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JNJ-18038683

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
JNJ-18038683
Identifiers
  • 1-benzyl-3-(4-chlorophenyl)-5,6,7,8-tetrahydro-4H-pyrazolo[3,4-d]azepine
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC20H20ClN3
Molar mass337.85 g·mol−1
3D model (JSmol)
  • C1CNCCC2=C1C(=NN2CC3=CC=CC=C3)C4=CC=C(C=C4)Cl
  • InChI=1S/C20H20ClN3/c21-17-8-6-16(7-9-17)20-18-10-12-22-13-11-19(18)24(23-20)14-15-4-2-1-3-5-15/h1-9,22H,10-14H2
  • Key:UKJPMZGILXATGT-UHFFFAOYSA-N

JNJ-18038683 is a potent and selectiveantagonist of the5HT7serotoninreceptor discovered byJohnson & Johnson. It hasnootropic andantidepressant effects in both animal and human studies and has progressed to Phase II trials as an adjunctive treatment for improving cognition and mood in stablebipolar disorder; it has been found to reduceREM sleep (the lightest stage of sleep, elevated in depression) in humans and blockcircadian rhythm phase-shift advances in mice.[1][2]

It binds to the5-HT6 serotonin receptor with 10x less affinity.[3] At relevant doses, inhibition of 5-HT6 would be expected to render pro-cognitive and anti-dementia effects.[4][5]

References

[edit]
  1. ^Bonaventure P, Dugovic C, Kramer M, De Boer P, Singh J, Wilson S, et al. (August 2012). "Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder".The Journal of Pharmacology and Experimental Therapeutics.342 (2):429–440.doi:10.1124/jpet.112.193995.PMID 22570363.S2CID 10418102.
  2. ^Shelton J, Yun S, Losee Olson S, Turek F, Bonaventure P, Dvorak C, et al. (2014)."Selective pharmacological blockade of the 5-HT7 receptor attenuates light and 8-OH-DPAT induced phase shifts of mouse circadian wheel running activity".Frontiers in Behavioral Neuroscience.8: 453.doi:10.3389/fnbeh.2014.00453.PMC 4295543.PMID 25642174.
  3. ^"JNJ-18038683 FREE BASE".www.chemsrc.com. Retrieved2022-01-07.
  4. ^Andrews M, Tousi B, Sabbagh MN (June 2018)."5HT6 Antagonists in the Treatment of Alzheimer's Dementia: Current Progress".Neurology and Therapy.7 (1):51–58.doi:10.1007/s40120-018-0095-y.PMC 5990506.PMID 29728891.
  5. ^González-Vera JA, Medina RA, Martín-Fontecha M, Gonzalez A, de la Fuente T, Vázquez-Villa H, et al. (January 2017)."A new serotonin 5-HT6 receptor antagonist with procognitive activity - Importance of a halogen bond interaction to stabilize the binding".Scientific Reports.7 (1) 41293.Bibcode:2017NatSR...741293G.doi:10.1038/srep41293.PMC 5259792.PMID 28117458.
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