CAS 486-12-4|triprolidine

Introduction:Basic information about CAS 486-12-4|triprolidine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common Nametriprolidine
CAS Number486-12-4Molecular Weight278.39100
Density1.061 g/cm3Boiling Point435.4ºC at 760 mmHg
Molecular FormulaC19H22N2Melting Point126-130°C
MSDS/Flash Point217.1ºC

Names

Nametriprolidine
SynonymMore Synonyms

triprolidine BiologicalActivity

DescriptionTriprolidine 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 CatalogSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>InfectionSignaling Pathways >>GPCR/G Protein >>Histamine Receptor
In VitroTriprolidine (maturing human dendritic cells) can antagonist histamine H1 and decreases the expression of CD45[1].
In VivoTriprolidine (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

Density1.061 g/cm3
Boiling Point435.4ºC at 760 mmHg
Melting Point126-130°C
Molecular FormulaC19H22N2
Molecular Weight278.39100
Flash Point217.1ºC
Exact Mass278.17800
PSA16.13000
LogP3.85540
Vapour Pressure6.16E-09mmHg at 25°C
InChIKeyCBEQULMOCCWAQT-WOJGMQOQSA-N
SMILESCc1ccc(C(=CCN2CCCC2)c2ccccn2)cc1

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 PhrasesS36/37

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
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