| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Histamine H1 receptors, as well as serotonin and acetylcholine receptors. Hydroxyzine pamoate is a histamine H1 receptor antagonist. It also has anticholinergic activity, which contributes to its sedative and antiemetic effects. Its effects on serotonin receptors may also play a role in its anxiolytic activity.
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| ln Vitro |
Hydroxyzine pamoate acts as a competitive antagonist at histamine H1 receptors. It also blocks muscarinic acetylcholine receptors, leading to anticholinergic effects such as dry mouth and drowsiness. Its effects on serotonin receptors are less well-characterized. The combination of these activities is thought to contribute to its anxiolytic, antihistaminic, and anti-pruritic effects.
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| ln Vivo |
In vivo, hydroxyzine pamoate is used for the symptomatic relief of anxiety and tension associated with psychoneurosis and as an adjunct in organic disease states. It is also used for the management of pruritus due to allergic conditions. Its sedative properties make it useful for premedication before anesthesia.
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| Enzyme Assay |
In vitro receptor binding assays for hydroxyzine pamoate involve measuring its affinity for histamine H1, muscarinic acetylcholine, and serotonin receptors using radioligand binding techniques. Membranes from cells expressing the receptors are incubated with radiolabeled ligands and increasing concentrations of hydroxyzine. Ki values are determined from competition binding curves.
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| Cell Assay |
Cellular assays for hydroxyzine pamoate involve treating cells expressing the target receptors with the compound and measuring its effects on receptor-mediated signaling. The compound's ability to block histamine-induced calcium mobilization or acetylcholine-induced responses can be assessed.
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| Animal Protocol |
In vivo animal studies for hydroxyzine pamoate typically involve administration to rodent models to assess its anxiolytic, antihistaminic, and sedative effects. Efficacy is assessed using behavioral assays such as the elevated plus maze, and by measuring histamine-induced responses.
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| ADME/Pharmacokinetics |
Hydroxyzine pamoate is well absorbed after oral administration, with a half-life of approximately 20 hours. It is metabolized in the liver, primarily by CYP3A4, to its active metabolite, cetirizine. The compound and its metabolites are excreted in urine and feces. Its pharmacokinetic profile supports once- or twice-daily dosing.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of hydroxyzine pamoate have established its safety profile. Common adverse effects include drowsiness, dry mouth, and dizziness. It can also cause blurred vision, constipation, and urinary retention due to its anticholinergic effects. The compound is contraindicated in patients with a history of hypersensitivity to hydroxyzine or its components.
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| References |
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| Additional Infomation |
Hydroxyzine pamoate is the pamoate form of hydroxyzine, a synthetic piperazine histamine H1 receptor antagonist with anti-allergic, antispasmodic, sedative, antiemetic, and anxiolytic effects. Hydroxyzine pamoate blocks H1 histamine receptors, thus 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 pamoate can cross the blood-brain barrier and act on histamine H1 receptors in the central nervous system. (NCI05) A histamine H1 receptor antagonist, it is effective in treating chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its main metabolite, cetirizine, it does not cause drowsiness. It is also used as an antiemetic and a sedative to relieve anxiety and tension.
Hydroxyzine pamoate is a first-generation antihistamine used for the treatment of anxiety, tension, and pruritus. It is a histamine H1 receptor antagonist with anticholinergic and sedative properties. It is available in oral capsule and suspension formulations. Its mechanism of action involves the antagonism of histamine H1 receptors, as well as the modulation of other neurotransmitter systems. |
| Molecular Formula |
C23H16O6.C21H27N2O2CL
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|---|---|
| Molecular Weight |
763.27382
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| Exact Mass |
762.27
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| CAS # |
10246-75-0
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| Related CAS # |
Hydroxyzine dihydrochloride;2192-20-3;Hydroxyzine;68-88-2;Hydroxyzine-d4 dihydrochloride
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| PubChem CID |
25096
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.182g/cm3
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| Boiling Point |
499.2ºC at 760mmHg
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| Flash Point |
255.7ºC
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| Vapour Pressure |
2.13E-17mmHg at 25°C
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| LogP |
7.323
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
55
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| Complexity |
945
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ASDOKGIIKXGMNB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H16O6.C21H27ClN2O2/c24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29;22-20-8-6-19(7-9-20)21(18-4-2-1-3-5-18)24-12-10-23(11-13-24)14-16-26-17-15-25/h1-10,24-25H,11H2,(H,26,27)(H,28,29);1-9,21,25H,10-17H2
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| Chemical Name |
4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid;2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethanol
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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, avoid exposure to moisture. |
| 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) |
DMSO : ~250 mg/mL (~327.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3102 mL | 6.5508 mL | 13.1015 mL | |
| 5 mM | 0.2620 mL | 1.3102 mL | 2.6203 mL | |
| 10 mM | 0.1310 mL | 0.6551 mL | 1.3102 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.
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