Cyproheptadine
CAS No. : 129-03-3
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| Cat. No. : | HY-B1622 |
| M.Wt: | 287.40 |
| Formula: | C21H21N |
| Purity: | >98 % |
| Solubility: | DMSO : 3.17 mg/mL (ultrasonic;warming;adjust pH to 3 with HCl;heat to 60°C) |
Cyproheptadine is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders[1][2].
In Vitro: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].
In Vivo:Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.
Cyproheptadine can be used in animal modeling to create diabetes models. In rats, Cyproheptadine undergoes demethylation and oxidation to form desmethylcyproheptadine (DMCPHepo), while cyproheptadine epoxide (CPHepo) is a minor metabolite. DMCPHepo accumulates in tissues and persists longer than predicted by its plasma concentration profile. DMCPHepo may be an active metabolite of Cyproheptadine and could be associated with islet cell damage. Additionally, the remaining dose of Cyproheptadine may be excreted via feces in the form of the parent compound or its metabolites[1].
Administration: 0-90 mg/kg• p.o. or i.p.• daily for 14 days[3]
Mice: Swiss Webster• male• weighing 25-30 g[3]
Administration: 0-90 mg/kg• p.o.• daily for 14 days[3]
Rabbits: New Zealand white• male• weighing 1000-1500 g[3]
Administration: 0, 225mg/kg• p.o.• daily for 14 days[3]
Hamsters: Golden• male• weighing 100-150 g[3]
Administration: 0-90 mg/kg• p.o.• daily for 14 days[3]
(2)Animals were allowed food and water ad libitum throughout the study unless otherwise stated[3].
Histological analysis: Cyproheptadine induced marked cytoplasmic vacuolization of islet cells in rat pancreas. Vacuoles varied in size and in the most severely affected cells occupied the major portion of the cytoplasm, displacing and slightly compressing the nucleus[3].
Organelle change: The majority of islet cells, presumably the β cell population, showed marked alteration of the rough endoplasmic reticulum and loss of secretory granules. Rough endoplasmic reticulum was vesiculated and the cisternae contained finely granular electron-dense material[3].
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