Cyproheptadine is a potent and orally active antagonist of the 5-HT 2A receptor. Cyproheptadine has antidepressant and antiserotonergic effects. Cyproheptadine also has antiplatelet and thromboprotective activities that can be used in thromboembolic disorders research [1] [2].

Cyproheptadine (0.01-100 nM; 1 minute) dose-dependently inhibits serotonin-enhanced ADP-induced mouse platelet aggregation in vitro [2]. Cyproheptadine (10 nM) has the ability to inhibit 15 μM serotonin-enhanced ADP-induced (1 μM) tyrosine phosphorylation in platelets in vitro [2]. Cyproheptadine inhibits human platelet PS exposure (Annexin V), P-selectin, and GPIIb-IIIa (PAC-1 binding) activation in vitro [2].

Cyproheptadine (1 mg/kg; i.p.; daily, for 5 days; C57BL/6 mice) exerts thromboprotective properties in vivo [2]. Animal Model: C57BL/6 mice (8-10 weeks old) [2] Dosage: 1 mg/kg Administration: Intraperitoneal injection; daily, for 5 days Result: Prolonged occlusion times and tail bleeding times in mice.