Ropivacaine是一种有效的钠通道(sodiumchannel)阻断剂，可以作为局部麻醉试剂。Ropivacaine通过可逆地抑制钠离子内流(sodiumioninflux)从而引起神经纤维脉冲传导阻滞。Ropivacaine也是一种K2P(双孔钾通道)TREK-1的抑制剂，在COS-7细胞膜上的IC50值为402.7μM。Ropivacaine用于局部麻醉和神经性疼痛的缓解的相关研究。
货号:ajcx31416
CAS:84057-95-4
分子式:C17H26N2O
分子量：274.4
溶解度:DMSO: 12.5 mg/mL (45.55 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Ropivacain is a potent sodium channel blocker and acts as a local anesthetic agent. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of regional anesthesia and neuropathic pain management[1].

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[1].Ropivacaine inhibits pressure-induced increases in filtration coefficient (Kf) without affecting pulmonary artery pressure (Ppa), pulmonary capillary pressures (Ppc), and zonal characteristics (ZC)[2].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[2].Ropivacaine inhibits pressure-induced NO production as evidenced by decreased lung nitro-tyrosine content when compared to hypertensive lungs[2]. Animal Model: Adult Sprague-Dawley rats (300-400g)[1]

[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. [3]. Hye Won Shin, et al. The inhibitory effects of bupivacaine, levobupivacaine, and ropivacaine on K2P (two-pore domain potassium) channel TREK-1. J Anesth [4]. Milan Patel, et al. Ropivacaine Inhibits Pressure-Induced Lung Endothelial Hyperpermeability in Models of Acute Hypertension. Life Sci. 2019 Apr 1;222:22-28.