| Size | Price | |
|---|---|---|
| Other Sizes |
| ln Vitro |
In mouse nucleus accumbens slices, dopamine uptake is markedly inhibited by diphenylpyrroline hydrochloride (10 μM) [2].
|
|---|---|
| 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].
|
| 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. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Well absorbed after oral administration. Metabolism / Metabolites Hepatic |
| Toxicity/Toxicokinetics |
Protein Binding
> 99% in human serum albumin |
| References | |
| Additional Infomation |
Diphenylpyraline is a member of the class of piperidines that is the benzhydryl ether derivative of 1-methyl-4-hydroxypiperidine. A sedating antihistamine, it is used as the hydrochloride for the symptomatic relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders. It is also used as the teoclate salt (piprinhydrinate) as an ingredient in compound preparations for the symptomatic relief of coughs and the common cold. It has a role as a H1-receptor antagonist and a cholinergic antagonist. It is a member of piperidines and a tertiary amine.
Diphenylpyraline is an antihistamine. Antihistamines used in the treatment of allergy act by competing with histamine for H 1-receptor sites on effector cells. Antihistamines prevent, but do not reverse, responses mediated by histamine alone. Antihistamines antagonize, in varying degrees, most of the pharmacological effects of histamine, including urticaria and pruritus. Allergen is a substance that elicits an allergic reaction. See also: Diphenylpyraline Hydrochloride (annotation moved to). Drug Indication For use in the treatment of allergic rhinitis, hay fever, and allergic skin disorders. Mechanism of Action Antihistamines such as diphenylpyraline used in the treatment of allergy act by competing with histamine for H1-receptor sites on effector cells. This reduces the effects of histamine, leading to a temporary reduction of allergy symptoms. Pharmacodynamics Diphenylpyraline is an antihistamine that prevents, but does not reverse, responses mediated by histamine alone. Diphenylpyraline antagonizes most of the pharmacological effects of histamine, including urticaria and pruritus. Also, diphenylpyraline may exhibit anticholinergic actions (as do most of the antihistamines) and may thus provide a drying effect on the nasal mucosa. |
| Molecular Formula |
C19H24CLNO
|
|---|---|
| Molecular Weight |
317.86
|
| Exact Mass |
317.155
|
| CAS # |
132-18-3
|
| Related CAS # |
132-18-3 (hydrochloride)
|
| PubChem CID |
3103
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
378.7ºC at 760mmHg
|
| Melting Point |
203-205ºC(lit.)
|
| Flash Point |
111.6ºC
|
| Vapour Pressure |
6.18E-06mmHg at 25°C
|
| LogP |
4.626
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
21
|
| Complexity |
268
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
OWQUZNMMYNAXSL-UHFFFAOYSA-N
|
| 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
|
| Chemical Name |
4-benzhydryloxy-1-methylpiperidine
|
| Synonyms |
Diaphen; Diafen hydrochloride; Diphenylpyraline hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~314.61 mM)
DMSO : ≥ 100 mg/mL (~314.61 mM) |
|---|---|
| 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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