CYPROHEPTADINE HYDROCHLORIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	2C21H21N.2ClH.3H2O
Molecular Weight	701.764
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of CYPROHEPTADINE HYDROCHLORIDE

Structure Search

SMILES

O.O.O.Cl.Cl.CN1CCC(CC1)=C2C3=CC=CC=C3C=CC4=CC=CC=C24.CN5CCC(CC5)=C6C7=CC=CC=C7C=CC8=CC=CC=C68

InChI

InChIKey=ZEAUHIZSRUAMQG-UHFFFAOYSA-N

InChI=1S/2C21H21N.2ClH.3H2O/c2*1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21;;;;;/h2*2-11H,12-15H2,1H3;2*1H;3*1H2

HIDE SMILES / InChI

Molecular Formula	H2O
Molecular Weight	18.0153
Charge	0
Count

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

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

Molecular Formula	ClH
Molecular Weight	36.461
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 316 Target ID: CHEMBL3943 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6261070	Antagonist 2849	2.7 nM [Ki]
Serotonin 2 (5-HT2) receptor 90 Target ID: CHEMBL2093870 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6261070	Antagonist 2849	6.5 nM [Ki]
Serotonin 2a (5-HT2a) receptor 237 Target ID: CHEMBL322 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9178521 \| https://www.ncbi.nlm.nih.gov/pubmed/12498911	Antagonist 2849	8.8 null [pKi]
Muscarinic acetylcholine receptor 162 Target ID: CHEMBL1907609 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6261070	Antagonist 2849	19.0 nM [Ki]
Histamine H1 receptor 316 Target ID: CHEMBL3943 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7650688	Antagonist 2849	0.537 nM [Ki]
Serotonin 2a (5-HT2a) receptor 237 Target ID: CHEMBL322 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11229772	Antagonist 2849	1.6 nM [Ki]
Serotonin 2c (5-HT2c) receptor 131 Target ID: CHEMBL3006 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11266163	Antagonist 2849	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 8583	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 8583	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 8583	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 101 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8583	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 8583	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 8583	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 47 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/087056s045lbl.pdf	Primary	Approved 8583	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 8583	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 8583	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 8583	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
30 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15083941/	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:		GLUTODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15083941/	8 mg single, sublingual dose: 8 mg route of administration: Sublingual experiment type: SINGLE co-administered:		GLUTODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.25 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21432861/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: COBAMAMIDE	COBAMAMIDE	GLUTODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
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
209 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15083941/	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:		GLUTODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
25 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15083941/	8 mg single, sublingual dose: 8 mg route of administration: Sublingual experiment type: SINGLE co-administered:		GLUTODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
40.82 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21432861/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: COBAMAMIDE	COBAMAMIDE	GLUTODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
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://pubmed.ncbi.nlm.nih.gov/21432861/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered: COBAMAMIDE	COBAMAMIDE	GLUTODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
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 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 Health Status: unhealthy Age Group: 17.6 month Sex: M+F 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 Health Status: healthy Age Group: 4 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 Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 Health Status: unhealthy Age Group: 9.8 Sex: M+F 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 Health Status: unhealthy Age Group: <40 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 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 Health Status: unhealthy Age Group: 17.6 month Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/
Constipation	3 patients	0.227 mg/kg 3 times / day multiple, digestive tract route 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 Health Status: unhealthy Age Group: 17.6 month Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/27194450/
Sleepiness	4 patients	0.227 mg/kg 3 times / day multiple, digestive tract route 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 Health Status: unhealthy Age Group: 17.6 month Sex: M+F 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 Health Status: healthy Age Group: 4 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 Health Status: healthy Age Group: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/2699315/
Somnolence	16%	6 mg multiple, digestive tract route Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 Health Status: unhealthy Age Group: 9.8 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/
Abdominal pain	2.5%	6 mg multiple, digestive tract route Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 Health Status: unhealthy Age Group: 9.8 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/
Increased appetite	5%	6 mg multiple, digestive tract route Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 Health Status: unhealthy Age Group: 9.8 Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/
Irritability	6%	6 mg multiple, digestive tract route Recommended Dose: 6 mg Route: digestive tract route Route: multiple Dose: 6 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23419589/	unhealthy, 9.8 Health Status: unhealthy Age Group: 9.8 Sex: M+F 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 Health Status: unhealthy Age Group: <40 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 Health Status: unhealthy Age Group: <40 Sources: https://pubmed.ncbi.nlm.nih.gov/638709/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
			inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 620 K+ channels 73 L-type Ca2+ channels 28	UGT1A3 470 UGT1A4 399 CYP1A2 1197

Drug as perpetrator

Target	Modality	Activity
K+ channels 73	inhibitor 4027 Sources: https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0041303 Page: 1.0	yes
L-type Ca2+ channels 30	inhibitor 4027 Sources: https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0041303 Page: 1.0	yes
OCT1 656	inhibitor 4027 Sources: https://www.tandfonline.com/doi/abs/10.1080/00498254.2016.1241449 Page: 5.0	yes

Drug as victim

Target	Modality	Activity
CYP1A2 1197	substrate 4014 Sources: https://link.springer.com/article/10.1007%2Fs002800100285 Page: 543.0	likely
UGT1A3 470	substrate 4014 Sources: https://link.springer.com/article/10.1007%2Fs002800100285 Page: 543.0	yes
UGT1A4 399	substrate 4014 Sources: https://link.springer.com/article/10.1007%2Fs002800100285 Page: 543.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 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
Aaron Chemicals	AR005T5T	http://www.aaronchem.com/969-33-5
abcr GmbH	AB497226	http://www.abcr.de/shop/en/AB497226
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
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
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
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
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
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
CSNpharm	CSN17333	https://www.csnpharm.com/products/cycloheptadine-hydrochloride.html
eNovation Chemicals	D332047	https://www.enovationchem.com/ProductDetails.asp?ProductID=D332047
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
Lab Network	LN00855395	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00855395
LGC Standards	DRE-C11912000	https://www.lgcstandards.com/US/en/p/DRE-C11912000
MedChem Express	HY-B0366A	https://www.medchemexpress.com/Cyproheptadine-hydrochloride.html
Molcore	MC553857	https://www.molcore.com/product/41354-29-4
Molcore	MC583159	https://www.molcore.com/product/969-33-5
MolPort	MolPort-003-940-781	https://www.molport.com/shop/molecule-link/MolPort-003-940-781
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

PubMed

Title	Date	PubMed
Polypharmacological in Silico Bioactivity Profiling and Experimental Validation Uncovers Sedative-Hypnotic Effects of Approved and Experimental Drugs in Rat.	2017-06-16	28414209
A short history of the 5-HT2C receptor: from the choroid plexus to depression, obesity and addiction treatment.	2017-05	28265714
Survey on treatments for primary headaches in 13 specialized juvenile Headache Centers: The first multicenter Italian study.	2017-05	28082014
Reconsideration of the diagnosis and treatment of childhood migraine: A practical review of clinical experiences.	2017-05	27993427
Cyproheptadine: A Potentially Effective Treatment for Functional Gastrointestinal Disorders in Children.	2017-03-01	28287686
Cyproheptadine use in hepatocellular carcinoma.	2017	28401014

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 `Mon Mar 31 17:51:16 GMT 2025` Edited by `admin` on `Mon Mar 31 17:51:16 GMT 2025`
Record UNII	NJ82J0F8QC
Record Status	`Validated (UNII)`
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Name

Type

Language

CYPROHEPTADINE HYDROCHLORIDE SESQUIHYDRATE

Preferred Name

English

CYPROHEPTADINE HYDROCHLORIDE

Common Name

English

CYPROHEPTADINE HYDROCHLORIDE [VANDF]

Common Name

English

CYPROHEPTADINE HYDROCHLORIDE [USP-RS]

Common Name

English

CYPROHEPTADINE HYDROCHLORIDE [MART.]

Common Name

English

CYPROHEPTADINE HYDROCHLORIDE SESQUIHYDRATE [MI]

Common Name

English

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

Common Name

English

CYPROHEPTADINE HYDROCHLORIDE HYDRATE [JAN]

Common Name

English

PERIACTINE

Brand Name

English

CYPROHEPTADINE HYDROCHLORIDE HYDRATE

Common Name

English

CYPROHEPTADINE HCL

Common Name

English

CYPROHEPTADINE HYDROCHLORIDE [ORANGE BOOK]

Common Name

English

PERITOL

Brand Name

English

PERIACTIN

Brand Name

English

NSC-759282

Code

English

CYPROHEPTADINE HYDROCHLORIDE [USP MONOGRAPH]

Common Name

English

4-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-1-methylpiperidine hydrochloride sesquihydrate

Common Name

English

PIPERIDINE, 4-(5H-DIBENZO(A,D)CYCLOHEPTEN-5-YLIDENE)-1-METHYL-, HYDROCHLORIDE, HYDRATE (2:2:3)

Common Name

English

CYPROHEPTADINE HYDROCHLORIDE [EP IMPURITY]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29578