Hydroxyzine 2HCl

Hydroxyzine is a histamine H1-receptor antagonist, inhibits binding of [3H]pyrilamine/[3H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM.

Hydroxyzine 2HCl Chemical Structure

Hydroxyzine 2HCl Chemical Structure

CAS: 2192-20-3

Selleck's Hydroxyzine 2HCl has been cited by 2 Publications

1 Customer Review

Purity & Quality Control

Batch: S402601 DMSO] 90 mg/mL] false] Water] 90 mg/mL] false] Ethanol] 15 mg/mL] false Purity: 99.97%
99.97

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Biological Activity

Description Hydroxyzine is a histamine H1-receptor antagonist, inhibits binding of [3H]pyrilamine/[3H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM.
Targets
Histamine H1 receptor [1]
10 nM-19 nM
In vitro
In vitro Hydroxyzine 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. [2] 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). [3] Hydroxyzine (500 µM) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 µg/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen. [4]
In Vivo
In vivo 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. [4] 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. [5]
Animal Research Animal Models Sprague-Dawley rats
Dosages 50 mg/kg
Administration Intraperitoneal injection
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04188106 Completed
Smoking Cessation|Stress|Sleep Disturbance|Nausea
Rose Research Center LLC|Foundation for a Smoke Free World INC
June 17 2019 Phase 4

Chemical Information & Solubility

Molecular Weight 447.83 Formula

C21H27ClN2O2.2HCl

CAS No. 2192-20-3 SDF --
Smiles C1CN(CCN1CCOCCO)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (200.96 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 90 mg/mL

Ethanol : 15 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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