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| Other Sizes |
| Targets |
Diphenylpyraline hydrochloride targets the histamine H1 receptor. By binding to these receptors, it prevents histamine from exerting its effects, which include vasodilation, increased vascular permeability, and smooth muscle contraction. It also has anticholinergic activity, targeting muscarinic acetylcholine receptors. Additionally, it acts as a dopamine reuptake inhibitor, targeting the dopamine transporter.
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| ln Vitro |
In mouse nucleus accumbens slices, dopamine uptake is markedly inhibited by diphenylpyrroline hydrochloride (10 μM) [2].
In vitro, diphenylpyraline hydrochloride binds to histamine H1 receptors with high affinity. It demonstrates anticholinergic activity. Its ability to inhibit dopamine reuptake has been characterized in neurotransmitter uptake assays. It shows significant variation in solubility across different solvent systems. |
| ln Vivo |
Intraperitoneal injection of diphenylpyraline hydrochloride (5–10 mg/kg) causes mice's locomotor activation and raises extracellular dopamine levels in the nucleus accumbens by approximately 200 percent [2].
In vivo, diphenylpyraline hydrochloride is used for its antihistamine properties, producing therapeutic antiallergic effects. It is also used in the treatment of Parkinsonism due to its anticholinergic and dopamine reuptake inhibitory effects. Its therapeutic effects are achieved by blocking histamine and acetylcholine receptors, and by increasing dopamine levels in the brain. |
| Enzyme Assay |
In vitro receptor binding assays for diphenylpyraline hydrochloride measure its affinity for histamine H1 receptors, muscarinic acetylcholine receptors, and the dopamine transporter. Radioligand binding assays are used to determine its binding affinity (Ki) for these targets.
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| Cell Assay |
In vitro cell-based assays for diphenylpyraline hydrochloride are not typically performed. Its activity is characterized by its receptor binding profile and its functional effects in animal models. Its effects on neurotransmitter uptake can be assessed in synaptosome preparations.
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice [2]
Doses: 5-10 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results:It has psychostimulant properties. In vivo animal experiments for diphenylpyraline hydrochloride have been conducted in models of allergy and Parkinsonism. Its antihistamine effects are assessed by measuring its ability to inhibit histamine-induced responses. Its antiparkinsonian effects are assessed in models of Parkinson's disease. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Absorbed well after oral administration. Metabolism/Metabolites Liver Diphenylpyraline hydrochloride has a molecular weight of 317.85 and a molecular formula of C19H24ClNO. It is a white to off-white powder. It is soluble in DMSO (61 mg/mL). Its exact mass is 317.1546. It is typically stored at room temperature. |
| Toxicity/Toxicokinetics |
Protein Binding
99% Human Serum Albumin Diphenylpyraline hydrochloride is a drug with a known safety profile. As a first-generation antihistamine, it can cause sedation, drowsiness, and anticholinergic side effects such as dry mouth and blurred vision. It is a research compound and is not intended for human use without proper authorization. |
| References | |
| Additional Infomation |
Diphenylpyraline is a piperidine compound, a diphenyl methyl ether derivative of 1-methyl-4-hydroxypiperidine. It is a sedative antihistamine; its hydrochloride salt is used to relieve allergy symptoms, including rhinitis and hay fever, as well as to treat itchy skin conditions. It can also be used as an ingredient in combination preparations to relieve cough and common cold symptoms. It acts as both an H1 receptor antagonist and a cholinergic antagonist. It belongs to the piperidine class of compounds and is also a tertiary amine. Diphenylpyraline is an antihistamine. Antihistamines used to treat allergies act by competing with histamine for H1 receptor sites on effector cells. Antihistamines can prevent, but cannot reverse, reactions mediated solely by histamine. Antihistamines antagonize most of the pharmacological effects of histamine to varying degrees, including urticaria and pruritus. An allergen is a substance that causes an allergic reaction. See also: Diphenylpyraline hydrochloride (note moved to). Drug Indications Used to treat allergic rhinitis, hay fever, and allergic dermatitis. Mechanism of Action Antihistamines used to treat allergies, such as diphenylpyrrolidine hydrochloride, act by competing with histamine for H1 receptor sites on effector cells. This reduces the effect of histamine, thus temporarily relieving allergy symptoms. Pharmacodynamics Diphenylpyrrolidine hydrochloride is an antihistamine that prevents but does not reverse histamine-mediated reactions. Diphenylpyrrolidine antagonizes most of the pharmacological effects of histamine, including urticaria and pruritus. Additionally, diphenylpyrrolidine may have anticholinergic effects (like most antihistamines) and may therefore cause dryness of the nasal mucosa.
Diphenylpyraline hydrochloride is a first-generation antihistamine with anticholinergic effects. It is a histamine H1 receptor antagonist. It also acts as a dopamine reuptake inhibitor and has been used in the treatment of Parkinsonism. It belongs to the diphenylpiperidine class of antihistamines. |
| Molecular Formula |
C19H24CLNO
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|---|---|
| Molecular Weight |
317.86
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| Exact Mass |
317.155
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| CAS # |
132-18-3
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| Related CAS # |
132-18-3 (hydrochloride)
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| PubChem CID |
3103
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| Appearance |
White to off-white solid powder
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| Boiling Point |
378.7ºC at 760mmHg
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| Melting Point |
203-205ºC(lit.)
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| Flash Point |
111.6ºC
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| Vapour Pressure |
6.18E-06mmHg at 25°C
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| LogP |
4.626
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
268
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OWQUZNMMYNAXSL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H23NO/c1-20-14-12-18(13-15-20)21-19(16-8-4-2-5-9-16)17-10-6-3-7-11-17/h2-11,18-19H,12-15H2,1H3
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| Chemical Name |
4-benzhydryloxy-1-methylpiperidine
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| Synonyms |
Diaphen; Diafen hydrochloride; Diphenylpyraline 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: 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 (~314.61 mM)
DMSO : ≥ 100 mg/mL (~314.61 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.87 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 (7.87 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 (7.87 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 (314.61 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 | 3.1460 mL | 15.7302 mL | 31.4604 mL | |
| 5 mM | 0.6292 mL | 3.1460 mL | 6.2921 mL | |
| 10 mM | 0.3146 mL | 1.5730 mL | 3.1460 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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