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Xanomeline
Systematic (IUPAC) name
3-(4-hexoxy-1,2,5-thiadiazol-3-yl)-1-methyl-5,6-dihydro-2H-pyridine
Identifiers
CAS number 131986-45-3
ATC code none
PubChem 60809
ChemSpider 54797
Chemical data
Formula C14H23N3OS 
Mol. mass 281.42 g/mol
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status Uncontrolled

Xanomeline is a muscarinic acetylcholine receptor agonist with reasonable selectivity for the M1 and M4 subtypes.[1][2][3][4] It has been studied for the treatment of both Alzheimer's disease and schizophrenia, particularly the cognitive and negative symptoms,[5] although gastrointestinal side effects led to a high drop-out rate in clinical trials.[6][7] Despite this, xanomeline has been shown to have reasonable efficacy for the treatment of schizophrenia symptoms, and one recent human study found robust improvements in verbal learning and short-term memory associated with xanomeline treatment.[8]

See also

References

  1. ^ Farde L, Suhara T, Halldin C, et al. (1996). "PET study of the M1-agonists [11C]xanomeline and [11C]butylthio-TZTP in monkey and man". Dementia (Basel, Switzerland) 7 (4): 187–95. PMID 8835881. 
  2. ^ Jakubík J, Michal P, Machová E, Dolezal V (2008). "Importance and prospects for design of selective muscarinic agonists". Physiological Research / Academia Scientiarum Bohemoslovaca 57 Suppl 3: S39–47. PMID 18481916. http://www.biomed.cas.cz/physiolres/pdf/57%20Suppl%203/57_S39.pdf. 
  3. ^ Woolley ML, Carter HJ, Gartlon JE, Watson JM, Dawson LA (January 2009). "Attenuation of amphetamine-induced activity by the non-selective muscarinic receptor agonist, xanomeline, is absent in muscarinic M4 receptor knockout mice and attenuated in muscarinic M1 receptor knockout mice". European Journal of Pharmacology 603 (1-3): 147–9. doi:10.1016/j.ejphar.2008.12.020. PMID 19111716. http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(08)01252-1. 
  4. ^ Heinrich JN, Butera JA, Carrick T, et al. (March 2009). "Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists". European Journal of Pharmacology 605 (1-3): 53–6. doi:10.1016/j.ejphar.2008.12.044. PMID 19168056. http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(09)00033-8. 
  5. ^ Lieberman JA, Javitch JA, Moore H (August 2008). "Cholinergic agonists as novel treatments for schizophrenia: the promise of rational drug development for psychiatry". The American Journal of Psychiatry 165 (8): 931–6. doi:10.1176/appi.ajp.2008.08050769. PMID 18676593. http://ajp.psychiatryonline.org/cgi/pmidlookup?view=long&pmid=18676593. 
  6. ^ Messer WS (2002). "The utility of muscarinic agonists in the treatment of Alzheimer's disease". Journal of Molecular Neuroscience : MN 19 (1-2): 187–93. doi:10.1007/s12031-002-0031-5. PMID 12212779. http://dx.doi.org/10.1007/s12031-002-0031-5. 
  7. ^ Mirza NR, Peters D, Sparks RG (2003). "Xanomeline and the antipsychotic potential of muscarinic receptor subtype selective agonists". CNS Drug Reviews 9 (2): 159–86. PMID 12847557. 
  8. ^ Shekhar A, Potter WZ, Lightfoot J, et al. (August 2008). "Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia". The American Journal of Psychiatry 165 (8): 1033–9. doi:10.1176/appi.ajp.2008.06091591. PMID 18593778. http://ajp.psychiatryonline.org/cgi/pmidlookup?view=long&pmid=18593778. 
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