Cyproheptadine
Based on 4 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 129-03-3
- Formula: C21H21N
- Molecular Weight:287.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Cyproheptadine
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Biological Activity
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5-HT2A Receptor |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (8-10 weeks old)[2]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; daily, for 5 days
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Result:Prolonged occlusion times and tail bleeding times in mice.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 129-03-3
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Appearance Solid
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Molecular Weight 287.40
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Formula C21H21N
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Color White to off-white
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SMILES
CN1CC/C(CC1)=C2C3=CC=CC=C3C=CC4=CC=CC=C/24
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Front Pharmacol
Prediction of Synergistic Drug Combinations for Prostate Cancer by Transcriptomic and Network Characteristics. [Abstract]2021 Apr 12;12:634097. PMID: 33986671 -
PLoS Negl Trop Dis
Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]2019 Aug 20;13(8):e0007681. PMID: 31430351 -
Cureus
2023 Nov 27;15(11):e49530. PMID: 38033435 -
Cureus
2023 Nov 27;15(11):e49530. PMID: 38033435
Solvent & Solubility
DMSO : 3.17 mg/mL (11.03 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (302 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Iwaki M, et al. Pharmacokinetics of cyproheptadine and its metabolites in rats. Biol Pharm Bull. 1993 Dec;16(12):1276-81. [Content Brief]
[2]. Codd EE, et al. Diabetogenic effect of a series of tricyclic delta opioid agonists structurally related to cyproheptadine. Toxicol Sci. 2010 Oct;117(2):493-504. [Content Brief]
[3]. Wold JS, et al. Species dependent pancreatic islet toxicity produced by cyproheptadine: alterations in beta cell structure and function. Toxicol Appl Pharmacol. 1971 Jun;19(2):188-201. [Content Brief]
[4]. Padrid PA, et al. Cyproheptadine-induced attenuation of type-I immediate-hypersensitivity reactions of airway smooth muscle from immune-sensitized cats. Am J Vet Res. 1995 Jan;56(1):109-15. Erratum in: Am J Vet Res 1995 Mar;56(3):402. [Content Brief]
[5]. Calka O, et, al. Effect of cyproheptadine on serum leptin levels. Adv Ther, 2005. 22(5): p. 424-8. [Content Brief]
[6]. Olivia A Lin, et al. The Antidepressant 5-HT2A Receptor Antagonists Pizotifen and Cyproheptadine Inhibit Serotonin-Enhanced Platelet Function. PLoS One. 2014; 9(1): e87026. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.4795 mL | 17.3974 mL | 34.7947 mL | 86.9868 mL |
| 5 mM | 0.6959 mL | 3.4795 mL | 6.9589 mL | 17.3974 mL | |
| 10 mM | 0.3479 mL | 1.7397 mL | 3.4795 mL | 8.6987 mL |
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