Ksanomelin

Из Википедије, слободне енциклопедије
Ksanomelin
(IUPAC) ime
3-(4-heksoksi-1,2,5-tiadiazol-3-il)-1-metil-5,6-dihidro-2H-piridin
Klinički podaci
Identifikatori
CAS broj 131986-45-3
ATC kod nije dodeljen
PubChem[1][2] 60809
ChemSpider[3] 54797
UNII 9ORI6L73CJ YesY
KEGG[4] D06330
ChEMBL[5] CHEMBL21536
Hemijski podaci
Formula C14H23N3OS 
Mol. masa 281,42 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

Ksanomelin (LY-246,708, Lumeron, Memkor) je agonist muskarisnkog acetilholinskog receptora sa umerenom selektivnošću za M1 i M4 podtipove.[6][7][8][9] Nije poznato da ksanomelin deluje kao antagonist M5 receptora.[10] On je bio ispitivan za lečenje Alchajmerove bolesti i šizofrenije, posebno kognitivnih i negativnih simptoma.[11] Gastrointestinalne nuspojave su dovele do visoke stope napuštanja kliničkih ispitivanja.[12][13] 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.[14]

Reference[уреди]

  1. ^ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.“. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ^ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities“. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ^ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining“. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ^ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG“. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. ^ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery“. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  6. ^ 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. 
  7. ^ 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. 
  8. ^ 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. 
  9. ^ 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. 
  10. ^ Grant MK, El-Fakahany EE (October 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. 
  11. ^ 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. 
  12. ^ 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. 
  13. ^ 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. 
  14. ^ 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. 

Vidi još[уреди]

Spoljašnje veze[уреди]