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Diphenidol (SKF478; SKF-478; SKF 478; Vontrol; Difenidol) is a potent antagonist of muscarinic M2 and M3 receptor used as an antiemetic and as an antivertigo agent.
ln Vitro |
In N2A cells, diphenidol (0.1-100 µM) inhibits Na+ current with an IC50 of 0.77 µM and a Hill coefficient of 1.15 [1].
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ln Vivo |
In rats, dofetidol (0.77 mg/rat; intrathecal injection; single dose) inhibits proprioception, nociception, and motor performance [1]. Rats with CCI-induced mechanical allodynia can be successfully reversed or entirely blocked by difenidol (0.62, 3.09 mg/kg; intraperitoneal injection; once daily for 7 days) [2].
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Animal Protocol |
Animal/Disease Models: Male Spraguee Dawley rat (275-325 g) [1].
Doses: 0.77 mg/rat (2.50 µmol/rat) Route of Administration: Intrathecal injection; single. Experimental Results: Resulting in 100% obstruction of motor function, proprioception and nociception, with durations of approximately 51 minutes, 77 minutes and 123 minutes respectively. Animal/Disease Models: Male adult SD (SD (Sprague-Dawley)) rat (200-250 g; CCI rat model) [2]. Doses: 0.62, 3.09 mg/kg (2, 10 µmol/kg) Route of Administration: intraperitoneal (ip) injection; single dose daily for 7 days. Experimental Results: Blockade of CCI-induced low mechanical withdrawal threshold 1 hour after administration. Reduces TNF-α levels on day 7 and alleviates neuropathic tactile allodynia after CCI in rats. |
References |
[1]. Leung YM, et al. Diphenidol inhibited sodium currents and produced spinal anesthesia. Neuropharmacology. 2010 Jun;58(7):1147-52.
[2]. Chen YW, et al. Systemic diphenidol reduces neuropathic allodynia and TNF-α overexpression in rats after chronic constriction injury. Neurosci Lett. 2013 Sep 27;552:62-5. |
Molecular Formula |
C21H27NO
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Molecular Weight |
309.4452
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Exact Mass |
309.2093
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CAS # |
972-02-1
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Related CAS # |
Diphenadol-d10
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1(C(C2C=CC=CC=2)(O)CCCN2CCCCC2)C=CC=CC=1
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Synonyms |
SKF478 SKF-478 SKF 478
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2315 mL | 16.1577 mL | 32.3154 mL | |
5 mM | 0.6463 mL | 3.2315 mL | 6.4631 mL | |
10 mM | 0.3232 mL | 1.6158 mL | 3.2315 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.