Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K 2P (two-pore domain potassium channel) TREK-1 with an IC 50 of 402.7 μM in COS-7 cells membrane. Ropivacaine is used for the research of neuropathic pain management.
性状
Solid
IC50 & Target[1][2]
IC50: sodium ion influxIC50: 402.7 μM (TREK-1 in COS-7 cells membrane)
体内研究(In Vivo)
Epidural administration of Ropivacaine effectively blocks neuropathic pain (both mechanical allodynia and heat hyperalgesia) without induction of analgesic tolerance and significantly delays the development of neuropathic pain produced by peripheral nerve injury.
Ropivacaine inhibits pressure-induced increases in filtration coefficient (Kf) without affecting pulmonary artery pressure (Ppa), pulmonary capillary pressures (Ppc), and zonal characteristics (ZC).
Ropivacaine prevents pressure-induced lung edema and associated hyperpermeability as evidence by maintaining PaO2, lung wet-to-dry ratio and plasma volume in levels similar to sham rats.
Ropivacaine inhibits pressure-induced NO production as evidenced by decreased lung nitro-tyrosine content when compared to hypertensive lungs.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Dene Simpson, et al. Ropivacaine: a review of its use in regional anaesthesia and acute pain management. Drugs. 2005;65(18):2675-717.[2]. Li TF, et al. Epidural sustained release ropivacaine prolongs anti-allodynia and anti-hyperalgesia in developing and established neuropathic pain. PLoS One. 2015 Jan 24;10(1):e0117321.
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (45.55 mM; Need ultrasonic)配制储备液