Ksanomelin

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Ksanomelin
Xanomeline.png
IUPAC ime
3-(4-heksoksi-1,2,5-tiadiazol-3-il)-1-metil-5,6-dihidro-2H-piridin
Identifikatori
CAS broj 131986-45-3 ДаY
ATC kod None
PubChem CID 60809
ChemSpider 54797
UNII 9ORI6L73CJ ДаY
KEGG D06330
ChEMBL CHEMBL21536
Hemijski podaci
Formula C14H23N3OS
Molarna masa 281,42 g/mol

Ksanomelin (LY-246,708, Lumeron, Memkor) je agonist muskarisnkog acetilholinskog receptora sa umerenom selektivnošću za M1 i M4 podtipove.[1][2][3][4] Nije poznato da ksanomelin deluje kao antagonist M5 receptora.[5] On je bio ispitivan za lečenje Alchajmerove bolesti i šizofrenije, posebno kognitivnih i negativnih simptoma.[6] Gastrointestinalne nuspojave su dovele do visoke stope napuštanja kliničkih ispitivanja.[7][8] Uprkos tome, za ksanomelin je pokazano da ima umerenu efikasnost u lečenju simptoma šizofrenije. Jedna nedavna studija je utvrdila robustno poboljšanje pri verbalnom učenju i u kratkotrajnoj memoriji usled tretmana ksanomelinom.[9]

Reference[уреди]

  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” (PDF). Physiological Research / Academia Scientiarum Bohemoslovaca. 57 Suppl 3: S39—47. PMID 18481916. 
  3. Woolley ML, Carter HJ, Gartlon JE, Watson JM, Dawson LA (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. 
  4. Heinrich JN, Butera JA, Carrick T; et al. (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. 
  5. Grant MK, El-Fakahany EE (2005). „Persistent binding and functional antagonism by xanomeline at the muscarinic M5 receptor”. The Journal of Pharmacology and Experimental Therapeutics 315 (1): 313—9. doi:10.1124/jpet.105.090134. PMID 16002459. 
  6. Lieberman JA, Javitch JA, Moore H (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. 
  7. 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. 
  8. 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. doi:10.1111/j.1527-3458.2003.tb00247.x. PMID 12847557. 
  9. Shekhar A, Potter WZ, Lightfoot J; et al. (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. 

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