Hydroxyzine 2HCl

Catalog No.S4026

Hydroxyzine 2HCl Chemical Structure

Molecular Weight(MW): 447.83

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.

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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

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 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]

Protocol

Animal Research:[5]
+ Expand
  • Animal Models: Sprague-Dawley rats
  • Formulation: Saline
  • Dosages: 50 mg/kg
  • Administration: Intraperitoneal injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (200.96 mM)
Water 90 mg/mL (200.96 mM)
Ethanol 15 mg/mL (33.49 mM)
In vivo Add solvents individually and in order:
Saline
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 447.83
Formula

C21H27ClN2O2.2HCl

CAS No. 2192-20-3
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02374567 Recruiting Dementia|Depression|Schizophrenia|Psychosomatic Disorders|Anxiety Disorders Hannover Medical School January 2015 Phase 3
NCT01496911 Completed Healthy Volunteers Utrecht Institute for Pharmaceutical Sciences|Royal Netherlands Navy April 2012 Phase 4
NCT01372670 Withdrawn Anxiety in Those Patients With Anorexia Nervosa|Eating Disorder Not Otherwise Specified, BMI (<=18) HealthPartners Institute|Park Nicollet Eating Disorder Institute January 2012 Phase 4
NCT01501591 Recruiting Placebo Effect|Placebo Drug Interaction King Faisal Specialist Hospital & Research Center December 2011 --
NCT01250652 Completed Chronic Urticaria Association Asthma, Bulgaria|UCB Pharma March 2011 Phase 4
NCT01151696 Completed Pain University Hospital, Toulouse May 2010 Phase 4

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