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Muscarinic receptors are widely distributed throughout the body and control distinct functions according to location and subtype (M1 - M5).They are predominantly expressed in the parasympathetic nervous system where they exert both inhibitory and excitatory effects.
Tocris offers the following scientific literature for Acetylcholine Muscarinic Receptors to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.
|Transduction Mechanism||↑PLC (Gq/11)||↓Adenylyl Cyclase (Gi/o)||↑PLC (Gq/11)||↓Adenylyl Cyclase (Gi/o)||↑PLC (Gq/11)|
|Primary Distribution||Neocortex, hippocampus, neostriatum, salivary glands, eye, heart||Brain, heart, smooth muscle, salivary glands||Smooth muscle, exocrine glands, brain, autonomic ganglia, salivary glands||Neostriatum, cortex, hippocampus, autonomic ganglia||Substantia nigra, pars compacta, ventral tegmental area, hippocampus|
|Tissue Function||Learning and memory, neuromodulation, M-current inhibition||Bradycardia, smooth muscle contraction, antinociception, hyperthermia, ↓ neurotransmitter release (presynaptic)||Smooth muscle contraction, gland secretion, ↓ neurotransmitter release (presynaptic)||Regulation of dopamine D1 stimulated locomotor activity||Unknown|
|Key Compounds||pKB Values|
Oxotremorine M (1067)
AF-DX 116 (1105)
AF-DX 384 (1345)
AQ-RA 741 (2292)
J 104129 (2507)
PD 102807 (1671)
J 104129 (2507)
* Ki values, ‡ pKi values, † EC50 value
Caulfield and Birdshall (1998) International union of pharmacology. XVII. Classification of muscarinic acetylcholine receptors. Pharmacol.Rev. 50 279. Mansfield et al (2005) Muscarinic receptor subtypes in human bladder detrusor and mucosa, studied by radioligand binding and quantitative competitive RT-PCR: changes in ageing. Br.J.Pharmacol. 144 1089. Pfaff et al (1995) The (S)-(+)-enantiomer of dimethindene: a novel M2-selective muscarinic receptor antagonist. Eur.J.Pharmacol. 286 229. Loudon et al (1997) SB 202026: a novel muscarinic partial agonist with functional selectivity for M1 receptors. J.Pharmacol.Exp.Ther. 283 1059. Burstein et al (1997) Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins. Mol.Pharmacol. 51 312. Mitsuya et al (2000) Discovery of a muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors among 2-[(1S,2S)-3-sulfonylaminocyclopentylacetamide derivatives. Bioorg.Med.Chem. 8 825. Watson et al (1995) Characterization of the interaction of zamifenacin at muscarinic receptors in vitro. Eur.J.Pharmacol. 285 135. Mitsuya et al J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors. Bioorg.Med.Chem.Lett. 7 2555.