Triprolidine hydrochloride

Names

[ CAS No. ]:
550-70-9

[ Name ]:
Triprolidine hydrochloride

[Synonym ]:
EINECS 208-985-0
MFCD00039044
Triprolidine Hydrochloride
Triprolidine HCl

Biological Activity

[Description]:

Triprolidine is an oral active, first-generation histamine H1-receptor antagonist. Triprolidine can be used for the research of allergic rhinitis. triprolidine exhibits spinal motor and sensory block in rats[1][2][3].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

H1 Receptor

[In Vivo]

Triprolidine (292.81-1467.20 μg/kg; intrathecal injection) produces a dose-dependent effect of spinal motor and sensory block in rats[3]. Animal Model: Male Sprague-Dawley rat (300-350 g)[3] Dosage: 292.81 μg/kg, 488.02 μg/kg, 733.60μg/kg, 1098.83 μg/kg, 1467.20 μg/kg Administration: Intrathecal injection Result: Elicited a dose-dependent spinal block.

[References]

[1]. K J Simons, et al. An investigation of the H1-receptor antagonist triprolidine: pharmacokinetics and antihistaminic effects. J Allergy Clin Immunol. 1986 Feb;77(2):326-30.

[2]. D L Deal, et al. Disposition and metabolism of triprolidine in mice. Drug Metab Dispos. Nov-Dec 1992;20(6):920-7.

[3]. Jann-Inn Tzeng, et al. Spinal sensory and motor blockade by intrathecal doxylamine and triprolidine in rats. J Pharm Pharmacol. 2018 Dec;70(12):1654-1661.

Chemical & Physical Properties

[ Density]:
1.061g/cm3

[ Boiling Point ]:
435.4ºC at 760mmHg

[ Melting Point ]:
59-61ºC

[ Molecular Formula ]:
C₁₉H₂₃ClN₂

[ Molecular Weight ]:
314.85200

[ Flash Point ]:
217.1ºC

[ Exact Mass ]:
314.15500

[ PSA ]:
16.13000

[ LogP ]:
4.65740

[ Storage condition ]:
2-8°C

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UT7657000

CHEMICAL NAME :: Pyridine, 2-(3-(1-pyrrolidinyl)-1-p-tolylpropenyl)-, monohydrochloride, (E)-

CAS REGISTRY NUMBER :: 550-70-9

LAST UPDATED :: 199803

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C19-H22-N2.Cl-H

MOLECULAR WEIGHT :: 314.89

WISWESSER LINE NOTATION :: T6NJ BYR D1&2- AT5NTJ &GH

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 :: 840 mg/kg

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

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 22,375,1980

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 495 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,525,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 247 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,525,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 21 mg/kg

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

REFERENCE :: BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 8,171,1953

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 8,171,1953 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 81570 No. of Facilities: 842 (estimated) No. of Industries: 2 No. of Occupations: 2 No. of Employees: 990 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 81570 No. of Facilities: 178 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 2378 (estimated) No. of Female Employees: 1467 (estimated)

Safety Information

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22-36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
UN 3249

[ WGK Germany ]:
3

[ RTECS ]:
UT7658000

[ Packaging Group ]:
III

[ Hazard Class ]:
6.1(b)

[ HS Code ]:
2933990090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%