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
Identifiers
CAS Number 554403-49-5
ATC code none
PubChem CID 10150497
IUPHAR/BPS 3240
ChemSpider 8326005
UNII WXE3H7W295 YesY
ChEMBL CHEMBL392760 YesY
Chemical data
Formula C15H13ClN4O2S2
Molar 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 2910165free to read. 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.