CAS 10246-75-0|Hydroxyzine (pamoate)

Introduction：Basic information about CAS 10246-75-0|Hydroxyzine (pamoate), including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Hydroxyzine (pamoate) BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles26
6. Synonyms

Common Name	Hydroxyzine (pamoate)
CAS Number	10246-75-0	Molecular Weight	763.274
Density	1.182g/cm3	Boiling Point	499.2ºC at 760mmHg
Molecular Formula	C₄₄H₄₃ClN₂O₈	Melting Point	/
MSDS	ChineseUSA	Flash Point	255.7ºC
Symbol	GHS07	Signal Word	Warning

Names

Name	hydroxyzine pamoate
Synonym	More Synonyms

Hydroxyzine (pamoate) BiologicalActivity

Description	Hydroxyzine pamoate 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 ug/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	Signaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/Immunology
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.

Description

Hydroxyzine pamoate 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 ug/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

Signaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/Immunology

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

Density	1.182g/cm3
Boiling Point	499.2ºC at 760mmHg
Molecular Formula	C₄₄H₄₃ClN₂O₈
Molecular Weight	763.274
Flash Point	255.7ºC
Exact Mass	762.270813
PSA	151.00000
LogP	7.32310
Vapour Pressure	2.13E-17mmHg at 25°C
InChIKey	ASDOKGIIKXGMNB-UHFFFAOYSA-N
SMILES	O=C(O)c1cc2ccccc2c(Cc2c(O)c(C(=O)O)cc3ccccc23)c1O.OCCOCCN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1
Storage condition	-20℃

Safety Information

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
Precautionary Statements	P301 + P312 + P330
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xn: Harmful;
Risk Phrases	R22
Safety Phrases	36
RIDADR	NONH for all modes of transport
WGK Germany	3

Articles26

Microencapsulation of hydroxyzine HCl by thermal phase separation: in vitro release enhancement and in vivo pharmacodynamic evaluation.

Pharm. Dev. Technol. 18(1) , 196-209, (2013)

The systemic effect of hydroxyzine hydrochloride following its oral administration or topical application is associated with non compliant anticholinergic effect. Subsequently, the present study aims ...

Worsening of contact dermatitis by oral hydroxyzine: a case report.

Dermatol. Online J. 19(2) , 4, (2013)

Hydroxyzine is commonly used to treat pruritic skin lesions. Although rare, hydroxyzine can sometimes be linked to worsening dermatitis in patients who have sensitivities to phenothiazines and/or ethy...

Acute generalized exanthematous pustulosis associated with 2 common medications: hydroxyzine and benzocaine.

J. Am. Acad. Dermatol. 71(4) , e147-9, (2014)

Synonyms

Paxistil {Pamoate}

Equipose {Pamoate}

4,4'-Methylenebis(3-hydroxy-2-naphthoic acid) - 2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]-1-piperazinyl}ethoxy)ethanol (1:1)

Paxisitil

4,4'-methanediylbis(3-hydroxynaphthalene-2-carboxylic acid) - 2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethanol (1:1)

Bobsule

Atarax P

Hydroxyzine pamoate salt

4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid,2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethanol

hydroxyzine pamoate

acide 4,4'-méthanediylbis(3-hydroxynaphtalène-2-carboxylique) - 2-(2-{4-[(4-chlorophényl)(phényl)méthyl]pipérazin-1-yl}éthoxy)éthanol (1:1)

2-Naphthalenecarboxylic acid, 4,4'-methylenebis[3-hydroxy-, compd. with 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]ethanol (1:1)

Hydroxyzyne pamoate

4,4'-Methandiylbis(3-hydroxynaphthalen-2-carbonsäure)--2-(2-{4-[(4-chlorphenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethanol(1:1)

EINECS 233-582-1

Hydroxyzine embonate

Hydroxyzine (pamoate)

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