41354-29-4

Basic information

• Product Name: Cyproheptadine hydrochloride
• Synonyms: CYPROHEPTADINE HCL;CYPROHEPTADINE HYDROCHLORIDE;CYPROHEPTADINE HYDROCHLORIDE HYDRATE;CYPROHEPTADINE HYDROCHLORIDE SESQUIHYDRATE;4-(5H-DIBENZO[A,D]CYCLOHEPTEN-5-YLIDINE)-METHYLPIPERIDINE HYDROCHLORIDE;CYPROHEPTADINE HCL USP(CRM STANDARD);CYPROHEPTADINE HYDROCHLORIDE EPC(CRM STANDARD);CyproheptadineHclUspGrade
• CAS NO: 41354-29-4
• Molecular Formula: C21H22ClN
• Molecular Weight: 323.86
• EINECS: 213-535-1
• Product Categories: Building Blocks;Heterocyclic Building Blocks;Piperidines;API;PERIACTIN
• Mol File: 41354-29-4.mol
• Article Data: 0

Chemical Properties

• Melting Point: 165 °C (dec.)(lit.)
• Boiling Point: 440.1oC at 760 mmHg
• Flash Point: 194.5oC
• Appearance: white to slightly yellow/
• Storage Temp.: Inert atmosphere,Room Temperature
• Solubility: ethanol: soluble
• Merck: 14,2773
• CAS DataBase Reference: Cyproheptadine hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: Cyproheptadine hydrochloride(41354-29-4)
• EPA Substance Registry System: Cyproheptadine hydrochloride(41354-29-4)

Safety Data

• Hazard Codes: Xn
• Statements: 22-36/37/38
• Safety Statements: 26-36
• RIDADR: UN 2811 6.1/PG 3
• WGK Germany: 3
• RTECS: TM7050000
• HazardClass: 6.1
• PackingGroup: III
• Hazardous Substances Data: 41354-29-4(Hazardous Substances Data)

Usage

Description

Cyproheptadine hydrochloride, also known as Periactin, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. It is a 5-HT2/5-HT1C serotonin receptor antagonist and an H1 histamine receptor antagonist. Cyproheptadine hydrochloride is used for the relief of allergic conditions and has a sedating effect with antimuscarinic and calcium-channel blocking actions.

Uses

Used in Pharmaceutical Industry:
Cyproheptadine hydrochloride is used as an antihistamine for the treatment of allergic conditions such as rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria, angioedema, and pruritic skin disorders.
Used in Anticoagulant and Anti-allergic Drug Applications:
Cyproheptadine hydrochloride is used as an anti-coagulant and anti-allergic drug for conditions like urticaria, eczema, allergic contact dermatitis, skin itching, and other allergic reactions.
Used in H1-antihistamine and Antipruritic Applications:
Cyproheptadine hydrochloride is used as an H1-antihistamine and antipruritic for the relief of itching and other symptoms associated with histamine release.
Used in Structural Studies of Antihistamines:
Cyproheptadine hydrochloride is used in structural studies of antihistamines to understand its mechanism of action and potential applications in various conditions.
Used in Testing Anti-inflammatory Activity:
Cyproheptadine hydrochloride sesquihydrate has been used in testing anti-inflammatory activity in serotonin receptor (5-HT) induced inflammation.
Used in Inhibition of 5-HT in Bioassays:
Cyproheptadine hydrochloride sesquihydrate has been used in the inhibition of 5-HT in in vivo and in vitro bioassays in crabs and embryo physiological experiments.
Used in Inhibition of Calcitonin Gene-Related Peptide (CGRP):
Cyproheptadine hydrochloride is used for the inhibition of calcitonin gene-related peptide (CGRP), which is involved in various physiological processes, including pain transmission and inflammation.
Used in Preventive Effect Against Pregolide-Induced Valvulopathy:
Cyproheptadine hydrochloride sesquihydrate has been used to induce a preventive effect against the development of pergolide-induced valvulopathy in a rat model.
Chemical Properties:
Cyproheptadine hydrochloride is a white or slightly yellow, crystalline powder.
Brand Name:
The brand name for Cyproheptadine hydrochloride is Periactin, manufactured by Merck.

Antihistamines

Cyproheptadine hydrochloride is a kind of pipecolic antihistamines,it can compete with histamine released from the organization for H1 receptor on effector cells , thereby it can prevent the onset of an allergic reaction, and release histamine-induced spasm and congestion effects, this product has a strong H1 receptor antagonism, its anti-histamine effect is stronger than chlorpheniramine, promethazine . There are mild to moderate anti-serotonin effects and anticholinergic effects. In addition, there is a stimulate appetite effect, and weight gains after a certain time. Clinically cyproheptadine hydrochloride is mainly used for acute and chronic urticaria (especially it has a good effect on cold urticaria ), papular urticaria, angioedema, atopic eczema, contact dermatitis, food allergy, drug allergy, allergic rhinitis, hay fever, allergic conjunctivitis, allergic to insect stings and migraine. It has some therapeutic effect on bronchial asthma . It is acceptable for the adjuvant treatment of Cushing's syndrome, acromegaly. In addition,as an appetite enhancer,it is used for neuropathic fear of food. There are reports about acanthosis nigricans treatment, prevention of necrotizing pyoderma. 【Dosage 】oral often release dosage : (1) allergic diseases: adult, once 2~4mg, one day 2 or 3 times. (2) Cushing's syndrome, applicable to the treatment of cases of bilateral adrenal hyperplasia,it can inhibit the hypothalamic release of corticotropin releasing hormone (CRH) and inhibit the secretion of pituitary adrenocorticotropic hormone (ACTH), thereby lowering plasma ACTH and cortisol levels; adults start one day 8mg,which can be gradually increased to one day24mg; the usual dose is one day 12~24mg, divided doses,it needs long-term use; in the case of cortical function inadequate after total resection or subtotal bilateral adrenal, on one hand ,supple corticosteroids, on the other hand,take cyproheptadine,which can reduce the chance of occurrence of pituitary tumors. The above information is edited by the lookchem of Tian Ye.

Biochem/physiol Actions

Cyproheptadine hydrochloride sesquihydrate is a serotonin receptor (5-HT2/5-HT1C) antagonist, H1 histamine receptor antagonist and an antipruritic. The inhibition of 5-HT by cyproheptadine improves cognitive function in schizophrenia disorder. Cyproheptadine is effective for treating functional gastrointestinal disorders (FGIDs). Food and Drug Administration (FDA) approved cyproheptadine, has antidepressant and antiplatelet functionality. It may be effective in treating thromboembolic disorders. Cyproheptadine inhibits lysine methyltransferase 7/9 (Set7/9) leading to a decrease in estrogen receptor (ERα) expression and growth arrest in breast cancer cells.

Veterinary Drugs and Treatments

Cyproheptadine may be useful in cats as an appetite stimulant. It potentially may be of benefit in the treatment of feline asthma or pruritus in cats, but clinical experience is marginal for this indication. Cyproheptadine is an antihistamine but its efficacy is questionable for this indication in dogs. The drug may be useful as adjunctive therapy for Cushing’s syndrome probably as result of its antiserotonin activity, however one study demonstrated efficacy in less than 10% of dogs treated for pituitary dependent hyperadrenocorticism. Cyproheptadine may be useful as adjunctive treatment in dogs or cats with serotonin syndrome. In horses, cyproheptadine has been used for treating photic head shaking and pars intermedia dysfunction (Equine Cushing’s Disease).