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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Choose Selective Histamine Receptor Inhibitors
|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.|
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.  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).  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. 
|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.  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. |
-  Anthes JC, et al. Eur J Pharmacol, 2002, 449(3), 229-237.
-  Minogiannis P, et al. Int J Immunopharmacol, 1998, 20(10), 553-563.
-  Dimitriadou V, et al. Int J Immunopharmacol, 2000, 22(9), 673-684.
|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:
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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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