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2192-20-3

2192-20-3 structure
2192-20-3 structure
  • Name: Hydroxyzine dihydrochloride
  • Chemical Name: hydroxyzine hydrochloride
  • CAS Number: 2192-20-3
  • Molecular Formula: C21H29Cl3N2O2
  • Molecular Weight: 447.826
  • Catalog: API Nervous system medication Anxiolytic
  • Create Date: 2018-08-24 13:55:48
  • Modify Date: 2024-01-01 22:15:06
  • Hydroxyzine Dihydrochloride is a histamine H1-receptor antagonist.Target: Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE) [2]. Hydroxyzine (500 M) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 g/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen [3].Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats [3]. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats [4].

Name hydroxyzine hydrochloride
Synonyms 2-(2-{4-[(4-Chlorophenyl)(phenyl)methyl]-1-piperazinyl}ethoxy)ethanol dihydrochloride
2-(2-{4-[(4-chlorphenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethanoldihydrochlorid
ethanol, 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-, dihydrochloride
Disron
Hydroxyzine hydrochloride
Hydroxyzin*2HCl
Ethanol, 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-, hydrochloride (1:2)
Arcanax
Hydroxyzine 2HCl
2-(2-{4-[(4-chlorophényl)(phényl)méthyl]pipérazin-1-yl}éthoxy)éthanol dichlorhydrate
2-(2-{4-[(4-Chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethanol dihydrochloride
EINECS 218-586-3
UNII:76755771U3
Hydroxyzine dihydrochloride
MFCD00058200
Vistaject
Vistarex
Quiess
Neurolax
Alamon
2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethanol,dihydrochloride
Hydroxyzine (dihydrochloride)
Description Hydroxyzine Dihydrochloride is a histamine H1-receptor antagonist.Target: Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE) [2]. Hydroxyzine (500 M) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 g/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen [3].Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats [3]. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats [4].
Related Catalog
References

[1]. Minogiannis, P., et al., Hydroxyzine inhibits neurogenic bladder mast cell activation. Int J Immunopharmacol, 1998. 20(10): p. 553-63.

[2]. Dimitriadou, V., X. Pang, and T.C. Theoharides, Hydroxyzine inhibits experimental allergic encephalomyelitis (EAE) and associated brain mast cell activation. Int J Immunopharmacol, 2000. 22(9): p. 673-84.

[3]. Kan, W.M., et al., Effect of hydroxyzine on the transport of etoposide in rat small intestine. Anticancer Drugs, 2001. 12(3): p. 267-73.

[4]. Morichi, R. and G. Pepeu, A study of the influence of hydroxyzine and diazepam on morphine antinociceptoion in the rat. Pain, 1979. 7(2): p. 173-80.

Density 1.182 g/cm3
Boiling Point 499.2ºC at 760 mmHg
Melting Point 190-192°C
Molecular Formula C21H29Cl3N2O2
Molecular Weight 447.826
Flash Point 255.7ºC
Exact Mass 446.129456
PSA 35.94000
LogP 4.53570
Vapour Pressure 8.78E-11mmHg at 25°C
Storage condition Refrigerator
Water Solubility H2O: soluble

CHEMICAL IDENTIFICATION

RTECS NUMBER :
KK2280000
CHEMICAL NAME :
Ethanol, 2-(2-(4-(p-chloro-alpha-phenylbenzyl)-1-piperazinyl)e thoxy)-, dihydrochloride
CAS REGISTRY NUMBER :
2192-20-3
LAST UPDATED :
199709
DATA ITEMS CITED :
11
MOLECULAR FORMULA :
C21-H27-Cl-N2-O2.2Cl-H
MOLECULAR WEIGHT :
447.87

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
500 ug/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
REFERENCE :
HUPSEC Human Psychopharmacology. (John Wiley & Sons Ltd., Baffins Lane, Chichester, W.Sussex PO19 1UD, United Kingdom) V.1- 1986- Volume(issue)/page/year: 7,25,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
357 ug/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex)
REFERENCE :
HUPSEC Human Psychopharmacology. (John Wiley & Sons Ltd., Baffins Lane, Chichester, W.Sussex PO19 1UD, United Kingdom) V.1- 1986- Volume(issue)/page/year: 7,25,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Human - child
DOSE/DURATION :
750 ug/kg
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
APHRER Annals of Pharmacotherpy. (Harvey Whitney Books Co., POB 42696, Cincinnati, OH 45242) V. 26- 1992- Volume(issue)/page/year: 31,327,1997
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
950 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
126 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
45 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
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: 109,127,1957
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
122 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 24,100,1973
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
48900 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 24,100,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 84615 No. of Facilities: 1397 (estimated) No. of Industries: 2 No. of Occupations: 2 No. of Employees: 2782 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 84615 No. of Facilities: 42 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 1296 (estimated) No. of Female Employees: 1246 (estimated)
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H315-H319-H335
Precautionary Statements P301 + P312 + P330-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn:Harmful;
Risk Phrases R22;R36/37/38
Safety Phrases S26
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS KK2280000
HS Code 2933990090

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2192-20-3 structure

2192-20-3

Literature: US2011/172425 A1, ; Page/Page column 8 ;
Precursor  2

DownStream  0

HS Code 2933599090
Summary 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%