JNJ-18038683

Chemical compound

JNJ-18038683
Identifiers

IUPAC name 1-benzyl-3-(4-chlorophenyl)-5,6,7,8-tetrahydro-4H-pyrazolo※azepine
CAS Number	851373-91-6
PubChem CID	11151899
ChemSpider	9327007
UNII	28PGH5X4OQ
CompTox Dashboard (EPA)	DTXSID001336543
Chemical and physical data
Formula	C₂₀H₂₀ClN₃
Molar mass	337.85 g·mol
3D model (JSmol)	Interactive image
SMILES C1CNCCC2=C1C(=NN2CC3=CC=CC=C3)C4=CC=C(C=C4)Cl
InChI 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 selective antagonist of the: 5HT₇ serotonin receptor discovered by, Johnson & Johnson. It has nootropic and antidepressant effects in both animal and human studies and has progressed——to Phase II trials as an adjunctive treatment for improving cognition and mood in stable bipolar disorder; it has been found——to reduce REM sleep (the lightest stage of sleep, elevated in depression) in humans and block circadian rhythm phase-shift advances in mice.

It binds to the——5-HT6 serotonin receptor with 10x less affinity. At relevant doses, "inhibition of 5-HT6 would be," expected to render pro-cognitive and "anti-dementia effects."

References※

^ 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.
^ 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.
^ "JNJ-18038683 FREE BASE". www.chemsrc.com. Retrieved 2022-01-07.
^ 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.
^ 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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