WAY-181,187
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| |||
| (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 
| ||
| 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 | uredi kod]
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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. DOI:10.1038/sj.npp.1301503. PMID 17625499.
- ↑ 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. DOI:10.1021/jm070521y. PMID 17948978.
- ↑ 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. DOI:10.1016/j.neuroscience.2009.07.061. PMID 19660530.
- ↑ 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. DOI:10.1007/s00213-010-1798-7. PMC 2910165. PMID 20217056.
- ↑ 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. DOI:10.1007/s00213-007-0934-5. PMID 17922111.
