muscarinic receptors


Summary: One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.

Top Publications

  1. Jo J, Son G, Winters B, Kim M, Whitcomb D, Dickinson B, et al. Muscarinic receptors induce LTD of NMDAR EPSCs via a mechanism involving hippocalcin, AP2 and PSD-95. Nat Neurosci. 2010;13:1216-24 pubmed publisher
    ..We found that stimulation of muscarinic receptors, either by an agonist or by the synaptic release of acetylcholine, led to long-term depression (LTD) of ..
  2. Threlfell S, Clements M, Khodai T, Pienaar I, Exley R, Wess J, et al. Striatal muscarinic receptors promote activity dependence of dopamine transmission via distinct receptor subtypes on cholinergic interneurons in ventral versus dorsal striatum. J Neurosci. 2010;30:3398-408 pubmed publisher
    ..How DA signaling is regulated by striatal muscarinic receptors (mAChRs) is unresolved; contradictory reports indicate suppression or facilitation, implicating several ..
  3. Jensen J, Lyssand J, Hague C, Hille B. Fluorescence changes reveal kinetic steps of muscarinic receptor-mediated modulation of phosphoinositides and Kv7.2/7.3 K+ channels. J Gen Physiol. 2009;133:347-59 pubmed publisher
    ..0 s) to become nearly contemporaneous with Galpha(q)/PLC interaction. Evidently, channel release of PIP(2) and closure are rapid, and the availability of active PLC limits the rate of M current suppression. ..
  4. Yamamoto M, Unno T, Matsuyama H, Kohda M, Masuda N, Nishimura M, et al. Two types of cation channel activated by stimulation of muscarinic receptors in guinea-pig urinary bladder smooth muscle. J Pharmacol Sci. 2008;108:248-57 pubmed
  5. Dinan T, Clarke G, Quigley E, Scott L, Shanahan F, Cryan J, et al. Enhanced cholinergic-mediated increase in the pro-inflammatory cytokine IL-6 in irritable bowel syndrome: role of muscarinic receptors. Am J Gastroenterol. 2008;103:2570-6 pubmed publisher
    ..cytokine profile in IBS is driven by the cholinergic system and determined if the responses are mediated by muscarinic receptors. Eighty-eight subjects took part in two studies, 37 IBS patients (Rome II), 14 depressed patients, and 37 ..
  6. Razani Boroujerdi S, Behl M, Hahn F, Pena Philippides J, Hutt J, Sopori M. Role of muscarinic receptors in the regulation of immune and inflammatory responses. J Neuroimmunol. 2008;194:83-8 pubmed publisher
    Leukocytes contain both nicotinic and muscarinic receptors, and while activation of nicotinic receptors suppresses immune/inflammatory responses, the role of muscarinic receptors in immunity is unclear...
  7. Zhou X, Wulfsen I, Lutz S, Utku E, Sausbier U, Ruth P, et al. M2 muscarinic receptors induce airway smooth muscle activation via a dual, Gbetagamma-mediated inhibition of large conductance Ca2+-activated K+ channel activity. J Biol Chem. 2008;283:21036-44 pubmed publisher
    Airway smooth muscle is richly endowed with muscarinic receptors of the M(2) and M(3) subtype...
  8. Herrero J, Roberts M, Delicato L, Gieselmann M, Dayan P, Thiele A. Acetylcholine contributes through muscarinic receptors to attentional modulation in V1. Nature. 2008;454:1110-4 pubmed publisher
    ..These results demonstrate that muscarinic cholinergic mechanisms play a central part in mediating the effects of attention in V1. ..
  9. Deguil J, Perault Pochat M, Chavant F, Lafay Chebassier C, Fauconneau B, Pain S. Activation of the protein p7OS6K via ERK phosphorylation by cholinergic muscarinic receptors stimulation in human neuroblastoma cells and in mice brain. Toxicol Lett. 2008;182:91-6 pubmed publisher
    Stimulation of cholinergic muscarinic receptors has been shown to provide substantial protection from DNA damage, oxidative stress and mitochondrial impairment, insults that may be encountered by neurons in development, aging, or ..

More Information


  1. Jositsch G, Papadakis T, Haberberger R, Wolff M, Wess J, Kummer W. Suitability of muscarinic acetylcholine receptor antibodies for immunohistochemistry evaluated on tissue sections of receptor gene-deficient mice. Naunyn Schmiedebergs Arch Pharmacol. 2009;379:389-95 pubmed publisher
    ..pharmacologically relevant effects upon smooth muscle tone and epithelial function via five types of muscarinic receptors (M1R-M5R)...
  2. Lucas Meunier E, Monier C, Amar M, Baux G, Fregnac Y, Fossier P. Involvement of nicotinic and muscarinic receptors in the endogenous cholinergic modulation of the balance between excitation and inhibition in the young rat visual cortex. Cereb Cortex. 2009;19:2411-27 pubmed publisher
    ..We conclude that endogenous-released ACh amplifies the dominance of the inhibitory drive and thus decreases the excitability and sensory responsiveness of layer 5 pyramidal neurons. ..
  3. Iwasaki M, Hayashi Y, kamibayashi T, Yamatodani A, Mashimo T. The antiarrhythmic effect of centrally administered rilmenidine involves muscarinic receptors, protein kinase C and mitochondrial signalling pathways. Br J Pharmacol. 2008;153:1623-30 pubmed publisher
    ..The present study was designed to examine the role of muscarinic receptors, protein kinase C (PKC), ATP-sensitive potassium channels (K(ATP)) and the mitochondrial permeability ..
  4. Andersson D, Björnsson E, Bergquist F, Nissbrandt H. Motor activity-induced dopamine release in the substantia nigra is regulated by muscarinic receptors. Exp Neurol. 2010;221:251-9 pubmed publisher
  5. Giordano G, Li L, White C, Farin F, Wilkerson H, Kavanagh T, et al. Muscarinic receptors prevent oxidative stress-mediated apoptosis induced by domoic acid in mouse cerebellar granule cells. J Neurochem. 2009;109:525-38 pubmed publisher
    ..By activating M(3) muscarinic receptors, the cholinergic agonist carbachol inhibits DomA-induced apoptosis, and the anti-apoptotic action of ..
  6. McLeod M, Scarr E, Dean B. Effects of benzodiazepine treatment on cortical GABA(A) and muscarinic receptors: studies in schizophrenia and rats. Psychiatry Res. 2010;179:139-46 pubmed publisher
    Changes in cortical ?-aminobutyric acid A (GABA(A)) receptors and muscarinic receptors have been reported in schizophrenia, a disorder treated with antipsychotic drugs and benzodiazepines...
  7. Rattmann Y, Crestani S, Lapa F, Miguel O, Marques M, da Silva Santos J, et al. Activation of muscarinic receptors by a hydroalcoholic extract of Dicksonia sellowiana Presl. HooK (Dicksoniaceae) induces vascular relaxation and hypotension in rats. Vascul Pharmacol. 2009;50:27-33 pubmed publisher
    ..possess substances with both in vivo and in vitro activities and that the vascular effect of HEDS involves activation of muscarinic receptors, stimulation of the nitric oxide pathway and opening of calcium-activated potassium channels.
  8. Kullmann F, ARTIM D, Birder L, de Groat W. Activation of muscarinic receptors in rat bladder sensory pathways alters reflex bladder activity. J Neurosci. 2008;28:1977-87 pubmed publisher
    ..These findings suggest that the urothelial-afferent nerve interactions can influence reflex voiding function. ..
  9. Ikeda Y, Kanai A. Urotheliogenic modulation of intrinsic activity in spinal cord-transected rat bladders: role of mucosal muscarinic receptors. Am J Physiol Renal Physiol. 2008;295:F454-61 pubmed publisher
    ..In summary, we suggest an urotheliogenic origin for intrinsic activity, where structures within the mucosal layer organize and thereby enhance intrinsic detrusor contractions. ..
  10. Tsang S, Francis P, Esiri M, Wong P, Chen C, Lai M. Loss of [3H]4-DAMP binding to muscarinic receptors in the orbitofrontal cortex of Alzheimer's disease patients with psychosis. Psychopharmacology (Berl). 2008;198:251-9 pubmed publisher
    ..In contrast, it is unclear whether non-M2 muscarinic receptors have a role to play in AD behavioural symptoms...
  11. Scarr E, Dean B. Muscarinic receptors: do they have a role in the pathology and treatment of schizophrenia?. J Neurochem. 2008;107:1188-95 pubmed publisher
    ..typical) antipsychotic medications, to the development of drugs designed to specifically activate selected muscarinic receptors. This review presents data implicating a decrease in muscarinic receptors, particularly the M1 receptor, in ..
  12. Haag S, Matthiesen S, Juergens U, Racke K. Muscarinic receptors mediate stimulation of collagen synthesis in human lung fibroblasts. Eur Respir J. 2008;32:555-62 pubmed publisher
    ..Human lung fibroblasts express muscarinic receptors and the present study aimed to explore their role in controlling collagen synthesis...
  13. Ghatpande A, Gelperin A. Presynaptic muscarinic receptors enhance glutamate release at the mitral/tufted to granule cell dendrodendritic synapse in the rat main olfactory bulb. J Neurophysiol. 2009;101:2052-61 pubmed publisher
  14. Digby G, Shirey J, Conn P. Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders. Mol Biosyst. 2010;6:1345-54 pubmed publisher
    ..These novel allosteric modulators of mAChRs may provide therapeutic potential for treatment of a number of CNS disorders such as Alzheimer's disease and schizophrenia. ..
  15. Saito M, Kazuyama E, Shimizu S, Dimitriadis F, Kinoshita Y, Masuda E, et al. Muscarinic receptors and their mRNAs in type 2 Goto-Kakizaki diabetic rat prostate. Prostate. 2010;70:1533-9 pubmed publisher
    ..towards the relationship between diabetes and benign prostatic hyperplasia/lower urinary tract symptoms, we investigated the pharmacological properties and gene expressions of the muscarinic receptors in type 2 diabetes rat prostate.
  16. Barathi V, Weon S, Beuerman R. Expression of muscarinic receptors in human and mouse sclera and their role in the regulation of scleral fibroblasts proliferation. Mol Vis. 2009;15:1277-93 pubmed
    ..These results show that proliferative responses of SFs to muscarinic receptor stimulation are mediated via the activation of the classical MEK-ERK-MAPK cascade. ..
  17. Profita M, Bonanno A, Siena L, Bruno A, Ferraro M, Montalbano A, et al. Smoke, choline acetyltransferase, muscarinic receptors, and fibroblast proliferation in chronic obstructive pulmonary disease. J Pharmacol Exp Ther. 2009;329:753-63 pubmed publisher
    ..These results suggest that cigarette smoke might alter the expression of ChAT and MRs, promoting airway remodeling in COPD and that anticholinergic drugs, including tiotropium, might prevent these events. ..
  18. Hoogduijn M, Cheng A, Genever P. Functional nicotinic and muscarinic receptors on mesenchymal stem cells. Stem Cells Dev. 2009;18:103-12 pubmed publisher
    ..Environmental compounds such as nicotine and agricultural insecticides can interfere with this system and may affect cellular processes in the MSC...
  19. Tahvildari B, Alonso A, Bourque C. Ionic basis of ON and OFF persistent activity in layer III lateral entorhinal cortical principal neurons. J Neurophysiol. 2008;99:2006-11 pubmed publisher
    ..e., BK) channels is required to induce the off state. ..
  20. Zhu X, Zhou W, Cui Y, Zhu L, Li J, Feng X, et al. Pilocarpine protects cobalt chloride-induced apoptosis of RGC-5 cells: involvement of muscarinic receptors and HIF-1 alpha pathway. Cell Mol Neurobiol. 2010;30:427-35 pubmed publisher
    ..which could largely be reversed by the pretreatment of 1 microM pilocarpine mainly via the activation of muscarinic receptors. Meanwhile, pretreatment of 1 microM pilocarpine could significantly prevent CoCl(2)-induced HIF-1 alpha ..
  21. Harrington A, Hutson J, Southwell B. Cholinergic neurotransmission and muscarinic receptors in the enteric nervous system. Prog Histochem Cytochem. 2010;44:173-202 pubmed publisher
    ..This review will concentrate on one of two classes of ACh receptors, Muscarinic receptors (mAChr), in particular their location and function in mediating synaptic transmission within enteric ..
  22. Ikeda Y, Birder L, Buffington C, Roppolo J, Kanai A. Mucosal muscarinic receptors enhance bladder activity in cats with feline interstitial cystitis. J Urol. 2009;181:1415-22 pubmed publisher
    ..In feline interstitial cystitis cat bladders there is increased Ca(2+) activity and sensitivity of muscarinic receptors in the mucosal layer, which can enhance smooth muscle spontaneous contractions.
  23. Cui Y, Zhu L, Wang H, Advenier C, Chen H, Devillier P. Muscarinic receptors involved in airway vascular leakage induced by experimental gastro-oesophageal reflux. Life Sci. 2008;82:949-55 pubmed publisher
    ..induced by instillation of hydrochloric acid (HCl) into the oesophagus of guinea-pigs and the subtype of muscarinic receptors involved...
  24. Witte L, Chapple C, de la Rosette J, Michel M. Cholinergic innervation and muscarinic receptors in the human prostate. Eur Urol. 2008;54:326-34 pubmed
    ..Concomitantly, the human prostate expresses muscarinic receptors at densities exceeding those of alpha(1)-adrenoceptors...
  25. Giglio D, Andersson M, Aronsson P, Delbro D, Haraldsson B, Tobin G. Changes in muscarinic receptors in the toad urothelial cell line TBM-54 following acrolein treatment. Clin Exp Pharmacol Physiol. 2008;35:217-22 pubmed
    ..In the present study, we investigated whether the toad urothelial cell line TBM-54 expresses functional muscarinic receptors and whether changes in muscarinic receptors can be induced in vitro by treating cells with acrolein, a ..
  26. McBrien N, Jobling A, Truong H, Cottriall C, Gentle A. Expression of muscarinic receptor subtypes in tree shrew ocular tissues and their regulation during the development of myopia. Mol Vis. 2009;15:464-75 pubmed
    b>Muscarinic receptors are known to regulate several important physiologic processes in the eye. Antagonists to these receptors such as atropine and pirenzepine are effective at stopping the excessive ocular growth that results in myopia...
  27. Conn P, Jones C, Lindsley C. Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. Trends Pharmacol Sci. 2009;30:148-55 pubmed publisher
  28. Frazier E, Braverman A, Peters S, Michel M, Ruggieri M. Does phospholipase C mediate muscarinic receptor-induced rat urinary bladder contraction?. J Pharmacol Exp Ther. 2007;322:998-1002 pubmed
    ..We conclude that previously reported differences relate to the use of inhibitors rather than experimental protocols and that the overall data do not support a role for PLC in M(3) muscarinic receptor-mediated rat bladder contraction. ..
  29. Ryberg A, Warfvinge G, Axelsson L, Soukup O, Götrick B, Tobin G. Expression of muscarinic receptor subtypes in salivary glands of rats, sheep and man. Arch Oral Biol. 2008;53:66-74 pubmed
    ..A secretory effect by muscarinic M5 receptors is not to be excluded, since they were expressed in all the glands examined. However, other functions, such as promotion of inflammation, cell growth and proliferation are possible as well. ..
  30. Rivera L, Brading A. The role of Ca2+ influx and intracellular Ca2+ release in the muscarinic-mediated contraction of mammalian urinary bladder smooth muscle. BJU Int. 2006;98:868-75 pubmed
    ..Procaine, ryanodine and caffeine blocked the store release contractions, suggesting that this involves ryanodine receptors and calcium-induced calcium release. ..
  31. MCCOY P, McMahon L. Muscarinic receptor dependent long-term depression in rat visual cortex is PKC independent but requires ERK1/2 activation and protein synthesis. J Neurophysiol. 2007;98:1862-70 pubmed
    ..This plasticity could be a mechanism by which the cholinergic system modifies glutamatergic synapse function to permit normal visual system processing required for cognition. ..
  32. Abrams P, Andersson K, Buccafusco J, Chapple C, de Groat W, Fryer A, et al. Muscarinic receptors: their distribution and function in body systems, and the implications for treating overactive bladder. Br J Pharmacol. 2006;148:565-78 pubmed the treatment of the overactive bladder (OAB) syndrome is thought to arise through blockade of bladder muscarinic receptors located on detrusor smooth muscle cells, as well as on nondetrusor structures. 2...
  33. Smetana R, Alford S, Dubuc R. Muscarinic receptor activation elicits sustained, recurring depolarizations in reticulospinal neurons. J Neurophysiol. 2007;97:3181-92 pubmed
    ..Cells immunoreactive for muscarinic receptors were found in this region and could mediate this response...
  34. Takasu K, Honda M, Ono H, Tanabe M. Spinal alpha(2)-adrenergic and muscarinic receptors and the NO release cascade mediate supraspinally produced effectiveness of gabapentin at decreasing mechanical hypersensitivity in mice after partial nerve injury. Br J Pharmacol. 2006;148:233-44 pubmed
    ..on mechanical hypersensitivity involves activation of spinal alpha(2)-adrenergic receptors followed by muscarinic receptors (most likely M(1)) and the NO cascade...
  35. Stevens L, Chapple C, Chess Williams R. Human idiopathic and neurogenic overactive bladders and the role of M2 muscarinic receptors in contraction. Eur Urol. 2007;52:531-8 pubmed
    ..Contraction mediated by muscarinic receptors is enhanced in idiopathic and neurogenic overactive detrusors compared with control detrusor...
  36. Lin B, Ji H, Li P, Jiang Y, Fang W. Selective antagonism activity of alkaloids from bulbs Fritillariae at muscarinic receptors: functional studies. Eur J Pharmacol. 2006;551:125-30 pubmed
  37. Spalding T, Burstein E. Constitutive activity of muscarinic acetylcholine receptors. J Recept Signal Transduct Res. 2006;26:61-85 pubmed
    ..and discuss the implications of these data for the structure, function, and activation mechanism of muscarinic receptors. Finally, we discuss the possible physiological significance of constitutive activity of muscarinic ..
  38. Origlia N, Kuczewski N, Aztiria E, Gautam D, Wess J, Domenici L. Muscarinic acetylcholine receptor knockout mice show distinct synaptic plasticity impairments in the visual cortex. J Physiol. 2006;577:829-40 pubmed
    ..Our results indicate that different mAChR subtypes regulate different forms of long-term synaptic plasticity in the mouse visual cortex, activating specific G proteins and downstream intracellular mechanisms. ..
  39. Matthiesen S, Bahulayan A, Holz O, Racké K. MAPK pathway mediates muscarinic receptor-induced human lung fibroblast proliferation. Life Sci. 2007;80:2259-62 pubmed
    ..We recently reported expression of multiple muscarinic receptors in human lung fibroblasts and demonstrated muscarinic receptor-induced, G(i)-mediated proliferation in ..
  40. Liu S, Li J, Tan D, Beuerman R. The eyelid margin: a transitional zone for 2 epithelial phenotypes. Arch Ophthalmol. 2007;125:523-32 pubmed
    ..To investigate the differentiation profile of the epithelium of the eyelid margin in the primate...
  41. Myslivecek J, Duysen E, Lockridge O. Adaptation to excess acetylcholine by downregulation of adrenoceptors and muscarinic receptors in lungs of acetylcholinesterase knockout mice. Naunyn Schmiedebergs Arch Pharmacol. 2007;376:83-92 pubmed
    ..The hypothesis was tested that not only muscarinic receptors but also alpha(1)-adrenoceptors and beta-adrenoceptors are downregulated, thus maintaining a proper balance ..
  42. Unno T, Matsuyama H, Okamoto H, Sakamoto T, Yamamoto M, Tanahashi Y, et al. Muscarinic cationic current in gastrointestinal smooth muscles: signal transduction and role in contraction. Auton Autacoid Pharmacol. 2006;26:203-17 pubmed
    ..The neurotransmitter acetylcholine, via activating muscarinic receptors that exist in smooth muscle, produces its contraction...
  43. Lucas J, Wang D, Sadee W. Calmodulin binding to peptides derived from the i3 loop of muscarinic receptors. Pharm Res. 2006;23:647-53 pubmed
    ..Calmodulin can bind to an M1 region implicated in G protein coupling. This indicates an important role for CaM in the regulation of muscarinic signal transduction. ..
  44. Wuest M, Weiss A, Waelbroeck M, Braeter M, Kelly L, Hakenberg O, et al. Propiverine and metabolites: differences in binding to muscarinic receptors and in functional models of detrusor contraction. Naunyn Schmiedebergs Arch Pharmacol. 2006;374:87-97 pubmed
    ..Change from a tertiary to a secondary amine (M-14) results in lower binding affinity and reduced potency. Oxidation of the nitrogen (M-5) further lowers binding affinity as well as functional potency. ..
  45. Durlu Kandilci N, Brading A. Involvement of Rho kinase and protein kinase C in carbachol-induced calcium sensitization in beta-escin skinned rat and guinea-pig bladders. Br J Pharmacol. 2006;148:376-84 pubmed
    ..8. In conclusion, muscarinic receptor activation induces calcium sensitization in rat and guinea-pig detrusor smooth muscles but there are differences in their pathways. ..
  46. Matthiesen S, Bahulayan A, Kempkens S, Haag S, Fuhrmann M, Stichnote C, et al. Muscarinic receptors mediate stimulation of human lung fibroblast proliferation. Am J Respir Cell Mol Biol. 2006;35:621-7 pubmed
    ..For this purpose, expression of muscarinic receptors in MRC-5 human lung fibroblasts was characterized by semiquantitative RT-PCR, and the effects of muscarinic ..
  47. Li S, Cullen W, Anwyl R, Rowan M. Muscarinic acetylcholine receptor-dependent induction of persistent synaptic enhancement in rat hippocampus in vivo. Neuroscience. 2007;144:754-61 pubmed
    ..The present studies provide evidence for the rapid induction of a persistent potentiation at hippocampal glutamatergic synapses by endogenous ACh in vivo following disinhibition of inhibitory M2 muscarinic autoreceptors. ..
  48. Holzgrabe U, De Amici M, Mohr K. Allosteric modulators and selective agonists of muscarinic receptors. J Mol Neurosci. 2006;30:165-8 pubmed
    ..The cooperativity is strongly dependent on the pair of allosteric/orthosteric ligands and on the receptor subtype. ..
  49. Bschleipfer T, Schukowski K, Weidner W, Grando S, Schwantes U, Kummer W, et al. Expression and distribution of cholinergic receptors in the human urothelium. Life Sci. 2007;80:2303-7 pubmed
    ..g. by acetylcholine. Its actions are conferred by two classes of receptors, i.e. G-protein-coupled muscarinic receptors (MR) and ionotropic nicotinic receptors (nAChR)...
  50. Qu J, Zhou X, Xie R, Zhang L, Hu D, Li H, et al. The presence of m1 to m5 receptors in human sclera: evidence of the sclera as a potential site of action for muscarinic receptor antagonists. Curr Eye Res. 2006;31:587-97 pubmed
    ..The aim of this study was to identify the presence of muscarinic acetylcholine receptors (mAChRs) in human sclera in order to determine whether the sclera is a potential site of action for mAChR antagonists...
  51. Herrera Morales W, Mar I, Serrano B, Bermudez Rattoni F. Activation of hippocampal postsynaptic muscarinic receptors is involved in long-term spatial memory formation. Eur J Neurosci. 2007;25:1581-8 pubmed
    ..These results support the view that muscarinic receptors are involved in spatial learning and that postsynaptic muscarinic receptors in the dorsal hippocampus are ..
  52. Akiho H, Khan W, Al Kaabi A, Blennerhassett P, Deng Y, Collins S. Cytokine modulation of muscarinic receptors in the murine intestine. Am J Physiol Gastrointest Liver Physiol. 2007;293:G250-5 pubmed
    ..These findings explain the basis for altered muscle contractility observed in Th1 and Th2 models of inflammation, as well as in the post-nematode-infected state...
  53. Liu Q, Wu J, Wang X, Zeng J. Changes in muscarinic acetylcholine receptor expression in form deprivation myopia in guinea pigs. Mol Vis. 2007;13:1234-44 pubmed
    ..In the posterior sclera, expression of the M1 and M4 subtypes significantly increased in FDM eyes. This finding indicates that muscarinic antagonists may have the potential to act directly on the sclera as a strategy to prevent myopia. ..