Muscarinic receptors subtypes

Hulme, EC, Birdsall, NJM and Buckley, NJ (1990) Muscarinic receptor subtypes. Ann. Rev. Pharm. Toxicol. 30 633-673. 

Birdsall NJ, Farries T, Gharagozloo P, Kobayashi S, Kuonen D, Lazareno S, Popham A, Sugimoto M. Selective allosteric enhancement of the binding and actions of acetylcholine at muscarinic receptor subtypes. Life Sci 1997 60 1047-1052. 

Ellis J, Huyler J, Brann MR. Allosteric regulation of cloned mrm5 muscarinic receptor subtypes. Biochem Pharmacol 1991 42 1927-1932. 

Baghdoyan, H. A. Lydic, R. (1999). M2 muscarinic receptor subtype in the feline medial pontine reticular formation modulates the amount of rapid eye movement sleep. Sleep 22, 835-47. 

Baghdoyan, H. A. (1997). Location and quantification of muscarinic receptor subtypes in rat pons implications for REM sleep generation. Am. J. Physiol. 273, R896-R904. 

Baghdoyan, H. A., Mallios, V. J Duckrow, R. B. Mash, D. C. (1994). Localization of muscarinic receptor subtypes in brain stem areas regulating sleep. Neuroreport 5, 1631-4. 

Imeri, L., Bianchi, S., Angeli, P. Mancia, M. (1994). Selective blockade of different brain stem muscarinic receptor subtypes effects on the sleep-wake cycle. Brain Res. 636, 68-72. 

Costa, P., Traver, D.J., Auger, C.B. and Costa, L.G. (1994) Expression of cholinergic muscarinic receptor subtypes mRNA in rat blood mononuclear cells. Immuno-pharmacology 28,113—123. 

Thus, cholinergic receptor classification can be considered in terms of three stages of development. Initially, Dale [2] distinguished nicotinic and muscarinic receptor subtypes with crude alkaloids. Then, chemical synthesis and structure-activity relationships clearly revealed that nicotinic and muscarinic receptors were heterogeneous, but chemical selectivity could not come close to uncovering the true diversity of receptor subtypes. Lastly, analysis of subtypes came from molecular cloning, making possible the classification of receptors on the basis of primary structure (Fig. 11-2). 

Ashkenazi, A., Winslow, J. W., Peralta, E. G. etal. An M2 muscarinic receptor subtype coupled to both adenylyl cyclase and phosphoinositide turnover. Science 238 672-675,1987. 

Fitzgerald BB, Costa LG. 1992. Modulation of Ml and M2 muscarinic receptor subtypes following repeated organophosphate exposure in rats. Toxicol Appl Pharmacol ] 17 112-125. 

Mutschler, E. Affinity profiles of hexahydro-sila-difenidol analogues at muscarinic receptor subtypes. 

So, parasympathetic nerves use acetylcholine as a neurotransmitter and cholinomimetic drugs mimic the action of acetylcholine at its receptors. Muscarinic receptor subtypes are found on neuroeffector junctions. Nicotinic receptor subtypes are found on ganglionic synapses. Chohnomimetics can be classified as ... 

Burstein ES, Spalding TA, Brann MR. Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins. Mol Pharmacol 1997 51(2) 312-9. 

Hulme EC, Birdsall NJM, Bickley NJ. Muscarinic receptor subtypes. Annu Rev Pharmacol Toxicol 1990 30 633-73. 

The airway effects of released acetylcholine are mediated via activation of three distinct muscarinic receptor subtypes Mj, in parasympathetic ganglia, mucous glands and alveolar walls autoinhibitory M2, in parasympathetic nerve terminals and M3, in airway smooth muscle, mucus glands, and airway epithelium. 

At present five different muscarinic receptor subtypes are known that mediate the parasympathetic activity of the autonomic nervous system M-,-, M2-, M3-, M4-, and Ms-receptors [88, 116]. The odd-numbered muscarinic receptors are... 

As indicated in Chapter 6, muscarinic receptor subtypes have been characterized by binding studies and cloned. Several cellular events occur when muscarinic receptors are activated, one or more of which might serve as second messengers for muscarinic activation. All muscarinic receptors appear to be of the G protein-coupled type (see Chapter 2 and Table 7-1). Muscarinic agonist binding activates the inositol trisphosphate (IP3), diacylglycerol (DAG) cascade. Some evidence... 

All five muscarinic receptor subtypes have been detected in the central nervous system. The roles of Mx through M3 have been analyzed by means of experiments in knockout mice. The Mx subtype is richly expressed in brain areas involved in cognition. Knockout of Mx receptors was associated with impaired neuronal plasticity in the forebrain, and pilocarpine did not induce seizures in Mx mutant mice. The central nervous system effects of the synthetic muscarinic agonist oxotremorine (tremor, hypothermia, and antinociception) were lacking in mice with homozygously mutated M2 receptors. Animals lacking M3 receptors, especially those in the hypothalamus, had reduced appetite and diminished body fat mass. 

Brodde OE et al Presence, distribution and physiological function of adrenergic and muscarinic receptor subtypes in the human heart. Basic Res Cardiol 2001 96 528. [PMID 11770070]... 

Bartolini, A., Ghelardini, C., Fantetti, L., Malcangio, M., Malmberg-Aiello, P., Giotti, A.. Role of muscarinic receptor subtypes in central antinociception, Br. J. Pharmacol. 1992, 105, 77-82. 

Naguib, M. and Yaksh, T.L. Characterization of muscarinic receptor subtypes that mediate antinociception in the rat spinal cord, Anesth. Analg. 1997, 85, 847-853. 

Salamone, J. D., Correa, M., Carlson, B. B., Wisniecki, A., Mayorga, A. J., Nisenbaum, E., Nisenbaum, L., Felder, C. Neostriatal muscarinic receptor subtypes involved in the generation of tremulous jaw movements in rodents. Implications for cholinergic involvement in Parkinsonism, Life Sci. 2001, 68, 2579-2584. 

FIGURE 12—10. Acetylcholine (ACh) receptors. There are numerous receptors for ACh. The major subdivision is between nicotinic (N) and muscarinic (M) cholinergic receptors. There are also numerous subtypes of these receptors, best characterized for muscarinic receptor subtypes (Ml, M2, Mx). Perhaps the Ml postsynaptic receptor is key to mediating the memory functions linked to cholinergic neurotransmission, but a role for other cholinergic receptor subtypes has not been ruled out. 

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