WAY-181,187
WAY-181,187 je visoko potentan i selektivan pun agonist 5-HT6 receptora.[1][2] 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.[1][3] WAY-181,187 je efikasan u modelima na glodarima za depresiju, anksioznost, i opsesivno-kompulzivni poremećaj,[1][4] mada je pokazano do umanjuje kogniciju i memoriju.[3][5]
 | |
| IUPAC ime | |
|---|---|
2-(16-hloroimidazo[2,1-b][1,3]tiazol-5-sulfonil1H-indol-3-il)etan-1-amin | |
| Identifikatori | |
| ATC kod | none |
| PubChem | CID 10150497 |
| ChEMBL | CHEMBL392760  |
| Hemijski podaci | |
| Formula | C15H13ClN4O2S2 |
| Molarna masa | 380,872 g/mol |
| |
Reference уреди
- ^ а б в Schechter LE; Lin Q; Smith DL; et al. (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.
- ^ Cole DC; Stock JR; Lennox WJ; et al. (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.
- ^ а б West PJ, Marcy VR, Marino MJ, Schaffhauser H (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.
- ^ Carr GV, Schechter LE, Lucki I (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.
- ^ Loiseau F, Dekeyne A, Millan MJ (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.
