Ropivacaine HCl 是一种强效钠通道阻滞剂，通过可逆抑制钠离子流入神经纤维来阻断冲动传导。
Ropivacaine hydrochloride is an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM.
Ropivacaine hydrochloride shows reversible inhibition of TREK-1 channels in a concentration-dependent manner. The half-maximal inhibitory concentrations (IC50) of Ropivacaine hydrochloride is 402.7±31.8 μM.. Hill coefficient is 0.89 for Ropivacaine hydrochloride[1].
Epidural injections of Ropivacaine hydrochloride (60, 180 and 600 μg) produce immediate and reversible motor paralysis. The motor blockade effect is dose-dependent, with paralysis duration of 4.6, 14.6 and 29.5 mins, respectively. Epidural Ropivacaine hydrochloride sustained release suspension also produces significant blockade of mechanical allodynia and thermal hyperalgesia by 59.5% and 70.9%, respectively (P<0.05). Ropivacaine hydrochloride sustained release suspension also produces a mild antinociception (response to heat stimulus) but longer anti-allodynic and anti-hyperalgesic effects, with biological half-lives of 6.4±2.5 hrs and 6.8±2.9 hrs, respectively (P<0.05). Multiple daily epidural administration of Ropivacaine hydrochloride sustained release suspension prolongs the preemptive effects (P<0.05)[2].
参考文献:
[1]. Shin HW, et al. The inhibitory effects of bupivacaine, levobupivacaine, and ropivacaine on K2P (two-pore domain potassium) channel TREK-1. J Anesth. 2014 Feb;28(1):81-6.
[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.
| Cell experiment [1]: | |
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Cell lines |
SW620 cells |
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Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0-1000 μM |
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Applications |
In SW620 cells, Ropivacaine concentration-dependently inhibited SW620 invasion through Matrigel with IC50 value of 3.8 μM. |
| Animal experiment [2]: | |
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Animal models |
male NMRI mice |
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Dosage form |
65 and 650 μM; intrascrotal injection |
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Application |
In male NMRI mice, Ropivacaine (650 μM) dose-dependently reduced TNF-a-induced leukocyte adhesion by 63%. Ropivacaine (650 μM) also abolished tissue accumulation of leukocytes in response to TNF-a activation by 79%. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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参考文献: [1]. Baptista-Hon DT1, Robertson FM1, Robertson GB1, et al. Potent inhibition by ropivacaine of metastatic colon cancer SW620 cell invasion and NaV1.5 channel function. Br J Anaesth. 2014 Jul;113 Suppl 1:i39-i48. [2]. Zhang XW1, Thorlacius H. Inhibitory actions of ropivacaine on tumor necrosis factor-alpha-induced leukocyte adhesion and tissue accumulation in vivo. Eur J Pharmacol. 2000 Mar 24;392(1-2):R1-3. | |
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