2. Induced Disease Models Products GPCR/G Protein Neuronal Signaling Apoptosis
  3. Endocrine and Metabolic Disease Models 5-HT Receptor Apoptosis
  4. Diabetes Models
  5. Cyproheptadine

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.

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Cyproheptadine Chemical Structure

Cyproheptadine Chemical Structure

CAS No. : 129-03-3

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Based on 3 publication(s) in Google Scholar

Other Forms of Cyproheptadine:

Cyproheptadine Related Antibodies

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Description

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cyproheptadine Related Antibodies
In Vivo

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].

Induction of diabetes disease[1].
Background
Cyproheptadine and its several metabolites, including desmethyl Cyproheptadine epoxide (DMCPH epoxide), desmethyl Cyproheptadine (DMCPH) and Cyproheptadine epoxide, inhibit insulin synthesis as well as glucose and stimulated insulin release[1].
Specific Mmodeling Methods
Rat: Wistar• male• weighing 150-225 g[3]
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]
Note
(1)Oral doses of Cyproheptadine were administered in aqueous solution or in an aqueous suspension containing 0.15 % methylcellulose. Intraperitoneally (ip)-treated rats received cyproheptadine in saline solution. Animals were sacrificed 24 h after the last dose[3].
(2)Animals were allowed food and water ad libitum throughout the study unless otherwise stated[3].
Modeling Indicators
Morphological change: Cyproheptadine caused a depression in weight gain and exhibited a markedly diminished glucose tolerance in animals[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].
Correlated Product(s): /
Opposite Product(s): /

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

287.40

Formula

C21H21N
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1CC/C(CC1)=C2C3=CC=CC=C3C=CC4=CC=CC=C/24
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4795 mL 17.3974 mL 34.7947 mL
5 mM 0.6959 mL 3.4795 mL 6.9589 mL
View the 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.

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Purity & Documentation
References

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
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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Cyproheptadine Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cyproheptadine129-03-35-HT ReceptorApoptosisSerotonin Receptor5-hydroxytryptamine ReceptorpiperidineantihistamineantiserotonergicantiplateletthromboprotectiveInhibitorinhibitorinhibit

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