offers access to both FLIPRTETRA® and FlexStation® 3 allowing you to select the right balance of speed, throughput and data quality to suit your needs.
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