Prodilidine
Prodilidine (CI-427) is an orally active, pyrrolidine-derived non-narcotic pain inhibitor. Prodilidine exerts analgesic activity against various nociceptive stimuli, and shows no antipyretic, anti-inflammatory or respiratory depressive effects. Prodilidine fails to inhibit withdrawal symptoms of addictive agents in monkeys, but exhibits excitatory effects and enhances the crossed extensor reflex at toxic doses. Prodilidine is well absorbed from the gastrointestinal tract and metabolized via hepatic microsomal N-demethylation, displaying isomer-specific activity, toxicity and metabolic characteristics. Prodilidine can be used in research related to chronic pain (e.g., cancer-, musculoskeletal/arthritis-derived), traumatic pain and arthritic pain.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3734-17-6
- 分子式: C15H21NO2
- 分子量:247.34
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
Prodilidine undergoes N-demethylation via liver microsomes from multiple species, with the (-)-Prodilidine showing greater demethylation than the (+)-Prodilidine by rat liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Prodilidine hydrochloride (11.2-17.8 mg/kg; p.o.; s.c.; i.v.) exhibits analgesic activity in rats, with ED50 values ranging from 11.2 mg/kg (intravenous) to 17.3 mg/kg (oral) in the tail-flick assay, and LD50 values ranging from 74 mg/kg (intravenous) to 253 mg/kg (oral)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:84.0 mg/kg (tail-pinch assay, p.o.); 72.3 mg/kg (tail-pinch assay, s.c.); 30.0 mg/kg (tail-pinch assay, i.v.); 7.2 mg/kg (writhing assay, s.c.); 318 mg/kg (LD50, p.o.); 194 mg/kg (LD50, s.c.); 91 mg/kg (LD50, i.v.)
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Administration:p.o. (tail-pinch assay); s.c. (tail-pinch assay, writhing assay); i.v. (tail-pinch assay)
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Result:Achieved an ED50 of 84.0 mg/kg orally in the tail-pinch assay.
Achieved an ED50 of 72.3 mg/kg subcutaneously in the tail-pinch assay.
Achieved an ED50 of 30.0 mg/kg intravenously in the tail-pinch assay.
Achieved an ED50 of 7.2 mg/kg subcutaneously in the writhing assay.
Reached an LD50 of 318 mg/kg orally in mice.
Reached an LD50 of 194 mg/kg subcutaneously in mice.
Reached an LD50 of 91 mg/kg intravenously in mice.
化学情報
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CAS 番号 3734-17-6
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分子量 247.34
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分子式 C15H21NO2
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SMILES
O=C(OC1(C=2C=CC=CC2)CCN(C)C1C)CC
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別名
CI-427
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)