Felodipine (Synonyms: 非洛di平)
Felodipine 是一種二氫吡啶，是一種有效的血管選擇性鈣通道 (b>calcium channel) 拮抗劑。Felodipine 通過(guò)選擇性作用于血管平滑肌，尤其是阻力血管來(lái)降低血壓。Felodipine 是具有抗高血壓活性，可誘導(dǎo)自噬。Felodipine 可以跨越血腦屏障。
生物活性
Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
體外研究(In Vitro)
Felodipine, a dihydropyridine calcium antagonist, is the most potent in relaxing porcine coronary arteries (IC50=0.15 nM)[1].
Felodipine, an L-type calcium channel blocker, induces autophagy and clears diverse aggregate-prone, neurodegenerative disease-associated proteins [2].
Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM[3].
分子量：384.25
性狀：Solid
Formula：C18H19Cl2NO4
CAS 號(hào)：72509-76-3
中文名稱(chēng)：非洛di平
運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 100 mg/mL (260.25 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6025 mL | 13.0124 mL | 26.0247 mL |
| 5 mM | 0.5205 mL | 2.6025 mL | 5.2049 mL |
| 10 mM | 0.2602 mL | 1.3012 mL | 2.6025 mL |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶
- 1.
請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution
- 2.
請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution
參考文獻(xiàn)
[1]. Johnson JD, et al. Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments. J Pharmacol Exp Ther. 1983;226(2):330-334. [Content Brief]
[2]. Siddiqi FH, et al. Felodipine induces autophagy in mouse brains with pharmacokinetics amenable to repurposing [published correction appears in Nat Commun. 2019 Jun 4;10(1):2530]. Nat Commun. 2019;10(1):1817. Published 2019 Apr 18. [Content Brief]
[3]. Yiu, S. and E.E. Knaus, Synthesis, biological evaluation, calcium channel antagonist activity, and anticonvulsant activity of felodipine coupled to a dihydropyridine-pyridinium salt redox chemical delivery system. J Med Chem, 1996. 39(23): p. 4576-82. [Content Brief]
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