| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| Targets |
Triprolidine HCl targets the histamine H1 receptor. It acts as a potent antagonist, binding to the H1 receptor and blocking the action of histamine. This inhibition prevents the vasodilation, increased vascular permeability, and smooth muscle contraction that are characteristic of allergic responses. By blocking these effects, triprolidine HCl alleviates symptoms such as itching, sneezing, runny nose, and watery eyes. The compound is a first-generation antihistamine, meaning it can cross the blood-brain barrier and cause sedation.
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| ln Vitro |
In vitro, triprolidine has been shown to be a potent antagonist of the histamine H1 receptor. In cell-based assays using cells expressing the H1 receptor, the compound inhibits histamine-induced calcium mobilization and other downstream signaling events. It has been used as a H1 histaminergic inhibitor to study its effect on long-term potentiation (LTP) in tuberomammillary nucleus (TMN) neurons. These studies confirm the compound's mechanism of action as an H1 receptor antagonist.
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| ln Vivo |
In rats, intrathecal injection of triprolidine hydrochloride monohydrate (292.81-1467.20 μg/kg) results in dose-dependent inhibition of spinal motor and sensory function [3].
In vivo, triprolidine HCl is effective in alleviating symptoms of allergic rhinitis, asthma, and urticaria. It is used as a symptomatic treatment for allergic reactions of the upper respiratory tract and for pruritic skin disorders. The compound is a component of many over-the-counter cough and cold medications. In rats, intrathecal injection of triprolidine hydrochloride monohydrate (292.81-1467.20 μg/kg) results in dose-dependent inhibition of spinal motor and sensory function. Male SD rats injected intrathecally with doses of 292.81 μg/kg, 488.02 μg/kg, 733.60 μg/kg, 1098.83 μg/kg, and 1467.20 μg/kg induced dose-dependent spinal block. |
| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for triprolidine HCl involve studying its binding affinity for the histamine H1 receptor. Radioligand binding assays are performed using membrane preparations from cells expressing the H1 receptor. The compound is incubated with a radiolabeled ligand, such as [3H]mepyramine, and the displacement of the ligand is measured to determine the Ki or IC50. These assays confirm the compound's affinity for the H1 receptor and its potency as an antagonist.
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| Cell Assay |
In vitro cell-based assays for triprolidine HCl are performed using cells that express the histamine H1 receptor. Cells are loaded with a calcium-sensitive fluorescent dye and stimulated with histamine. The inhibition of the calcium response by triprolidine HCl is measured as a functional readout of receptor antagonism. The compound's effects on cell signaling pathways and gene expression can also be assessed.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (300-350 g) [3]
Doses: 292.81 μg/kg, 488.02 μg/kg, 733.60 μg/kg, 1098.83 μg/kg, 1467.20 μg/kg Route of Administration: Intrathecal Injection Experimental Results: Induced dose-dependent spinal block. In vivo animal experiments for triprolidine HCl are conducted using rodent models of allergy and inflammation. The compound is administered orally or intrathecally. Models of passive cutaneous anaphylaxis (PCA) or histamine-induced skin reactions are used to evaluate the compound's antihistaminic activity. The compound's effects on behavior, such as sedation, are also assessed. In male SD rats (300-350 g), intrathecal injection of triprolidine hydrochloride monohydrate at doses of 292.81-1467.20 μg/kg resulted in dose-dependent inhibition of spinal motor and sensory function. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of triprolidine HCl indicate that it is well-absorbed after oral administration. The compound has a molecular weight of 314.857 and a molecular formula of C19H23ClN2. It is a white to off-white solid powder with a melting point of 115-120°C. The LogP is 4.657. The compound is metabolized in the liver, and its half-life is relatively short. It is excreted renally. The compound can cross the blood-brain barrier, which contributes to its central nervous system side effects, such as drowsiness.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for triprolidine HCl indicate that it is generally well-tolerated. Common side effects include drowsiness, dizziness, and dry mouth, which are typical of first-generation antihistamines. The compound may also cause gastrointestinal disturbances. As an anticholinergic agent, it should be used with caution in patients with glaucoma, prostatic hypertrophy, or other conditions that may be exacerbated by anticholinergic effects. It may cause sedation and should be used with caution when driving or operating machinery.
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| References |
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| Additional Infomation |
Triprilidine hydrochloride monohydrate is an odorless white crystalline powder with a bitter taste. (NTP, 1992)
Triprilidine hydrochloride (anh.) is a hydrochloride salt formed by the reaction of equimolar amounts of triprolidine and hydrogen chloride. Its monohydrate is used to relieve symptoms of urticaria, rhinitis, and various itchy skin conditions. It is an H1 receptor antagonist containing triprolidine (1+). Histamine H1 receptor antagonists are used to treat allergic rhinitis, asthma, and urticaria. It is an ingredient in cold and cough medicines. It may cause drowsiness. See also: Triprilidine (containing the active moiety)... See more... Other information: Triprolidine HCl is a first-generation antihistamine used for the symptomatic treatment of allergic conditions. It is a component of many over-the-counter cough and cold medications. The compound is also known as triprolidine hydrochloride monohydrate. Its CAS number is 6138-79-0. The related CAS numbers include triprolidine (486-12-4) and triprolidine hydrochloride (550-70-9). |
| Molecular Formula |
C19H23CLN2
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| Molecular Weight |
314.857
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| Exact Mass |
314.155
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| CAS # |
6138-79-0
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| Related CAS # |
Triprolidine;486-12-4;Triprolidine hydrochloride;550-70-9
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| PubChem CID |
5702129
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| Appearance |
White to off-white solid powder
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| Boiling Point |
462ºC at 760 mmHg
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| Melting Point |
115-120ºC
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| Flash Point |
233.2ºC
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| LogP |
4.657
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
336
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)/C(=C\CN2CCCC2)/C3=CC=CC=N3.Cl
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| InChi Key |
WYUYEJNGHIOFOC-NWBUNABESA-N
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| InChi Code |
InChI=1S/C19H22N2.ClH/c1-16-7-9-17(10-8-16)18(19-6-2-3-12-20-19)11-15-21-13-4-5-14-21/h2-3,6-12H,4-5,13-15H2,1H31H/b18-11+
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| Chemical Name |
2-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridine hydrochloride
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| Synonyms |
Triprolidine HCl Pro-Entra EntraVenenActidilat Pro-Actidil Actidilon.
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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) |
H2O : ~100 mg/mL (~300.42 mM)
DMSO : ~100 mg/mL (~300.42 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.51 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 (7.51 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 (7.51 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 (300.42 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 | 3.1760 mL | 15.8801 mL | 31.7601 mL | |
| 5 mM | 0.6352 mL | 3.1760 mL | 6.3520 mL | |
| 10 mM | 0.3176 mL | 1.5880 mL | 3.1760 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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