| Size | Price | Stock | Qty |
|---|---|---|---|
| 10g |
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| 50g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
5-HT2 Receptor
Cyproheptadine HCl hydrate targets histamine H1 receptors, muscarinic receptors, and serotonin 5-HT2 receptors. It acts as an antagonist at these receptors, blocking the effects of histamine, acetylcholine, and serotonin. This multi-receptor antagonism underlies its diverse pharmacological effects, including antihistamine, anticholinergic, and antiserotonergic actions. |
|---|---|
| ln Vitro |
Cyproheptadine HCl hydrate binds to histamine H1, muscarinic, and serotonin 5-HT2 receptors with Ki values of 0.38, 1.26, and 0.83 nM, respectively. It induced a preventive effect against the development of pergolide-induced valvulopathy in a rat model. It is a serotonin antagonist and histamine H1 receptor blocker.
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| ln Vivo |
Cyproheptadine HCl hydrate is used as an antipruritic, appetite stimulant, anti-allergic agent, and for the treatment of dumping syndrome after gastrectomy. It induced a preventive effect against the development of pergolide-induced valvulopathy in a rat model. It is a sedating antihistamine.
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| Enzyme Assay |
Cyproheptadine HCl hydrate is evaluated in cell-free receptor binding assays to determine its affinity for histamine H1, muscarinic, and serotonin 5-HT2 receptors. Radioligand binding displacement assays are performed using membrane preparations expressing these receptors. Ki values are determined.
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| Cell Assay |
Cyproheptadine HCl hydrate is assessed in cell-based assays to measure its antagonist activity at histamine H1, muscarinic, and serotonin 5-HT2 receptors. Cells expressing these receptors are treated with the compound, and receptor activity is measured by assessing downstream signaling pathways.
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| Animal Protocol |
Cyproheptadine HCl hydrate is administered in animal models to evaluate its antihistamine, antiserotonergic, and anticholinergic effects. It has been studied in models of allergy, appetite regulation, and valvulopathy. However, specific animal study protocols are not extensively documented.
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| ADME/Pharmacokinetics |
Cyproheptadine HCl hydrate has a molecular weight of 350.88 and a molecular formula of C21H21N·HCl·1.5H2O. It has a CAS number of 41354-29-4. The compound is hygroscopic and should be stored under nitrogen at -20°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Cyproheptadine HCl hydrate beyond its known use as a medication. The compound is a therapeutic agent and is not for research purposes only. It is generally well-tolerated but can cause sedation and other side effects.
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| References | |
| Additional Infomation |
Cyproheptadine hydrochloride sesquihydrate is the sesquihydrate of cyproheptadine hydrochloride. It's important to note that when people refer to cyproheptadine hydrochloride, they are usually referring to cyproheptadine hydrochloride sesquihydrate. It is an antihistamine with sedative effects, as well as anticholinergic and calcium channel blocking effects. It is used to relieve allergic diseases, including inhaled allergen and food-induced rhinitis, conjunctivitis, urticaria, and angioedema, as well as pruritic skin diseases. Unlike other antihistamines, it is also a serotonin receptor antagonist, and therefore can be used to treat vascular headaches and anorexia. It has various pharmacological effects, including serotonergic antagonist, antipruritic, anti-allergic, gastrointestinal, and H1 receptor antagonist. This product contains cyproheptadine hydrochloride (anhydrous). Cyproheptadine hydrochloride is the hydrochloride salt of a synthetic methylpiperidine derivative, possessing antihistamine and antiserotonergic properties. Cyproheptadine competitively binds to HA receptors with free histamine (HA), thereby competitively antagonizing the stimulatory effects of histamine on HA receptors in the gastrointestinal tract, large blood vessels, and bronchial smooth muscle. It also competitively binds to serotonin receptors with free serotonin. Cyproheptadine has anticholinergic and sedative effects and has been shown to stimulate appetite and increase weight. (NCI04)
A serotonin antagonist and histamine H1 receptor blocker, used as an antipruritic, appetite stimulant, anti-allergic agent, and for the treatment of dumping syndrome after gastrectomy, etc. See also: Cyproheptadine hydrochloride (note moved to). Cyproheptadine HCl hydrate is a sedating antihistamine with antiserotonergic and anticholinergic activities. It has a CAS number of 41354-29-4. It is used as an antipruritic, appetite stimulant, anti-allergic agent, and for the treatment of dumping syndrome. It is a therapeutic agent. |
| Molecular Formula |
C21H21N.HCL.1.5H2O
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|---|---|
| Molecular Weight |
350.0
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| Exact Mass |
287.17
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| Elemental Analysis |
C, 71.88; H, 7.18; Cl, 10.10; N, 3.99; O, 6.84
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| CAS # |
41354-29-4
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| Related CAS # |
Cyproheptadine hydrochloride; 969-33-5
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| PubChem CID |
11954233
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| Appearance |
White to off-white solid powder
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| Boiling Point |
440.1ºC at 760 mmHg
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| Melting Point |
165 °C (dec.)(lit.)
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| Flash Point |
194.5ºC
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| LogP |
5.373
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
0
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| Heavy Atom Count |
49
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| Complexity |
423
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1CC/C(CC1)=C2C3=CC=CC=C3C=CC4=CC=CC=C/24.[H]Cl.[1.5H2O]
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| InChi Key |
OERTXEVZEWASFH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21N.ClH.H2O/c1-22-12-10-16(11-13-22)21-15-18-7-3-2-6-17(18)14-19-8-4-5-9-20(19)21;;/h2-9,14-15H,10-13H2,1H3;1H;1H2
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| Chemical Name |
4-(dibenzo[1,2-a:1',2'-e][7]annulen-11-ylidene)-1-methylpiperidine hydrochloride sesquihydrate
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| Synonyms |
Periactin; Eiproheptadine; Cyproheptadine Hydrochloride; Sesquihydrate; Periactinol; Dronactin; Ciproheptadina; Peritol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~33.3 mg/mL (~95 mM)
H2O: ~0.67 mg/mL (~1.9 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8571 mL | 14.2857 mL | 28.5714 mL | |
| 5 mM | 0.5714 mL | 2.8571 mL | 5.7143 mL | |
| 10 mM | 0.2857 mL | 1.4286 mL | 2.8571 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02418949 | Active Recruiting |
Drug: Placebo for Cyproheptadine Drug: Cyproheptadine |
Stroke Hemiparesis Muscle Spasticity |
Shirley Ryan AbilityLab | November 2015 | Not Applicable |
| NCT06175273 | Not yet recruiting | Drug: Cyproheptadine Drug: Dronabinol Other: Standard of Care |
Pediatric Cancer Muscle Loss Malnutrition, Child |
Corey Hawes | January 2024 | Phase 2 Phase 3 |
| NCT05469165 | Recruiting | Drug: Cyproheptadine 4 Mg Oral Tablet Other: Placebo |
Ischemic Mitral Regurgitation | Laval University | June 20, 2023 | Phase 2 |
| NCT06147622 | Not yet recruiting | Drug: Prazosin + cyproheptadine Drug: KT110 |
Alcohol Use Disorder | Kinnov Therapeutics | February 2024 | Phase 1 |
| NCT00066248 | Completed | Drug: cyproheptadine hydrochloride Drug: megestrol acetate |
Brain Tumor Cachexia Leukemia Lymphoma |
University of South Florida | June 2003 | Phase 2 |
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