Acetylcholine muscarinic

Felder, C. C. (1995). Muscarinic acetylcholine receptors . Signal transduction through multiple effectors. FASEB j. 9, 619-625. 

Jakubic, J., and El-Fakahany, E. E. (1997). Positive coopera -tivity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mot. Pharmacol. 52 172-177. 

Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol. Pharmacol. 52 172—179. 

Jakubic, J., Bacakova, L., Lisd, V., El-Fakahany, E. E., and Tucek, S. (1996). Activation of muscarinic acetylcholine receptors via their allosteric binding sites. Proc. Natl. Acad. Sci. USA 93 8705-8709. 

Antagonists of muscarinic acetylcholine receptors had widely been used since 1860 for the treatment of Parkinson s disease, prior to the discovery of l-DOPA. They block receptors that mediate the response to striatal cholinergic interneurons. The antiparkinsonian effects of drugs like benzatropine, trihexyphenidyl and biper-iden are moderate the resting tremor may sometimes respond in a favorable manner. The adverse effects, e.g., constipation, urinary retention, and mental confusion, may be troublesome, especially in the elderly. 

Muscarinic acetylcholine receptors (mAChRs) form a class of cell surface receptors that are activated upon binding of the neurotransmitter, acetylcholine. Structurally and functionally, mAChRs are prototypical members of the superfamily of G protein-coupled receptors. Following acetylcholine binding, the activated mAChRs interact with distinct classes of heterotrimeric G proteins resulting in the activation or inhibition of distinct downstream signaling cascades. 

Wess J (1996) Molecular biology of muscarinic acetylcholine receptors. CritRev Neurobiol 10 69-99... 

Caulfield MP, Birdsall NJM (1998) International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors. Pharmacol Rev 50 279-290... 

Wess J (2004) Muscarinic acetylcholine receptor knockout mice novel phenotypes and clinical implications. Annu Rev Pharmacol Toxicol 44 423-450... 

Lanzafame A A, Christopoulos A, Mitchelson F (2003) Cellular signaling mechanisms for muscarinic acetylcholine receptors. Recept Chann 9 241-260... 

Levey, A, Kitt, CA, Simmonds, WF, Price, DL and Brann, MR (1991) Identification and localisation of muscarinic acetylcholine receptor proteins in brain with subtype specific antibodies. J. Neurosci. 11 3218-3226. 

Basu N, Stamler CJ, Loua KM, Chan HM. 2005a. An interspecies comparison of mercury inhibition on muscarinic acetylcholine receptor binding in the cerebral cortex and cerebellum. Toxicol Appl Pharmacol 205 71-76. 

Tucek S, Proska J. Allosteric modulation of muscarinic acetylcholine receptors. Trends Pharmacol Sci 1995 16 205-212. 

Tucek S, Musilkova J, Neduoma J, Proska J, Shelkovnikov SW, Vorlicek J. Positive cooperativity in the binding of alcuronium and A-methy lscopolamine to muscarinic acetylcholine receptors. Mol Pharmacol 1990 38 674-680. 

Jakubik J, Bacakova L, El-Fakahany EE, Tucek S. Subtype selectivity of the positive allosteric action of alcuronium at cloned M M5 muscarinic acetylcholine receptors. J Pharmacol Exp Ther 1995 274 1077-1083. 

Gharagozloo P, Lazareno S, Popham A, Birdsall N. Allosteric interactions of quaternary strychnine and brucine derivatives with muscarinic acetylcholine receptors. J Med Chem 1999 42 438-445. 

A G-protein-mediated effect has an absolute requirement for GTP. Reference has already been made to the requirement for GTP in reconstituting hormone-stimulated adenylate cyclase activity. A similar requirement can be demonstrated when the effector is an ion channel, such as the cardiac atrial inward-rectifier K+ channel which is activated following stimulation of the M2 muscarinic acetylcholine receptor. Thus, in the experiment illustrated in Figure 7.8, the channel recorded with a cell-... 

V2 VIP/PACAP (VPAC1 3) prostanoid DP, IP CRFU calcitonin/amylin/CGRP Gj/G0 a2-Adrenoceptor M2/4 muscarinic acetylcholine dopamine D2 4 5HT2 opioid 5, p, K, OFQ ... 

Caulfield, M. P. Birdsall, N. J. (1998). International union of pharmacology. XVIII. Classification of muscarinic acetylcholine receptors. Pharmacol. Rev. 50, 279-90. 

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