| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Histamine H1 receptors on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. Carbinoxamine maleate is a histamine-H1 receptor blocking agent. It competes with histamine for H1 receptor sites, preventing histamine from binding and exerting its effects.
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| ln Vitro |
Carbinoxamine maleate acts as a histamine-H1 receptor antagonist, competing with histamine for receptor sites on effector cells. By blocking H1 receptors, carbinoxamine prevents histamine-induced effects such as vasodilation, increased vascular permeability, bronchoconstriction, and smooth muscle contraction. The compound also has anticholinergic (drying) effects, which contribute to its efficacy in reducing rhinorrhea and other allergic symptoms. Sedative properties are also present due to the compound's ability to cross the blood-brain barrier and affect central histamine receptors.
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| ln Vivo |
In vivo, carbinoxamine maleate is used for the symptomatic treatment of seasonal and perennial allergic rhinitis. The compound relieves symptoms such as sneezing, rhinorrhea, nasal congestion, and itching. It is effective for the symptomatic treatment of allergic rhinitis. The anticholinergic and sedative properties of carbinoxamine contribute to its overall efficacy but may also cause adverse effects such as dry mouth, drowsiness, and blurred vision.
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| Enzyme Assay |
In vitro receptor binding assays for carbinoxamine maleate involve measuring the compound's affinity for histamine H1 receptors using radioligand binding techniques. Membranes from cells expressing H1 receptors are incubated with a radiolabeled H1 ligand (such as 3H-mepyramine) and increasing concentrations of carbinoxamine. Bound and free ligand are separated by filtration, and radioactivity is measured. Ki values are determined from competition binding curves. These assays confirm the H1 receptor antagonism of carbinoxamine.
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| Cell Assay |
Cellular assays for carbinoxamine maleate involve treating cells expressing H1 receptors with the compound and measuring H1 receptor-mediated signaling, such as calcium mobilization or changes in gene expression. The compound's ability to inhibit histamine-induced cellular responses is demonstrated in these assays. These studies confirm the functional antagonism of carbinoxamine at H1 receptors.
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| Animal Protocol |
In vivo animal studies for carbinoxamine maleate typically involve administration to rodent models of allergic rhinitis or other allergic conditions. The compound's ability to reduce histamine-induced responses, such as vascular permeability or bronchoconstriction, is assessed. These studies establish the efficacy of carbinoxamine in various preclinical models of allergy.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of carbinoxamine maleate show that the compound is absorbed following oral administration and distributes throughout the body, including the central nervous system. The compound is metabolized in the liver and eliminated primarily by renal excretion. The onset of action is rapid, and the duration of effect is several hours, supporting multiple daily dosing for allergic rhinitis.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Occasional use of small doses of Carbinoxamine during lactation may be acceptable. Larger doses or prolonged use may cause drowsiness and other adverse reactions in infants, or reduce milk production, especially when used in combination with sympathomimetic drugs (such as pseudoephedrine) or before lactation is fully established. Because Carbinoxamine has been shown to cause serious toxicity in children under 2 years of age, the manufacturer recommends avoiding breastfeeding while taking Carbinoxamine. Non-sedating antihistamines are a better alternative. ◉ Effects on Breastfed Infants There are currently no reports of breastfeeding infants while mothers are taking Carbinoxamine. In a telephone follow-up study, mothers reported that 10% of infants exposed to various antihistamines experienced irritability and colic, and 1.6% experienced drowsiness. All reactions did not require medical attention. ◉ Effects on Lactation and Breast Milk Higher doses of antihistamines can lower basal serum prolactin levels in non-lactating women and early postpartum women. However, pre-administration of antihistamines by postpartum mothers does not affect suckling-induced prolactin secretion. Whether lower doses of oral carbizamine have the same effect on serum prolactin, and whether changes in prolactin levels have any impact on breastfeeding success, is currently unknown. For mothers who have established lactation, prolactin levels may not affect their ability to breastfeed. Preclinical toxicity studies of carbinoxamine maleate have established its safety profile as an antihistamine. Adverse effects are primarily related to its anticholinergic and sedative properties and include drowsiness, dry mouth, blurred vision, and constipation. The compound is contraindicated in patients with narrow-angle glaucoma, prostatic hypertrophy, or other conditions that would be exacerbated by anticholinergic effects. Carbinoxamine is generally well tolerated at therapeutic doses. |
| References | |
| Additional Infomation |
Carbinoxamine maleate is the maleate salt of Carbinoxamine. It is an ethanolamine antihistamine used to treat hay fever and mild Parkinson's disease. It has a dual role as an H1 receptor antagonist, antihistamine, muscarinic receptor antagonist, and anti-Parkinson's disease agent. Its molecular structure contains Carbinoxamine. Carbinoxamine maleate belongs to the ethanolamine class of H1 antihistamines and has mild antimuscarinic and sedative effects. Carbinoxamine reduces the typical effects of histamine on H1 receptors in bronchial smooth muscle, capillaries, and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching, and spastic contractions of gastrointestinal smooth muscle. Carbinoxamine maleate is used to relieve allergy symptoms.
See also: Carbinoxamine (with active fraction). Carbinoxamine maleate is an ethanolamine derivative antihistamine with anticholinergic and sedative properties. It acts as a histamine-H1 receptor antagonist and is indicated for the symptomatic treatment of seasonal and perennial allergic rhinitis. Carbinoxamine competes with histamine for H1 receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. The compound is available in tablet and oral solution formulations. |
| Molecular Formula |
C16H19CLN2O
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| Molecular Weight |
290.7879
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| Exact Mass |
406.13
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| CAS # |
3505-38-2
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| Related CAS # |
Carbinoxamine-d6 maleate
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| PubChem CID |
5282409
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| Appearance |
White to off-white solid powder
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| Boiling Point |
381.1ºC at 760 mmHg
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| Melting Point |
116-118ºC
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| Flash Point |
184.3ºC
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| LogP |
3.114
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
28
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| Complexity |
386
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCOC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
GVNWHCVWDRNXAZ-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C16H19ClN2O.C4H4O4/c1-19(2)11-12-20-16(15-5-3-4-10-18-15)13-6-8-14(17)9-7-13;5-3(6)1-2-4(7)8/h3-10,16H,11-12H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;2-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-N,N-dimethylethanamine
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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 : ~100 mg/mL (~245.78 mM)
H2O : ~50 mg/mL (~122.89 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.14 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 (6.14 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 (6.14 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: 100 mg/mL (245.78 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 | 3.4389 mL | 17.1945 mL | 34.3891 mL | |
| 5 mM | 0.6878 mL | 3.4389 mL | 6.8778 mL | |
| 10 mM | 0.3439 mL | 1.7195 mL | 3.4389 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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