Hydroxyzine

Modify Date: 2026-07-01 13:33:55

Hydroxyzine Structure
Hydroxyzine structure
 Common Name Hydroxyzine
CAS Number 68-88-2 Molecular Weight 374.90400
Density N/A Boiling Point 220 (0.5 torr)
Molecular Formula C21H27ClN2O2 Melting Point 190°C
MSDS N/A Flash Point N/A

 Use of Hydroxyzine


Hydroxyzine 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].

 Names

This table lists Chinese names, IUPAC names and various aliases of this chemical substance.

Name hydroxyzine
Synonym More Synonyms

 Hydroxyzine Biological Activity

This table contains bioactivity, target information and biological‑assay experimental data of this compound.

Description Hydroxyzine 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.

 Chemical & Physical Properties

This table shows physicochemical parameters including melting point, boiling point, density, solubility and optical rotation. Missing data is marked as N/A.

Boiling Point 220 (0.5 torr)
Melting Point 190°C
Molecular Formula C21H27ClN2O2
Molecular Weight 374.90400
Exact Mass 374.17600
PSA 35.94000
LogP 2.93170
InChIKey ZQDWXGKKHFNSQK-UHFFFAOYSA-N
SMILES OCCOCCN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1
Storage condition 2-8℃
Water Solubility < 700 MG/ML

 Toxicological Information

This table summarizes toxicological test data, acute & chronic toxicity and ecological hazard parameters for this chemical.

CHEMICAL IDENTIFICATION

RTECS NUMBER :
KK2275000
CHEMICAL NAME :
Ethanol, 2-(2-(4-(p-chloro-alpha-phenylbenzyl)-1-piperazinyl)e thoxy)-
CAS REGISTRY NUMBER :
68-88-2
BEILSTEIN REFERENCE NO. :
0321392
LAST UPDATED :
199612
DATA ITEMS CITED :
11
MOLECULAR FORMULA :
C21-H27-Cl-N2-O2
MOLECULAR WEIGHT :
374.95
WISWESSER LINE NOTATION :
T6N DNTJ AYR&R D6& D2O2Q

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 :
CHTPBA Chimica Therapeutica. (Paris, France) V.1-8, 1965-73. For publisher information, see EJMCA5. Volume(issue)/page/year: 3,210,1968
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
160 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CHTPBA Chimica Therapeutica. (Paris, France) V.1-8, 1965-73. For publisher information, see EJMCA5. Volume(issue)/page/year: 3,210,1968
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 :
ANPBAZ Acta Neurologia et Psychiatrica Belgica. (Brussels, Belgium) V.48-69, 1948-69. For publisher information, see ANUBBR. Volume(issue)/page/year: 61,669,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
400 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CHTPBA Chimica Therapeutica. (Paris, France) V.1-8, 1965-73. For publisher information, see EJMCA5. Volume(issue)/page/year: 3,210,1968
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
81300 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DPHFAK Dissertationes Pharmaceuticae et Pharmacologicae. (Warsaw, Poland) V.18-24, 1966-72. For publisher information, see PJPPAA. Volume(issue)/page/year: 23,281,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
137 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,237,1972 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
400 mg/kg
SEX/DURATION :
female 13-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - homeostasis
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 17,67,1970
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
DOSE :
40 mg/kg
SEX/DURATION :
female 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
REFERENCE :
FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 12,346,1961
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
350 mg/kg
SEX/DURATION :
female 15-21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
28QFAD "Laboratory Animals in Drug Testing, Symposium of the 5th International Committee on Laboratory Animals, Hanover, 1972," Speigel, A. ed., Stuttgart, Fed. Rep. Ger., Gustav Fischer Verlag, 1973 Volume(issue)/page/year: -,233,1973
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1500 mg/kg
SEX/DURATION :
female 1-60 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - stillbirth
REFERENCE :
28QFAD "Laboratory Animals in Drug Testing, Symposium of the 5th International Committee on Laboratory Animals, Hanover, 1972," Speigel, A. ed., Stuttgart, Fed. Rep. Ger., Gustav Fischer Verlag, 1973 Volume(issue)/page/year: -,233,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6151 No. of Facilities: 52 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 1362 (estimated) No. of Female Employees: 719 (estimated)

 Synthetic Route

This table presents publicly reported synthetic routes, reaction conditions, reactants and product information of the compound.

ETHYLENE OXIDE structure

ETHYLENE OXIDE

CAS#:75-21-8

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Hydroxyzine Structure

Hydroxyzine

CAS#:68-88-2

Learn More
Literature: Industrie Chimique Belge, , vol. 19, p. 1176,1181

 Precursor & DownStream

This table lists upstream starting materials and downstream derivative products related to this chemical.

Precursor  1

DownStream  0

 Customs

This table shows customs‑related data including HS‑code, tariff and regulatory conditions for import and export.

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%

 HydroxyzineBioassay

View more

This table contains target information, in‑vitro & in‑vivo assay data for this compound.

Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase
Name: Cytochrome P450 Family 1 Subfamily A Member 2 (CYP1A2) small molecule antagonists: lu...
Source: 824
External Id: CYP273
Name: Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolis...
Source: ChEMBL
Target: Cytochrome P450 2C9
External Id: CHEMBL4478999
Name: Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolis...
Source: ChEMBL
Target: Cytochrome P450 3A4
External Id: CHEMBL4479053
Name: Lipophilicity, log D at pH7.4
Source: ChEMBL
Target: N/A
External Id: CHEMBL895152
Name: Acid dissociation constant, pKa of the compound
Source: ChEMBL
Target: N/A
External Id: CHEMBL895153
Name: Dissociation constant, pKa by capillary electrophoresis
Source: ChEMBL
Target: N/A
External Id: CHEMBL1023026
Name: Lipophilicity, log D at pH 7.4 by liquid chromatography
Source: ChEMBL
Target: N/A
External Id: CHEMBL1023023
Name: Lipophilicity, log P by microemulsion electrokinetic chromatography
Source: ChEMBL
Target: N/A
External Id: CHEMBL1023024
Name: Primary qHTS for inhibitors of NSP2Pro chikungunya virus (CHIKV)
Source: NCGC
External Id: APP-Toga-CHIKV-nsp2-p
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 Synonyms

This table collects all English aliases, systematic names and CAS‑related synonyms of the compound.

Hydroxyzine
EINECS 200-693-1
2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethanol

 Hydroxyzine | FAQ

This section contains frequently‑asked‑questions about this compound, including basic parameters, properties, storage conditions and corresponding answers.

Q: What are the upstream materials of hydroxyzine?
A: Related upstream materials(CAS) of hydroxyzine: 75-21-8.
Q: What English synonyms does hydroxyzine have?
A: English synonyms of hydroxyzine: Hydroxyzine, EINECS 200-693-1, 2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethanol.
Q: What is the CAS number of hydroxyzine?
A: CAS number of hydroxyzine is 68-88-2.
Q: What is the molecular formula of hydroxyzine?
A: Molecular formula of hydroxyzine is C21H27ClN2O2.
Q: What are the storage conditions for hydroxyzine?
A: Storage conditions for hydroxyzine: 2-8℃.
Q: What is the polar surface area (PSA) of hydroxyzine?
A: Polar surface area (PSA) of hydroxyzine is 35.94000.
Q: What is the safety information for hydroxyzine?
A: Safety information for hydroxyzine: S3:Keep in a cool place . S16:Keep away from sources of ignition - No smoking . S23:Do not breathe gas/fumes/vapor/spray (appropriate wording to be specified by the manufacturer) . S26:In case of contact with eyes, rinse immediately with plenty of water an.
Q: What is the molecular weight of hydroxyzine?
A: Molecular weight of hydroxyzine is 374.90400.
Q: What is the LogP of hydroxyzine?
A: LogP of hydroxyzine is 2.93170.
Q: What is the SMILES notation of hydroxyzine?
A: SMILES notation of hydroxyzine is OCCOCCN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1.

 Hydroxyzinefactory

This table lists manufacturers and suppliers of this compound, including vendor names and product supply reference information.

Shanghai Nianxing Industrial Co., Ltd
Dayang Chem (Hangzhou) Co., Ltd.
Henan Tianfu Chemical Co., Ltd.
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