WAY-181,187

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WAY-181,187
WAY-181,187.svg
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C15H13ClN4O2S2
Molar mass 380.872 g/mol
3D model (Jmol)

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. PMID 17625499. doi:10.1038/sj.npp.1301503. 
  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. PMID 17948978. doi:10.1021/jm070521y. 
  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. PMID 19660530. doi:10.1016/j.neuroscience.2009.07.061. 
  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. PMC 2910165Freely accessible. PMID 20217056. doi:10.1007/s00213-010-1798-7. 
  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. PMID 17922111. doi:10.1007/s00213-007-0934-5.