CYPROHEPTADINE OROTATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C21H21N.C5H4N2O4
Molecular Weight	443.4944
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)C1=CC(=O)NC(=O)N1.CN2CCC(CC2)=C3C4=CC=CC=C4C=CC5=CC=CC=C35

InChI

InChIKey=VSFJAKGNJUZEHH-UHFFFAOYSA-N

InChI=1S/C21H21N.C5H4N2O4/c1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21;8-3-1-2(4(9)10)6-5(11)7-3/h2-11H,12-15H2,1H3;1H,(H,9,10)(H2,6,7,8,11)

HIDE SMILES / InChI

Description
Sources: https://www.drugs.com/dosage/cyproheptadine.htmlhttps://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf
Curator's Comment: description was created based on several sources, including: https://www.drugs.com/monograph/cyproheptadine-hydrochloride.html | http://www.mentalmeds.org/prescription_meds/Periactin.pdf

Cyproheptadine hydrochloride anhydrous is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. It is indicted for the treatment of perennial and seasonal allergic rhinitis; vasomotor rhinitis; allergic conjunctivitis due to inhalant allergens and foods; mild, uncomplicated allergic skin manifestations of urticaria and angioedema. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. MAO inhibitors prolong and intensify the anticholinergic effects of antihistamines. Antihistamines may have additive effects with alcohol and other CNS depressants, e.g., hypnotics, sedatives, tranquilizers, antianxiety agents. Common adverse effects are: sedation, sleepiness (often transient), dizziness, disturbed coordination, restlessness, excitation.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Histamine H1 receptor 315 Target ID: CHEMBL3943 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6261070	Antagonist 2778	2.7 nM [Ki]
Serotonin 2 (5-HT2) receptor 87 Target ID: CHEMBL2093870 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6261070	Antagonist 2778	6.5 nM [Ki]
Serotonin 2a (5-HT2a) receptor 231 Target ID: CHEMBL322 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9178521 \| https://www.ncbi.nlm.nih.gov/pubmed/12498911	Antagonist 2778	8.8 null [pKi]
Muscarinic acetylcholine receptor 160 Target ID: CHEMBL1907609 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6261070	Antagonist 2778	19.0 nM [Ki]
Histamine H1 receptor 315 Target ID: CHEMBL3943 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7650688	Antagonist 2778	0.537 nM [Ki]
Serotonin 2a (5-HT2a) receptor 231 Target ID: CHEMBL322 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11229772	Antagonist 2778	1.6 nM [Ki]
Serotonin 2c (5-HT2c) receptor 124 Target ID: CHEMBL3006 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11266163	Antagonist 2778	11.0 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Vasomotor rhinitis 21 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8429	CYPROHEPTADINE HYDROCHLORIDE Approved Use Cyproheptadine hydrochloride is indicated for the treatment of Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis due to inhalant allergens and foods; Mild, uncomplicated allergic skin manifestations of urticaria and angioedema; Amelioration of allergic reactions to blood or plasma; Cold urticaria; Dermatographism; As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1980
Perennial allergic rhinitis 47 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8429	CYPROHEPTADINE HYDROCHLORIDE Approved Use Cyproheptadine hydrochloride is indicated for the treatment of Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis due to inhalant allergens and foods; Mild, uncomplicated allergic skin manifestations of urticaria and angioedema; Amelioration of allergic reactions to blood or plasma; Cold urticaria; Dermatographism; As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1980
Seasonal allergic rhinitis 64 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8429	CYPROHEPTADINE HYDROCHLORIDE Approved Use Cyproheptadine hydrochloride is indicated for the treatment of Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis due to inhalant allergens and foods; Mild, uncomplicated allergic skin manifestations of urticaria and angioedema; Amelioration of allergic reactions to blood or plasma; Cold urticaria; Dermatographism; As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1980
Allergic conjunctivitis 100 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8429	CYPROHEPTADINE HYDROCHLORIDE Approved Use Cyproheptadine hydrochloride is indicated for the treatment of Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis due to inhalant allergens and foods; Mild, uncomplicated allergic skin manifestations of urticaria and angioedema; Amelioration of allergic reactions to blood or plasma; Cold urticaria; Dermatographism; As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1980
Urticaria 39 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8429	CYPROHEPTADINE HYDROCHLORIDE Approved Use Cyproheptadine hydrochloride is indicated for the treatment of Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis due to inhalant allergens and foods; Mild, uncomplicated allergic skin manifestations of urticaria and angioedema; Amelioration of allergic reactions to blood or plasma; Cold urticaria; Dermatographism; As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1980
Angioedema 20 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8429	CYPROHEPTADINE HYDROCHLORIDE Approved Use Cyproheptadine hydrochloride is indicated for the treatment of Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis due to inhalant allergens and foods; Mild, uncomplicated allergic skin manifestations of urticaria and angioedema; Amelioration of allergic reactions to blood or plasma; Cold urticaria; Dermatographism; As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1980
Anaphylaxis 46 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8429	CYPROHEPTADINE HYDROCHLORIDE Approved Use Cyproheptadine hydrochloride is indicated for the treatment of Perennial and seasonal allergic rhinitis; Vasomotor rhinitis; Allergic conjunctivitis due to inhalant allergens and foods; Mild, uncomplicated allergic skin manifestations of urticaria and angioedema; Amelioration of allergic reactions to blood or plasma; Cold urticaria; Dermatographism; As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1980
Cold urticaria 10 Sources: https://www.drugs.com/pro/cyproheptadine.html	Primary	Approved 8429	PERIACTIN Approved Use Indications and Usage. Perennial and seasonal allergic rhinitis, Vasomotor rhinitis, Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Amelioration of allergic reactions to blood or plasma, Cold urticaria, Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1961
Vasomotor rhinitis 21 Sources: https://www.drugs.com/pro/cyproheptadine.html	Primary	Approved 8429	PERIACTIN Approved Use Indications and Usage. Perennial and seasonal allergic rhinitis, Vasomotor rhinitis, Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Amelioration of allergic reactions to blood or plasma, Cold urticaria, Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1961
Uncomplicated allergic skin manifestations of angioedema 10 Sources: https://www.drugs.com/pro/cyproheptadine.html	Primary	Approved 8429	PERIACTIN Approved Use Indications and Usage. Perennial and seasonal allergic rhinitis, Vasomotor rhinitis, Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Amelioration of allergic reactions to blood or plasma, Cold urticaria, Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Launch Date 1961

C_max

Value	Dose	Co-administered	Analyte	Population
1.25 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21432861	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: COBAMAMIDE	COBAMAMIDE	CYPROHEPTADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
40.82 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21432861	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: COBAMAMIDE	COBAMAMIDE	CYPROHEPTADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
38.21 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21432861	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: COBAMAMIDE	COBAMAMIDE	CYPROHEPTADINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
0.227 mg/kg 3 times / day multiple, digestive tract route (median) Recommended Dose: 0.227 mg/kg, 3 times / day Route: digestive tract route Route: multiple Dose: 0.227 mg/kg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/	unhealthy, 17.6 month n = 39 Health Status: unhealthy Condition: feeding intolerance or vomiting Age Group: 17.6 month Sex: M+F Population Size: 39 Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/	Other AEs: Sleepiness, Constipation... Other AEs: Sleepiness (4 patients) Constipation (3 patients) Abnormal behaviour NOS (2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/
22.5 mg single, oral Dose: 22.5 mg Route: oral Route: single Dose: 22.5 mg Sources: https://pubmed.ncbi.nlm.nih.gov/2699315/	healthy, 4 n = 1 Health Status: healthy Age Group: 4 Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/2699315/	Other AEs: Disorientation, Abnormal behaviour... Other AEs: Disorientation Abnormal behaviour Sources: https://pubmed.ncbi.nlm.nih.gov/2699315/
6 mg multiple, digestive tract route (median) Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 n = 80 Health Status: unhealthy Condition: refractory upper gastrointestinal symptoms Age Group: 9.8 Sex: M+F Population Size: 80 Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	Other AEs: Somnolence, Irritability... Other AEs: Somnolence (16%) Irritability (6%) Increased appetite (5%) Abdominal pain (2.5%) Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/
32 mg multiple, oral Recommended Dose: 32 mg Route: oral Route: multiple Dose: 32 mg Sources: https://pubmed.ncbi.nlm.nih.gov/638709/	unhealthy, <40 n = 20 Health Status: unhealthy Condition: endocrine disorders Age Group: <40 Population Size: 20 Sources: https://pubmed.ncbi.nlm.nih.gov/638709/	Other AEs: Weight gain, Drowsiness... Other AEs: Weight gain (19 patients) Drowsiness Sources: https://pubmed.ncbi.nlm.nih.gov/638709/

AEs

AE	Significance	Dose	Population
Abnormal behaviour NOS	2 patients	0.227 mg/kg 3 times / day multiple, digestive tract route (median) Recommended Dose: 0.227 mg/kg, 3 times / day Route: digestive tract route Route: multiple Dose: 0.227 mg/kg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/	unhealthy, 17.6 month n = 39 Health Status: unhealthy Condition: feeding intolerance or vomiting Age Group: 17.6 month Sex: M+F Population Size: 39 Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/
Constipation	3 patients	0.227 mg/kg 3 times / day multiple, digestive tract route (median) Recommended Dose: 0.227 mg/kg, 3 times / day Route: digestive tract route Route: multiple Dose: 0.227 mg/kg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/	unhealthy, 17.6 month n = 39 Health Status: unhealthy Condition: feeding intolerance or vomiting Age Group: 17.6 month Sex: M+F Population Size: 39 Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/
Sleepiness	4 patients	0.227 mg/kg 3 times / day multiple, digestive tract route (median) Recommended Dose: 0.227 mg/kg, 3 times / day Route: digestive tract route Route: multiple Dose: 0.227 mg/kg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/	unhealthy, 17.6 month n = 39 Health Status: unhealthy Condition: feeding intolerance or vomiting Age Group: 17.6 month Sex: M+F Population Size: 39 Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/
Abnormal behaviour		22.5 mg single, oral Dose: 22.5 mg Route: oral Route: single Dose: 22.5 mg Sources: https://pubmed.ncbi.nlm.nih.gov/2699315/	healthy, 4 n = 1 Health Status: healthy Age Group: 4 Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/2699315/
Disorientation		22.5 mg single, oral Dose: 22.5 mg Route: oral Route: single Dose: 22.5 mg Sources: https://pubmed.ncbi.nlm.nih.gov/2699315/	healthy, 4 n = 1 Health Status: healthy Age Group: 4 Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/2699315/
Somnolence	16%	6 mg multiple, digestive tract route (median) Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 n = 80 Health Status: unhealthy Condition: refractory upper gastrointestinal symptoms Age Group: 9.8 Sex: M+F Population Size: 80 Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/
Abdominal pain	2.5%	6 mg multiple, digestive tract route (median) Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 n = 80 Health Status: unhealthy Condition: refractory upper gastrointestinal symptoms Age Group: 9.8 Sex: M+F Population Size: 80 Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/
Increased appetite	5%	6 mg multiple, digestive tract route (median) Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 n = 80 Health Status: unhealthy Condition: refractory upper gastrointestinal symptoms Age Group: 9.8 Sex: M+F Population Size: 80 Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/
Irritability	6%	6 mg multiple, digestive tract route (median) Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 n = 80 Health Status: unhealthy Condition: refractory upper gastrointestinal symptoms Age Group: 9.8 Sex: M+F Population Size: 80 Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/
Drowsiness		32 mg multiple, oral Recommended Dose: 32 mg Route: oral Route: multiple Dose: 32 mg Sources: https://pubmed.ncbi.nlm.nih.gov/638709/	unhealthy, <40 n = 20 Health Status: unhealthy Condition: endocrine disorders Age Group: <40 Population Size: 20 Sources: https://pubmed.ncbi.nlm.nih.gov/638709/
Weight gain	19 patients	32 mg multiple, oral Recommended Dose: 32 mg Route: oral Route: multiple Dose: 32 mg Sources: https://pubmed.ncbi.nlm.nih.gov/638709/	unhealthy, <40 n = 20 Health Status: unhealthy Condition: endocrine disorders Age Group: <40 Population Size: 20 Sources: https://pubmed.ncbi.nlm.nih.gov/638709/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
			inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 512 K+ channels 70 L-type Ca2+ channels 28	UGT1A3 422 UGT1A4 347 CYP1A2 1054

Drug as perpetrator

Target	Modality	Activity
K+ channels 70	inhibitor 3277 Sources: https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0041303 Page: 1.0	yes
L-type Ca2+ channels 30	inhibitor 3277 Sources: https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0041303 Page: 1.0	yes
OCT1 543	inhibitor 3277 Sources: https://www.tandfonline.com/doi/abs/10.1080/00498254.2016.1241449 Page: 5.0	yes

Drug as victim

Target	Modality	Activity
CYP1A2 1054	substrate 3367 Sources: https://link.springer.com/article/10.1007%2Fs002800100285 Page: 543.0	likely
UGT1A3 422	substrate 3367 Sources: https://link.springer.com/article/10.1007%2Fs002800100285 Page: 543.0	yes
UGT1A4 347	substrate 3367 Sources: https://link.springer.com/article/10.1007%2Fs002800100285 Page: 543.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.jstage.jst.go.jp/article/jphs/advpub/0/advpub_13159FP/_article/-char/ja/ Page: 6.0

Sourcing

Vendor/Aggregator	ID	URL
3B Scientific (Wuhan) Corp	3B1-00277	http://www.3bsc.com/index/pro_info.php?id=20489
AA Blocks	AA005SE1	https://www.aablocks.com/goods/Goods/detail?id=AA005SE1
AHH Chemical co.,ltd	API-1807	http://www.ahhchemical.com/product/API-1807.html
AK Scientific, Inc. (AKSCI)	J10393	http://www.aksci.com/item_detail.php?cat=J10393
AK Scientific, Inc. (AKSCI)	M230	http://www.aksci.com/item_detail.php?cat=M230
Aaron Chemicals	AR005T5T	http://www.aaronchem.com/969-33-5
Achemtek	0104-016666	http://www.achemtek.com/41354-29-4
Acorn PharmaTech	ACN-052222	http://www.acornpharmatech.com/
Adooq BioScience	A11709	https://www.adooq.com/cyproheptadine-hydrochloride.html
Ambeed	A359851	https://www.ambeed.com/products/969-33-5.html
Angel Pharmatech	AG301658	http://www.angelpharmatech.com/969-33-5.html
ApexBio Technology	B3309	http://www.apexbt.com/cyproheptadine-hydrochloride.html
Ark Pharm	AK544118	http://www.arkpharminc.com/products/969-33-5.html
Aurora Fine Chemicals LLC	A13.140.591	http://online.aurorafinechemicals.com/info?ID=A13.140.591
AvaChem Scientific	3763	http://www.avachem.com/productSearch.asp?3763
Avantor Inc	700008-706	https://us.vwr.com/store/product/21572758/cyproheptadine-hydrochloride-98-5-usp
BLD Pharm	BD627798	http://www.bldpharm.com/products/969-33-5.html
BOC Sciences	129-03-3	https://www.bocsci.com/cyproheptadine-cas-129-03-3-item-56810.html
BioChemPartner	BCP34399	http://www.biochempartner.com/969-33-5-BCP34399
BioCrick	BCC5161	http://www.biocrick.com/Cyproheptadine-hydrochloride-BCC5161.html
BioSynth	W-106308	https://www.biosynth.com/en/products/life-science/other-biochemicals/products/W-106308.html
CSNpharm	CSN17333	https://www.csnpharm.com/products/cycloheptadine-hydrochloride.html
Chem Scene	CS-2423	http://www.chemscene.com/969-33-5.html
ChemMol	30104911	http://www.chemmol.com/chemmol/30104911.html
ChemMol	49429217	http://www.chemmol.com/chemmol/49429217.html
Chemspace	CSSB00016997370	https://chem-space.com/CSSB00016997370
Clearsynth	CS-O-15509	https://www.clearsynth.com/en/CSO15509.html
Combi-Blocks	QA-9006	http://www.combi-blocks.com/cgi-bin/find.cgi?QA-9006
Finetech	FT-0603147	http://www.finetechnology-ind.com/prod/detail/pub/41354-29-4.html
Glentham Life Sciences	GP6863	http://www.glentham.com/products/product/GP6863/
Hairui	HR135310	http://www.hairuichem.com/en/product/41354-29-4.html
Hairui	HR138051	http://www.hairuichem.com/en/product/969-33-5.html
Hello Bio	HB1657	https://www.hellobio.com/cyproheptadine-hydrochloride.html
LGC Standards	DRE-C11912000	https://www.lgcstandards.com/US/en/p/DRE-C11912000
Lab Network	LN00855395	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00855395
MedChem Express	HY-B0366A	https://www.medchemexpress.com/Cyproheptadine-hydrochloride.html
MolPort	MolPort-003-940-781	https://www.molport.com/shop/molecule-link/MolPort-003-940-781
Molcore	MC553857	https://www.molcore.com/product/41354-29-4
Molcore	MC583159	https://www.molcore.com/product/969-33-5
MuseChem	A000399	https://www.musechem.com/product/A000399.html
Selleck Chemicals	S2044	http://www.selleckchem.com/products/cyproheptadine-hydrochloride-periactin.html
TCI (Tokyo Chemical Industry)	C3218	http://www.tcichemicals.com/eshop/en/us/commodity/C3218/index.html
Tocris	996	https://www.tocris.com/products/cyproheptadine-hydrochloride_0996
abcr GmbH	AB497226	http://www.abcr.de/shop/en/AB497226
eNovation Chemicals	D332047	https://www.enovationchem.com/ProductDetails.asp?ProductID=D332047

PubMed

Title	Date	PubMed
Cyproheptadine use in hepatocellular carcinoma.	2017	28401014
Polypharmacological in Silico Bioactivity Profiling and Experimental Validation Uncovers Sedative-Hypnotic Effects of Approved and Experimental Drugs in Rat.	2017 Jun 16	28414209
Cyproheptadine: A Potentially Effective Treatment for Functional Gastrointestinal Disorders in Children.	2017 Mar 1	28287686
Survey on treatments for primary headaches in 13 specialized juvenile Headache Centers: The first multicenter Italian study.	2017 May	28082014
Reconsideration of the diagnosis and treatment of childhood migraine: A practical review of clinical experiences.	2017 May	27993427
A short history of the 5-HT(2C) receptor: from the choroid plexus to depression, obesity and addiction treatment.	2017 May	28265714

Patents

Sample Use Guides

In Vivo Use Guide

4 mg PO q8hr initially; maintenance: 4-20 mg/day, up to 32 mg/day divided q8hr in some patients; not to exceed 0.5 mg/kg/day

Route of Administration: Oral

In Vitro Use Guide

Cytotoxic effect of Cyproheptadine (Glutodine) on urothelial cancer cells was determined in SV-HUC1, TSGH 8301, BFTC 905, BFTC 909, J82, 5637 cell lined. Cells were treated with 25-- 150 mkM of Cyproheptadine for 24 h. Apoptosis analysis was performed using the Annexin V-FITC Apoptosis Detection Kit. Treatment with high dose Cyproheptadine (≥100 mkM) for 24 h induced significant cytotoxicity toward all bladder cancer cells, 50 mkM of Cyproheptadine only induced cytotoxicity in cancer cell lines but not in the immortalized normal urothelial SV-HUC1 cells

Name

Type

Language

CYPROHEPTADINE OROTATE

Common Name

English

OROTIC ACID, COMPD. WITH 4-(5H-DIBENZO(A,D)CYCLOHEPTEN-5-YLIDENE)-1-METHYLPIPERIDINE (1:1)

Systematic Name

English

4-(5H-DIBENZO(A,D)CYCLOHEPTEN-5-YLIDENE)-1-METHYLPIPERIDINE OROTATE

Systematic Name

English

4-PYRIMIDINECARBOXYLIC ACID, 1,2,3,6-TETRAHYDRO-2,6-DIOXO-, COMPD. WITH 4-(5H-DIBENZO(A,D)CYCLOHEPTEN-5-YLIDENE)-1-METHYLPIPERIDINE (1:1)

Systematic Name

English

CYPROHEPTADINE OROTIC ACID

Common Name

English

Cyproheptadine orotate [WHO-DD]

Common Name

English

Code System Code Type Description

PUBCHEM

163203617

Created by admin on Sat Dec 16 18:18:36 GMT 2023 , Edited by admin on Sat Dec 16 18:18:36 GMT 2023

PRIMARY

CAS

34334-52-6

Created by admin on Sat Dec 16 18:18:36 GMT 2023 , Edited by admin on Sat Dec 16 18:18:36 GMT 2023

PRIMARY

FDA UNII

NK346734MK

Created by admin on Sat Dec 16 18:18:36 GMT 2023 , Edited by admin on Sat Dec 16 18:18:36 GMT 2023

PRIMARY

SMS_ID

300000001582

Created by admin on Sat Dec 16 18:18:36 GMT 2023 , Edited by admin on Sat Dec 16 18:18:36 GMT 2023

PRIMARY

PARENT (SALT/SOLVATE)


					2YHB6175DO

CYPROHEPTADINE

SUBSTANCE RECORD


					NK346734MK

CYPROHEPTADINE OROTATE

Details

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OverviewOther

Drug as perpetrator​

Drug as victim

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Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2

Drug as perpetrator