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The H3-receptor decreases neurotransmitter release: histamine, acetylcholine, norepinephrine, serotonin. Thus, H3-receptor-antagonists increases cognition, vigilance, and wakefulness. Ciproxifan—produces wakefulness and attentiveness in animal studies, and produced cognitive enhancing effects without prominent stimulant effects at relatively low levels of receptor occupancy, and pronounced wakefulness at higher doses.[117] A-349,821—It has nootropic effects in animal studies.[118] ABT-239 – strong H3 receptor inverse agonist that is more active than ciproxifan, but its investigation into human use was dropped after it was discovered to cause QT prolongation in subjects Betahistine Modafinil |
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