Absorption, Distribution and Excretion
Easily absorbed from the gastrointestinal tract Biological Half-Life 1 to 2 hours

Protein Binding

93%

Profenamine belongs to the phenothiazine class of compounds, characterized by the substitution of a hydrogen atom on a nitrogen atom with a 2-(diethylamino)propyl group. It is an antimuscarinic drug, and its hydrochloride salt is used for the symptomatic treatment of Parkinson's disease. Profenamine has various pharmacological effects, including acting as a muscarinic receptor antagonist, an anti-Parkinson's drug, a histamine receptor antagonist, an adrenergic receptor antagonist, and an anti-movement disorder drug. It belongs to the phenothiazine class of compounds and is also a tertiary amine compound. Profenamine (also known as ethylpromethazine) is a phenothiazine derivative. It is primarily used as an anti-movement disorder drug to treat Parkinson's disease. In Canada, Profenamine is marketed under the brand name Parsitan. In the United States, Profenamine is discontinued. See also: Ethylpromethazine hydrochloride (note moved to) Profenamine (hibenzate) (note moved here).

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Drug Indications
Profenamide is indicated for the treatment of drug-induced extrapyramidal reactions and symptoms of encephalitis, arteriosclerosis, or idiopathic Parkinson's disease (such as rigidity, akinesia, drooling, oculomotor crisis, tremor, etc.). It is also used to control severe reactions to certain drugs (such as reserpine).

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Mechanism of Action
The anti-Parkinsonian effect of propfenamide can be attributed to its anticholinergic properties. Profenamide partially blocks central (striatal) cholinergic receptors, thereby helping to balance cholinergic and dopaminergic activity in the basal ganglia; salivation may be reduced, and smooth muscle may relax. Drug-induced extrapyramidal symptoms and Parkinsonian syndrome symptoms may be relieved, but tardive dyskinesia is not relieved, and the anticholinergic effect may actually worsen these symptoms. The local anesthetic effect of propfenamide is due to its antagonistic effect on NMDA glutamate receptors. Glutamate is an important neurotransmitter in the nociceptive pathway, especially N-methyl-D-aspartate (NMDA) glutamate receptors, which are closely related to the mediation of neuropathic pain. Excessive release of glutamate from NMDA receptors on spinal dorsal horn neurons leads to overactivation and hypersensitivity of these receptors (manifested as hyperalgesia), which is considered a component of neuropathic pain. Profenalamine is a phenothiazine anti-motor dyskinesia drug used to treat Parkinson's disease. This drug helps patients regain normal physical activity while alleviating disease symptoms by improving muscle control and reducing rigidity. It is also used to control serious adverse reactions caused by certain drugs, such as reserpine, phenothiazines, chlorprothixone, thiothixone, loxapine, and haloperidol. Unlike other NMDA receptor antagonists, profenalamine—due to its anticholinergic effects—has few neurotoxic side effects. Profenalamine also has mild antihistamine and local anesthetic effects.

C19H24N2S

312.475

312.166

522-00-9

1094-08-2 (HCl);522-00-9;

3290

Typically exists as solid at room temperature

1.1±0.1 g/cm3

430.1±34.0 °C at 760 mmHg

53-55°

213.9±25.7 °C

0.0±1.0 mmHg at 25°C

1.599

5.84

0

3

5

22

322

0

CCN(CC)C(C)CN1C2=CC=CC=C2SC3=CC=CC=C31

CDOZDBSBBXSXLB-UHFFFAOYSA-N

InChI=1S/C19H24N2S/c1-4-20(5-2)15(3)14-21-16-10-6-8-12-18(16)22-19-13-9-7-11-17(19)21/h6-13,15H,4-5,14H2,1-3H3

10H-Phenothiazine-10-ethanamine, N,N-diethyl-alpha-methyl-

Profenamine SC 2538 SKF 2538W 483 W483W-483 RP 3356

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)