| Size | Price | Stock | Qty |
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| 5g |
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| Other Sizes |
| Targets |
Promethazine hydrochloride primarily targets histamine H1 receptors, acting as a competitive antagonist. By blocking H1 receptors, it prevents the effects of histamine, including vasodilation, increased vascular permeability, and bronchoconstriction. It also has affinity for muscarinic acetylcholine receptors (anticholinergic effects), dopamine D2 receptors (antiemetic effects), and α1-adrenergic receptors (hypotension). Its broad receptor binding profile contributes to its diverse therapeutic effects and side effect profile.
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| ln Vitro |
In vitro, promethazine hydrochloride binds to histamine H1 receptors and other neurotransmitter receptors. Its activity is assessed using radioligand binding assays, where the compound displaces radiolabeled ligands from receptor preparations. The compound's antihistamine activity is characterized by its ability to inhibit histamine-induced signaling in cell-based assays. Specific IC50 values for receptor binding are not detailed in the provided search results.
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| ln Vivo |
In vivo, promethazine hydrochloride is used for the treatment of allergic conditions (rhinitis, urticaria), motion sickness, and as a sedative. It is also used for the management of nausea and vomiting, including postoperative nausea and chemotherapy-induced nausea. The compound is available in various formulations, including oral tablets, syrups, suppositories, and injectable solutions.
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| Enzyme Assay |
The in vitro activity of promethazine hydrochloride is assessed using radioligand binding assays. Membrane preparations from cells or tissues expressing histamine H1 receptors are incubated with a radiolabeled H1 receptor ligand (e.g., [³H]mepyramine) in the presence of varying concentrations of promethazine hydrochloride. The displacement of the radiolabeled ligand is measured to determine the Ki or IC50. For functional assays, cells expressing H1 receptors are treated with promethazine hydrochloride, and histamine-induced signaling responses are measured.
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| Cell Assay |
For cellular assays, cell lines expressing histamine H1 receptors or other relevant receptors are used. Cells are cultured in appropriate media and treated with various concentrations of promethazine hydrochloride (typically 0.1 nM to 100 μM) for defined periods. Receptor occupancy is assessed by radioligand binding. Functional assays measure the inhibition of histamine-induced calcium mobilization. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo, promethazine hydrochloride is administered orally, rectally, or intramuscularly. In animal models, antihistamine effects are assessed by measuring inhibition of histamine-induced responses. Antiemetic effects are assessed in models of motion sickness or chemotherapy-induced emesis. In clinical settings, dosing regimens vary depending on the indication and route of administration.
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| ADME/Pharmacokinetics |
Promethazine hydrochloride has a molecular weight of 320.88 g/mol and a molecular formula of C17H20N2S·HCl. It is a phenothiazine derivative. The compound is soluble in water and should be stored under appropriate conditions to maintain stability. Specific pharmacokinetic parameters are not detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Based on the minimal excretion of other phenothiazine derivatives, occasional short-term use of Promethazine to treat nausea and vomiting poses little risk to breastfed infants. When used repeatedly, the infant should be monitored for excessive sedation. Because Promethazine can reduce basal prolactin levels, taking it during labor before lactation is fully established, or in combination with sympathomimetic drugs (such as pseudoephedrine), may interfere with lactation. Breastfeeding women should prioritize antiemetics that do not have potent histamine-blocking effects. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk Unlike most phenothiazine drugs, Promethazine typically reduces basal prolactin levels in non-lactating women. In a small study, women who took Promethazine, meperidine, and secobarbital during labor experienced a 14-hour delay in the onset of lactation stage II. Compared to women who did not take any medication, women who took meperidine or secobarbital alone experienced a 7-hour delay in the onset of lactation stage II, but the difference was not statistically significant. The effects of postpartum Promethazine use are unclear, but if taken early postpartum, it may interfere with lactation establishment. Promethazine hydrochloride can cause sedation, anticholinergic effects (dry mouth, constipation, blurred vision), hypotension, and extrapyramidal symptoms. Neuroleptic malignant syndrome is a rare but potentially fatal complication. The compound should be used with caution in patients with cardiovascular disease, liver disease, or a history of seizures. |
| References |
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| Additional Infomation |
Promethazine hydrochloride is an odorless white to pale yellow Crystals powder with a bitter taste. A 10% aqueous solution has a pH of 3.5–5.0. (NTP, 1992)
Promethazine hydrochloride is the hydrochloride salt of Promethazine. It possesses a variety of pharmacological effects, including antipruritic, H1 receptor antagonist, local anesthetic, antiemetic, sedative, anti-allergic, anticoronavirus, and anti-aging properties. It contains a Promethazine (1+) molecule. Promethazine hydrochloride is the hydrochloride form of Promethazine, a phenothiazine derivative with antihistamine, sedative, and antiemetic effects. Promethazine hydrochloride selectively blocks peripheral H1 receptors, thereby weakening the effects of histamine on effector cells. Promethazine hydrochloride can also block central histamine receptors, thereby inhibiting the reticular formation and producing sedative and hypnotic effects. Furthermore, Promethazine hydrochloride also possesses central anticholinergic properties, possibly mediating nausea and vomiting through action on the medullary chemoreceptor trigger zone. It is a phenothiazine derivative with histamine H1 receptor blocking, antimuscarinic, and sedative effects. It is used as an antihistamine, antipruritic, motion sickness medication, and sedative, and is also used in animals. See also: Promethazine (active ingredient); phenothiazine (subclass); codeine phosphate; Promethazine hydrochloride (ingredient)... See more... Promethazine hydrochloride is a clinically approved medication used for allergic conditions, motion sickness, sedation, and antiemesis. It is available as a generic medication. The hydrochloride salt is the most common formulation for oral and parenteral administration. Promethazine is included on the World Health Organization's List of Essential Medicines. |
| Molecular Formula |
C17H21CLN2S
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|---|---|
| Molecular Weight |
320.8800
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| Exact Mass |
320.111
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| CAS # |
58-33-3
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| Related CAS # |
Promethazine-d4 hydrochloride;1173018-74-0
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| PubChem CID |
6014
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| Appearance |
White to off-white solid powder
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| Density |
1.131 g/cm3
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| Boiling Point |
403.7ºC at 760 mmHg
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| Melting Point |
230-232°C
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| Flash Point |
198ºC
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| LogP |
5.106
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
298
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XXPDBLUZJRXNNZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20N2S.ClH/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19;/h4-11,13H,12H2,1-3H3;1H
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| Chemical Name |
N,N-dimethyl-1-phenothiazin-10-ylpropan-2-amine;hydrochloride
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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: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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) |
H2O : ~100 mg/mL (~311.64 mM)
DMSO : ~50 mg/mL (~155.82 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.79 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 25.0 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: ≥ 2.5 mg/mL (7.79 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 120 mg/mL (373.97 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1164 mL | 15.5821 mL | 31.1643 mL | |
| 5 mM | 0.6233 mL | 3.1164 mL | 6.2329 mL | |
| 10 mM | 0.3116 mL | 1.5582 mL | 3.1164 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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