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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	10150497
ChEMBL	CHEMBL392760
Hemijski podaci
Formula	C15H13ClN4O2S2
Mol. masa	380,872 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C15H13ClN4O2S2/c16-13-14(19-7-8-23-15(19)18-13)24(21,22)20-9-10(5-6-17)11-3-1-2-4-12(11)20/h1-4,7-9H,5-6,17H2 ; Key: RYBOXBBYCVOYNO-UHFFFAOYSA-N
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

↑ 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
↑ 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. edit
↑ ^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.

Povezano

WAY-208,466

Vanjske veze

	Portal Medicina
	Portal Hemija

[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] 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

[pmid17625499-4] 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. DOI:10.1038/sj.npp.1301503. PMID 17625499.

[pmid17948978-5] 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. DOI:10.1021/jm070521y. PMID 17948978.

[pmid19660530-6] 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. DOI:10.1016/j.neuroscience.2009.07.061. PMID 19660530.

[pmid20217056-7] 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. DOI:10.1007/s00213-010-1798-7. PMC 2910165. PMID 20217056.

[pmid17922111-8] 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. DOI:10.1007/s00213-007-0934-5. PMID 17922111.

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