CYPROHEPTADINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C21H21N
Molecular Weight	287.3981
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1CCC(CC1)=C2C3=C(C=CC=C3)C=CC4=C2C=CC=C4

InChI

InChIKey=JJCFRYNCJDLXIK-UHFFFAOYSA-N

InChI=1S/C21H21N/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/h2-11H,12-15H2,1H3

HIDE SMILES / InChI

Molecular Formula	C21H21N
Molecular Weight	287.3981
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdfhttps://www.drugs.com/dosage/cyproheptadine.html
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/7650688 | http://www.empr.com/cyproheptadine/drug/23/ | http://reference.medscape.com/drug/cyproheptadine-343389

Glutodine (Cyproheptadine), sold under the brand name Periactin or Peritol, is a first-generation antihistamine with additional antiserotonergic, anticholinergic and local anesthetic properties. Glutodine is a white to slightly yellowish crystalline solid, which is soluble in water, freely soluble in methanol, sparingly soluble in ethanol, soluble in chloroform, and practically insoluble in ether. Cyproheptadine is used to treat allergic reactions (specifically hay fever), Vasomotor rhinitis, Allergic conjunctivitis due to inhalant allergens and foods, uncomplicated allergic skin manifestations of urticaria and angioedema amelioration of allergic reactions to blood or plasma, Cold urticaria, and Dermatographism. Cyproheptadine is used off-label to treat Spasticity Associated With Spinal Cord, Migraine Headache Prophylaxis, Decreased Appetite Secondary to Chronic Disease, Drug-Induced Sexual Dysfunction, Serotonin Syndrome.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Histamine H1 receptor 313 Target ID: CHEMBL3943 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6261070	Antagonist 2760	2.7 nM [Ki]
Serotonin 2 (5-HT2) receptor 87 Target ID: CHEMBL2093870 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6261070	Antagonist 2760	6.5 nM [Ki]
Serotonin 2a (5-HT2a) receptor 230 Target ID: CHEMBL322 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9178521 \| https://www.ncbi.nlm.nih.gov/pubmed/12498911	Antagonist 2760	8.8 null [pKi]
Muscarinic acetylcholine receptor 160 Target ID: CHEMBL1907609 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6261070	Antagonist 2760	19.0 nM [Ki]
Histamine H1 receptor 313 Target ID: CHEMBL3943 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7650688	Antagonist 2760	0.537 nM [Ki]
Serotonin 2a (5-HT2a) receptor 230 Target ID: CHEMBL322 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11229772	Antagonist 2760	1.6 nM [Ki]
Serotonin 2c (5-HT2c) receptor 122 Target ID: CHEMBL3006 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11266163	Antagonist 2760	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 8360	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 3.16224012E11
Perennial allergic rhinitis 47 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8360	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 3.16224012E11
Seasonal allergic rhinitis 63 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8360	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 3.16224012E11
Allergic conjunctivitis 97 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8360	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 3.16224012E11
Urticaria 39 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8360	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 3.16224012E11
Angioedema 20 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8360	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 3.16224012E11
Anaphylaxis 46 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8360	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 3.16224012E11
Cold urticaria 10 Sources: https://www.drugs.com/pro/cyproheptadine.html	Primary	Approved 8360	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 -2.59113599E11
Vasomotor rhinitis 21 Sources: https://www.drugs.com/pro/cyproheptadine.html	Primary	Approved 8360	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 -2.59113599E11
Uncomplicated allergic skin manifestations of angioedema 10 Sources: https://www.drugs.com/pro/cyproheptadine.html	Primary	Approved 8360	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 -2.59113599E11

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 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 506 K+ channels 56 L-type Ca2+ channels 26	UGT1A3 422 UGT1A4 347 CYP1A2 1032

Drug as perpetrator

Target	Modality	Activity
K+ channels 56	inhibitor 3240 Sources: https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0041303 Page: 1.0	yes
L-type Ca2+ channels 28	inhibitor 3240 Sources: https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0041303 Page: 1.0	yes
OCT1 523	inhibitor 3240 Sources: https://www.tandfonline.com/doi/abs/10.1080/00498254.2016.1241449 Page: 5.0	yes

Drug as victim

Target	Modality	Activity
CYP1A2 1032	substrate 3326 Sources: https://link.springer.com/article/10.1007%2Fs002800100285 Page: 543.0	likely
UGT1A3 422	substrate 3326 Sources: https://link.springer.com/article/10.1007%2Fs002800100285 Page: 543.0	yes
UGT1A4 347	substrate 3326 Sources: https://link.springer.com/article/10.1007%2Fs002800100285 Page: 543.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 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
A short history of the 5-HT(2C) receptor: from the choroid plexus to depression, obesity and addiction treatment.	2017 May	28265714
Reconsideration of the diagnosis and treatment of childhood migraine: A practical review of clinical experiences.	2017 May	27993427

Patents

Sample Use Guides

In Vivo Use Guide

The total daily dose for adults should not exceed 0.5 mg/kg/day. The therapeutic range is 4 to 20 mg a day, with the majority of patients requiring 12 to 16 mg a day. An occasional patient may require as much as 32 mg a day for adequate relief. It is suggested that dosage be initiated with 4 mg (1 tablet) three times a day and adjusted according to the size and response of the patient.

Route of Administration: Oral

In Vitro Use Guide

The IC50 of cyproheptadine, determined as the concentration of the drug that inhibited cell growth by 50% after 24 h of treatment, was found to be 44.4, 44.7, and 118.1 uM in HepG2 cells, Huh-7 cells, and normal human hepatocytes, respectively.

Substance Class	Chemical Created by `admin` on `Thu Jul 06 22:14:09 UTC 2023` Edited by `admin` on `Thu Jul 06 22:14:09 UTC 2023`
Record UNII	2YHB6175DO
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CYPROHEPTADINE

Official Name

English

CYPROHEPTADINE [MI]

Common Name

English

CIPROVIT

Brand Name

English

CYPROHEPTADINE [VANDF]

Common Name

English

CYPROHEPTADINE [HSDB]

Common Name

English

Cyproheptadine [WHO-DD]

Common Name

English

PIPERIDINE, 4-(5H-DIBENZO(A,D)CYCLOHEPTEN-5-YLIDENE)-1-METHYL-

Systematic Name

English

cyproheptadine [INN]

Common Name

English

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

Systematic Name

English

Classification Tree Code System Code

WHO-ATC

R06AX02