WAY-181,187

Iz Wikipedije, slobodne enciklopedije
Idi na navigaciju Idi na pretragu
WAY-181,187
(IUPAC) ime
2-(16-hloroimidazo[2,1-b][1,3]tiazol-5-sulfonil1H-indol-3-il)etan-1-amin
Klinički podaci
Identifikatori
ATC kod nije dodeljen
PubChem[1][2] 10150497
ChEMBL[3] CHEMBL392760 YesY
Hemijski podaci
Formula C15H13ClN4O2S2 
Mol. masa 380,872 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

WAY-181,187 je visoko potentan i selektivan pun agonist 5-HT6 receptora.[4][5] On indukuje robustno povišenje ekstracelularnih GABA nivoa u frontalnom režnju, hipokampusu, strijatumu, i amigdali kod pacova, nema uticaja na koncentraciju u cingularnom režnju ili talamusu, i umereno utiče na nivoe norepinefrina, serotonina, dopamina, ili glutamata u tim oblastima.[4][6] WAY-181,187 je efikasan u modelima na glodarima za depresiju, anksioznost, i opsesivno-kompulzivni poremećaj,[4][7] mada je pokazano do umanjuje kogniciju i memoriju.[6][8]

Reference[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. 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. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  4. 4,0 4,1 4,2 Schechter LE, Lin Q, Smith DL et al. (May 2008). "Neuropharmacological profile of novel and selective 5-HT6 receptor agonists: WAY-181187 and WAY-208466". Neuropsychopharmacology 33 (6): 1323–35. PMID 17625499. doi:10.1038/sj.npp.1301503. 
  5. Cole DC, Stock JR, Lennox WJ et al. (November 2007). "Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist". Journal of Medicinal Chemistry 50 (23): 5535–8. PMID 17948978. doi:10.1021/jm070521y. 
  6. 6,0 6,1 West PJ, Marcy VR, Marino MJ, Schaffhauser H (December 2009). "Activation of the 5-HT(6) receptor attenuates long-term potentiation and facilitates GABAergic neurotransmission in rat hippocampus". Neuroscience 164 (2): 692–701. PMID 19660530. doi:10.1016/j.neuroscience.2009.07.061. 
  7. Carr GV, Schechter LE, Lucki I (March 2010). "Antidepressant and anxiolytic effects of selective 5-HT(6) receptor agonists in rats". Psychopharmacology 213 (2–3): 499–507. PMC 2910165. PMID 20217056. doi:10.1007/s00213-010-1798-7. 
  8. Loiseau F, Dekeyne A, Millan MJ (January 2008). "Pro-cognitive effects of 5-HT6 receptor antagonists in the social recognition procedure in rats: implication of the frontal cortex". Psychopharmacology 196 (1): 93–104. PMID 17922111. doi:10.1007/s00213-007-0934-5. 

Vidi još[uredi - уреди | uredi izvor]

Spoljašnje veze[uredi - уреди | uredi izvor]