Home Neuronal Signaling Histamine Receptor antagonist Hydroxyzine 2HCl

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Hydroxyzine 2HCl Histamine Receptor antagonist

Cat.No.S4026

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 Histamine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 447.83

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 447.83 Formula

C21H27ClN2O2.2HCl

 Storage (From the date of receipt)
CAS No. 2192-20-3 -- Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCN1CCOCCO)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl.Cl.Cl

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (200.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 90 mg/mL

Ethanol : 15 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
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]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11290874/
  • [5] https://pubmed.ncbi.nlm.nih.gov/523173/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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