CAS 129-03-3|Cyproheptadine

Introduction：Basic information about CAS 129-03-3|Cyproheptadine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Cyproheptadine BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Customs
7. Synonyms

Common Name	Cyproheptadine
CAS Number	129-03-3	Molecular Weight	323.85900
Density	1.115g/cm3	Boiling Point	440.1ºC at 760mmHg
Molecular Formula	C₂₁H₂₂ClN	Melting Point	298 °C (dec.)(lit.)
MSDS	/	Flash Point	194.5ºC

Names

Name	cyproheptadine
Synonym	More Synonyms

Cyproheptadine BiologicalActivity

Description	Cyproheptadine is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders[1][2].
Related Catalog	Signaling Pathways >>Apoptosis >>ApoptosisResearch Areas >>Cardiovascular DiseaseResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor
In Vitro	Cyproheptadine (0.01-100 nM; 1 minute) dose-dependently inhibits serotonin-enhanced ADP-induced mouse platelet aggregation in vitro[2]. Cyproheptadine (10 nM) has the ability to inhibit 15 µM serotonin-enhanced ADP-induced (1 µM) tyrosine phosphorylation in platelets in vitro[2]. Cyproheptadine inhibits human platelet PS exposure (Annexin V), P-selectin, and GPIIb-IIIa (PAC-1 binding) activation in vitro[2].
In Vivo	Cyproheptadine (1 mg/kg; i.p.; daily, for 5 days; C57BL/6 mice) exerts thromboprotective properties in vivo[2]. Animal Model: C57BL/6 mice (8-10 weeks old)[2] Dosage: 1 mg/kg Administration: Intraperitoneal injection; daily, for 5 days Result: Prolonged occlusion times and tail bleeding times in mice.
References	[1]. Calka O, et, al. Effect of cyproheptadine on serum leptin levels. Adv Ther, 2005. 22(5): p. 424-8. [2]. Olivia A Lin, et al. The Antidepressant 5-HT2A Receptor Antagonists Pizotifen and Cyproheptadine Inhibit Serotonin-Enhanced Platelet Function. PLoS One. 2014; 9(1): e87026.

Chemical & Physical Properties

Density	1.115g/cm3
Boiling Point	440.1ºC at 760mmHg
Melting Point	298 °C (dec.)(lit.)
Molecular Formula	C₂₁H₂₂ClN
Molecular Weight	323.85900
Flash Point	194.5ºC
Exact Mass	323.14400
PSA	3.24000
LogP	5.43780
Vapour Pressure	6.03E-08mmHg at 25°C
Index of Refraction	1.5339 (20ºC)
InChIKey	JJCFRYNCJDLXIK-UHFFFAOYSA-N
SMILES	CN1CCC(=C2c3ccccc3C=Cc3ccccc32)CC1

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM7000000

CHEMICAL NAME :: Piperidine, 4-(5H-dibenzo(a,d)cyclohepten-5-ylidene)-1-methyl-

CAS REGISTRY NUMBER :: 129-03-3

BEILSTEIN REFERENCE NO. :: 1685976

LAST UPDATED :: 199706

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C21-H21-N

MOLECULAR WEIGHT :: 287.43

WISWESSER LINE NOTATION :: L C676 BYJ BU- DT6N DYTJ A1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 295 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,69,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 52 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,69,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 106 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,1723,1975

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 43300 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,1723,1975

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 107 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,69,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 15 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,1723,1975

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 50 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZIAQ "Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973 Volume(issue)/page/year: -,82,1973

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 3500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,69,1972 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 10 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 257,168,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 20 mg/kg

SEX/DURATION :: female 13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 257,168,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 20 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 257,168,1982

Safety Information

Packaging Group	I; II; III
HS Code	29143900

Customs

HS Code	2933399090
Summary	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Synonyms

cyproheptadiene

EINECS 204-928-9

Dronactin

Periactine

Periactinol

MFCD00242817

Eiproheptadine

Cyproheptadine

1-methyl-4-(5-dibenzo[a,e]cycloheptatrienylidene)piperidine

MK 141

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine

Periactin

Cypoheptadine

4-dibenzo[a,d]cyclohepten-5-ylidene-1-methyl-piperidine

Periactin(R)

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