WAY-181,187

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WAY-181,187
WAY-181,187.svg
Systematic (IUPAC) name
2-(1-{6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl}-1H-indol-3-yl)ethan-1-amine
Clinical data
Legal status
?
Identifiers
CAS number ?
ATC code None
PubChem CID 10150497
ChEMBL CHEMBL392760 YesY
Chemical data
Formula C15H13ClN4O2S2 
Mol. mass 380.872 g/mol

WAY-181,187 is a high affinity and selective 5-HT6 receptor full agonist.[1][2] It induces robust increases in extracellular GABA levels in the frontal cortex, hippocampus, striatum, and amygdala of rats without affecting concentrations in the nucleus accumbens or thalamus, and has modest to no effects on norepinephrine, serotonin, dopamine, or glutamate levels in these areas.[1][3] WAY-181,187 has demonstrated preclinical efficacy in rodent models of depression, anxiety, and notably obsessive-compulsive disorder,[1][4] though it has also been shown to impair cognition and memory.[3][5]

See also[edit]

References[edit]

  1. ^ a b c 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. 
  2. ^ 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. 
  3. ^ a b 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. 
  4. ^ 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. 
  5. ^ 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.