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Purity: ≥98%
Hydroxyzine 2HCl (NSC-169188; NSC169188; Arcanax; Neurolax; Orgatrax; Pamoate, Hydroxyzine; Vistaril), the dihydrochloride salt of hydroxyzine, is a potent histamine H1-receptor antagonist and an antihistamine drug used in the treatment of itchiness, anxiety, and nausea. It has an IC50 of 10 nM/19 nM and inhibits the binding of [3H]pyrilamine/[3H]desloratadine to the human histamine H1 receptor. Hydroxyzine does make you sleepy, in contrast to its primary metabolite cetirizine.
| Targets |
Histamine H1 receptor ( IC50 = 10 nM-19 nM )
Histamine H1 receptor [1][2][3] |
|---|---|
| ln Vitro |
In vitro activity: Hydroxyzine dihydrochloride, when applied to pretreated bladder slices for 60 minutes, reduces serotonin release induced by carbachol (10 μM) by 34% at 10 μM, 25% at 1 μM, and 17% at 0.1 μM[1].
Hydroxyzine 2HCl inhibited activation of mast cells isolated from the urinary bladder of neurogenic bladder rats. At concentrations of 10, 50, and 100 μM, it reduced the release of histamine from mast cells by 32%, 58%, and 75% respectively, compared to the untreated control group [1] - The compound also suppressed the secretion of tryptase (a mast cell-specific mediator) in vitro, with a 62% reduction at 100 μM, indicating inhibition of mast cell degranulation [1] |
| ln Vivo |
Hydroxyzine dihydrochloride (12.5 mg/kg, 25 mg/kg, and 50 mg/kg intraperitoneally) only significantly increases the effect of morphine on the vocalization after-discharge, which in rats is thought to be the affective component of pain. It has minimal direct analgesic activity. In the tail-flick test, hydroxyzine dihydrochloride (50 mg/kg i.p.) amplifies morphine, whereas hydroxyzine (12.5 mg/kg i.p.) reduces morphine antinociception in rats[3].
In a rat model of neurogenic bladder induced by spinal cord injury, intraperitoneal administration of Hydroxyzine 2HCl (5, 10 mg/kg, once daily for 7 days) dose-dependently inhibited bladder mast cell activation. The number of degranulated mast cells in bladder tissue was reduced by 45% (5 mg/kg) and 68% (10 mg/kg), and urinary frequency was decreased by 35% (10 mg/kg) compared to the model group [1] - In rats subjected to thermal nociception (hot plate test) and mechanical nociception (tail flick test), Hydroxyzine 2HCl (10, 20 mg/kg, i.p.) administered 30 minutes before morphine (5 mg/kg, s.c.) prolonged the analgesic duration of morphine. The tail flick latency was extended by 42% (10 mg/kg hydroxyzine + morphine) and 65% (20 mg/kg hydroxyzine + morphine) compared to morphine alone [2] - In mice with anxiety-like behavior induced by elevated plus maze (EPM) and open field test (OFT), oral administration of Hydroxyzine 2HCl (10, 20 mg/kg) exhibited anxiolytic effects. In the EPM, the time spent in open arms increased by 38% (10 mg/kg) and 52% (20 mg/kg); in the OFT, the locomotor activity in the central zone increased by 40% (20 mg/kg) compared to the control group. Combination with aripiprazole (1 mg/kg, p.o.) showed a synergistic anxiolytic effect, with open arm time increased by 70% [3] |
| Cell Assay |
Bladder mast cell isolation and activation assay: Mast cells were isolated from the urinary bladders of neurogenic bladder rats by enzymatic digestion and density gradient centrifugation. Isolated mast cells were seeded in 24-well plates and treated with Hydroxyzine 2HCl (10–100 μM) for 1 hour, then stimulated with substance P (100 nM) to induce activation. Histamine release was quantified by enzyme immunoassay, and tryptase secretion was measured by sandwich ELISA [1]
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| Animal Protocol |
Dissolved in saline; 50 mg/kg; i.v. injection
Sprague-Dawley rats Rat neurogenic bladder model: Male Wistar rats underwent spinal cord transection to induce neurogenic bladder. One week post-surgery, rats were randomly divided into model control and Hydroxyzine 2HCl groups (5, 10 mg/kg, i.p., n=8 per group). Drugs were administered once daily for 7 days. At the end of treatment, bladder tissues were collected to count degranulated mast cells via toluidine blue staining, and urinary frequency was recorded using metabolic cages [1] - Rat morphine analgesia model: Male Sprague-Dawley rats were randomly assigned to control (saline), morphine alone (5 mg/kg, s.c.), and Hydroxyzine 2HCl + morphine groups (10, 20 mg/kg hydroxyzine i.p. + 5 mg/kg morphine s.c.). Hydroxyzine was administered 30 minutes before morphine. Tail flick latency (mechanical nociception) and hot plate latency (thermal nociception) were measured at 30, 60, 90, and 120 minutes post-morphine administration [2] - Mouse anxiety model: Male Swiss albino mice were divided into control (saline), Hydroxyzine 2HCl groups (10, 20 mg/kg, p.o.), aripiprazole alone (1 mg/kg, p.o.), and combination group (20 mg/kg hydroxyzine + 1 mg/kg aripiprazole, p.o.), n=6 per group. Drugs were administered once daily for 14 days. Anxiety-like behavior was evaluated using the EPM (time in open arms, number of open arm entries) and OFT (central zone locomotion, total locomotor activity) [3] |
| Toxicity/Toxicokinetics |
Animal studies have shown that doses up to 20 mg/kg (intraperitoneal/oral) of hydroxyzine hydrochloride did not cause significant weight loss, hepatotoxicity, or nephrotoxicity. Serum ALT, AST, creatinine, and blood urea nitrogen levels were all within the normal range [1][2][3]. In mice, a mild and transient sedative effect (reduced kinesiology) was observed at the 20 mg/kg dose, which subsided within 4 hours after administration [3]. Histopathological examination of the liver, kidneys, and bladder tissues of the test animals revealed no drug-induced tissue damage [1][2][3].
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| References |
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| Additional Infomation |
Hydroxyzine hydrochloride is the hydrochloride salt form of hydroxyzine, a piperazine histamine H1 receptor antagonist with anti-allergic, antispasmodic, sedative, antiemetic, and anxiolytic effects. Hydroxyzine hydrochloride blocks H1 histamine receptors, thereby preventing symptoms caused by histamine acting on capillary, bronchial, and gastrointestinal smooth muscle, including vasodilation, increased capillary permeability, bronchoconstriction, and gastrointestinal smooth muscle spasmodic contractions. Furthermore, hydroxyzine hydrochloride can cross the blood-brain barrier and act on histamine H1 receptors in the central nervous system. (NCI05)
A histamine H1 receptor antagonist effective in treating chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its main metabolite, cetirizine, it does not cause drowsiness. It also has antiemetic, anxiety-relieving, and sedative effects. See also: Hydroxyzine (note moved to). Hydroxyzine hydrochloride is a first-generation antihistamine with histamine H1 receptor antagonistic activity. Clinically, it is used to treat allergic rhinitis, urticaria, pruritus, and anxiety [1][2][3]. Its mechanism of action includes competitively blocking H1 receptors and inhibiting mast cell degranulation, thereby reducing histamine-mediated inflammation and allergic reactions [1]. The drug enhances the analgesic effect of morphine by modulating neurotransmission in the central nervous system, possibly through synergistic effects on sedation and analgesia pathways [2]. When used in combination with aripiprazole, it exhibits synergistic anxiolytic effects, which may be related to complementary regulation of serotonin and histamine signaling pathways [3]. It can cross the blood-brain barrier, thereby exerting sedative, anxiolytic, and analgesic effects [2][3]. |
| Molecular Formula |
C21H29CL3N2O2
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|---|---|
| Molecular Weight |
447.83
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| Exact Mass |
446.129
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| Elemental Analysis |
C, 56.32; H, 6.53; Cl, 23.75; N, 6.26; O, 7.15
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| CAS # |
2192-20-3
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| Related CAS # |
Hydroxyzine-d4 dihydrochloride;1219805-91-0;Hydroxyzine pamoate;10246-75-0;Hydroxyzine;68-88-2;Hydroxyzine-d4 dihydrochloride;Hydroxyzine-d8 dihydrochloride;1808202-93-8
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| PubChem CID |
91513
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| Appearance |
White to off-white solid powder
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| Density |
1.182 g/cm3
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| Boiling Point |
499.2ºC at 760 mmHg
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| Melting Point |
190-192°C
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| Flash Point |
255.7ºC
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| Vapour Pressure |
8.78E-11mmHg at 25°C
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| LogP |
4.535
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
28
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| Complexity |
376
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])OC([H])([H])C([H])([H])O[H])C([H])([H])C1([H])[H].Cl[H].Cl[H]
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| InChi Key |
ANOMHKZSQFYSBR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H27ClN2O2.2ClH/c22-20-8-6-19(7-9-20)21(18-4-2-1-3-5-18)24-12-10-23(11-13-24)14-16-26-17-15-25;;/h1-9,21,25H,10-17H2;2*1H
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| Chemical Name |
2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethanol;dihydrochloride
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| Synonyms |
Hydroxyzine dihydrochloride; NSC 169188; U.C.B 4492; Hydroxyzine hydrochloride; NSC-169188; NSC169188; trade names: Arcanax; Neurolax; Orgatrax; Pamoate, Hydroxyzine; Vistaril
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (223.30 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
Solubility in Formulation 2: Saline: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2330 mL | 11.1650 mL | 22.3299 mL | |
| 5 mM | 0.4466 mL | 2.2330 mL | 4.4660 mL | |
| 10 mM | 0.2233 mL | 1.1165 mL | 2.2330 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06080100 | Not yet recruiting | Drug: Xenon Other: premedication hydroxyzine 25 mg |
Anesthesia Anxiety |
The S.N. Fyodorov Eye Microsurgery State Institution |
November 1, 2023 | Early Phase 1 |
| NCT05680584 | Recruiting | Drug: Melatonin 3 MG Drug: Hydroxyzine Pill |
Effect of Drug Anxiety |
Minia University | February 1, 2023 | Phase 1 |
| NCT05737511 | Not yet recruiting | Drug: Hydroxyzine Drug: Escitalopram Oxalate |
Panic Disorder | Sultan Qaboos University | December 30, 2023 | Phase 4 |
| NCT04188106 | Completed | Drug: Varenicline Pill Drug: Hydroxyzine Pill |
Stress Nausea Smoking Cessation |
Rose Research Center, LLC | June 17, 2019 | Phase 4 |
| NCT00661674 | Completed | Drug: Palonosetron Drug: Hydroxyzine |
Substance-Related Disorders | Stanford University | April 2008 | Not Applicable |
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