Ropivacaine mesylate 是一种有效的钠通道 (Sodium Channel) 阻断剂。Ropivacaine 通过可逆地抑制钠离子内流 (sodium ion influx) 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 402.7 μM。
产品描述
Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1] [2]. 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 cell's membrane [3].
体内活性
Epidural administration of Ropivacaine mesylate 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 mesylate inhibits pressure-induced increases in filtration coefficient (Kf) without affecting pulmonary artery pressure (Ppa), pulmonary capillary pressures (Ppc), and zonal characteristics (ZC) [2]. Ropivacaine mesylate 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 mesylate 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) [2] Dosage: 1 μM Administration: Infusion (added to the perfusate reservoir) Result: Attenuated pressure-dependent increases in filtration coefficient (K f ).
Cas No.
854056-07-8
分子式
C18H30N2O4S
分子量
370.51
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years