triprolidine

Modify Date: 2024-01-05 09:28:26

triprolidine Structure
triprolidine structure
Common Name triprolidine
CAS Number 486-12-4 Molecular Weight 278.39100
Density 1.061 g/cm3 Boiling Point 435.4ºC at 760 mmHg
Molecular Formula C19H22N2 Melting Point 126-130°C
MSDS N/A Flash Point 217.1ºC

 Use of triprolidine


Triprolidine is an orally active H1R Antagonist antagonist. Triprolidine has the function of spinal cord motor and sensory block. Triprolidine can be used for the research of allergic rhinitis[1][2][3].

 Names

Name triprolidine
Synonym More Synonyms

 triprolidine Biological Activity

Description Triprolidine is an orally active H1R Antagonist antagonist. Triprolidine has the function of spinal cord motor and sensory block. Triprolidine can be used for the research of allergic rhinitis[1][2][3].
Related Catalog
In Vitro Triprolidine (maturing human dendritic cells) can antagonist histamine H1 and decreases the expression of CD45[1].
In Vivo Triprolidine (292.81-1467.20 μg/kg; i.p.; Male Sprague-Dawley rat) produces a dose-dependent effect of spinal motor and sensory block in rats[2]. Animal Model: Male Sprague-Dawley rat (300-350 g)[2] Dosage: 292.81, 488.02, 733.60, 1098.83 and 1467.20 μg/kg Administration: Intrathecal injection Result: Elicited spinal block in a dose-dependent.
References

[1]. Szeberényi JB, et, al. Inhibition of effects of endogenously synthesized histamine disturbs in vitro human dendritic cell differentiation. Immunol Lett. 2001 Apr 2;76(3):175-82.

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

[3]. Deal DL, Chandrasurin P, Shockcor J, Minick DJ, Findlay JW, McNulty MJ. Disposition and metabolism of triprolidine in mice. Drug Metab Dispos. 1992 Nov-Dec;20(6):920-7.

 Chemical & Physical Properties

Density 1.061 g/cm3
Boiling Point 435.4ºC at 760 mmHg
Melting Point 126-130°C
Molecular Formula C19H22N2
Molecular Weight 278.39100
Flash Point 217.1ºC
Exact Mass 278.17800
PSA 16.13000
LogP 3.85540
Vapour Pressure 6.16E-09mmHg at 25°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UT5812000
CHEMICAL NAME :
Pyridine, 2-(1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl)- , (E)-
CAS REGISTRY NUMBER :
486-12-4
LAST UPDATED :
199801
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C19-H22-N2
MOLECULAR WEIGHT :
278.43

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
143 ug/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - alteration of operant conditioning Behavioral - changes in psychophysiological tests
REFERENCE :
EJCPAS European Journal of Clinical Pharmacology. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.3- 1970- Volume(issue)/page/year: 47,331,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2700 mg/kg/90D-C
TOXIC EFFECTS :
Gastrointestinal - changes in structure or function of salivary glands Liver - fatty liver degeneration
REFERENCE :
TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 5,96,1985

 Safety Information

Safety Phrases S36/37

 Synthetic Route

~82%

triprolidine Structure

triprolidine

CAS#:486-12-4

Literature: HIKAL LIMITED Patent: WO2009/84035 A1, 2009 ; Location in patent: Page/Page column 5; 9-10 ;

 Precursor & DownStream

Precursor  1

DownStream  1

 Synonyms

MFCD00038040
(e)-pyridin
Triprolidin
(E)-2-[3-(1-Pyrrolidinyl)-1-p-toluenepropenyl]pyridine
(E)-1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidino prop-1-ene
trans-2-[3-(1-Pyrrolidinyl)-1-p-tolypropenyl]pyridine
trans-1-(2-Pyridyl)-3-pyrrolidino-1-p-tolylprop-1-ene
trans-2-[3-(1-pyrrolidinyl)-1-p-tolylpropenyl]pyridine
EINECS 207-627-0
Triprolidine
Tripyrolidine
1t-[2]Pyridyl-3-pyrrolidino-1c-p-tolyl-propen
(E)-1-(2-pyridyl)-3-pyrrolidin-1-yl-1-p-tolylpropene
1t-[2]pyridyl-3-pyrrolidino-1c-p-tolyl-propene
(E)-2-[1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]pyridine