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The Sound of Evolution
Cyproheptadine
Mechanism of action:
Cyproheptadine is a first-generation H₁ receptor antagonist. Cyproheptadine binds to H₁ receptors, preventing histamine from binding and blocking histamine-induced capillary dilation, increased vascular permeability, and smooth muscle contraction. Cyproheptadine is also a serotonin 5-HT₂ receptor antagonist and can inhibit serotonin-induced vasoconstriction and appetite suppression.
Reference(s):
1. Tokunaga S et al. (2007). Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci.
2. Milani N et al. (2020). Use of phenotypically poor metabolizer individual donor human liver microsomes to identify selective substrates of UGT2B10. Drug Metab Dispos.
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