Cyproheptadine is a potent, orally active antagonist of the 5-HT 2A receptor with antidepressant, antiserotonergic, antiplatelet, and thromboprotective effects, useful in thromboembolic disorders research [1] [2].

Cyproheptadine, in concentrations ranging from 0.01 to 100 nM and applied for 1 minute, effectively inhibits serotonin-enhanced ADP-induced platelet aggregation in mice in a dose-dependent manner in vitro [2]. At a concentration of 10 nM, it also inhibits serotonin-enhanced ADP-induced tyrosine phosphorylation in platelets at 1 μM ADP and 15 μM serotonin levels in vitro [2]. Furthermore, Cyproheptadine suppresses PS exposure (Annexin V), P-selectin, and GPIIb-IIIa (PAC-1 binding) activation in human platelets 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.