JNJ-18038683 is a potent and selective
antagonist of the
5HT7serotoninreceptor 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.[1][2]
It binds to the
5-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
^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.
PMID22570363.
S2CID10418102.