Triprolidine hydrochloride

Triprolidine hydrochloride monohydrate is an orally active, cell-permeable and first-generation histamine H1 antagonist[1]. Triprolidine hydrochloride monohydrate is an antihistamine and can be used in allergic rhinitis; asthma; and urticaria[2].

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

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

H1 Receptor

Triprolidine (intraseptal infusion; 0.5 μM in 0.5 μl; 30, 60, and 180 min after tetanus) had no significant effects on the baseline fEPSPs, however, it is followed by a smaller Long-term potentiation (LTP) induced during walking (173% of the baseline at 60 min) compared with saline infusion (208% at 60 min) in rats[2]. Animal Model: Adult male Long–Evans TMN (tuberomammillary nucleus (TMN) neurons) lesion rats[2] Dosage: 0.5 μm in 0.5 μl Administration: Intraseptal infusion; 30, 60, and 180 min after tetanus Result: Attenuated the walking-associated enhancement of LTP.

[1]. Tao Luo, et al. Endogenous Histamine Facilitates Long-Term Potentiation in the Hippocampus During WalkingJ Neurosci. 2010 Jun 9;30(23):7845-52.

[2]. Sang-Chul Shin, et al. Controlled Release of Triprolidine Using Ethylene-Vinyl Acetate Membrane and Matrix Systems. Eur J Pharm Biopharm

MOLECULAR FORMULA :

C19-H22-N2.Cl-H.H2-O

MOLECULAR WEIGHT :

332.91

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 :

NCTR** National Center for Toxicology Research Technical Report. Office of Associate Director for Scientific Coordination, Jefferson, Arkansas 72079 Volume(issue)/page/year: #414/415,1991

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

163 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

NCTR** National Center for Toxicology Research Technical Report. Office of Associate Director for Scientific Coordination, Jefferson, Arkansas 72079 Volume(issue)/page/year: #414/415,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

10760 mg/kg/90D-I

TOXIC EFFECTS :

Cardiac - changes in heart weight Gastrointestinal - changes in structure or function of salivary glands Blood - changes in leukocyte (WBC) count

REFERENCE :

JACTDZ Journal of the American College of Toxicology. (Mary Ann Liebert, Inc., 1651 Third Ave., New York, NY 10128) V.1-12, 1982-1993. Discontinued. Volume(issue)/page/year: 12,359,1993

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

103 gm/kg/2Y-C

TOXIC EFFECTS :

Liver - changes in liver weight Endocrine - changes in spleen weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :

FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 27,223,1995

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

175 gm/kg/2Y-C

TOXIC EFFECTS :

Liver - other changes Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :

NCTR** National Center for Toxicology Research Technical Report. Office of Associate Director for Scientific Coordination, Jefferson, Arkansas 72079 Volume(issue)/page/year: #414/415,1991 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X2762 No. of Facilities: 269 (estimated) No. of Industries: 1 No. of Occupations: 4 No. of Employees: 4419 (estimated) No. of Female Employees: 2546 (estimated)