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首页> 外文期刊>Life sciences >Inhibitory effects of opioids on compound action potentials in frog sciatic nerves and their chemical structures.
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Inhibitory effects of opioids on compound action potentials in frog sciatic nerves and their chemical structures.

机译：阿片类药物对青蛙坐骨神经及其化学结构的复合动作电位的抑制作用。

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An opioid tramadol more effectively inhibits compound action potentials (CAPs) than its metabolite mono-O-demethyl-tramadol (M1). To address further this issue, we examined the effects of opioids (morphine, codeine, ethylmorphine and dihydrocodeine) and cocaine on CAPs by applying the air-gap method to the frog sciatic nerve. All of the opioids at concentrations less than 10 mM reduced the peak amplitude of the CAP in a reversible and dose-dependent manner. The sequence of the CAP peak amplitude reductions was ethylmorphine>codeine>dihydrocodeine> or = morphine; the effective concentration for half-maximal inhibition (IC(50)) of ethylmorphine was 4.6 mM. All of the CAP inhibitions by opioids were resistant to a non-specific opioid-receptor antagonist naloxone. The CAP peak amplitude reductions produced by morphine, codeine and ethylmorphine were related to their chemical structures in such that this extent enhanced with an increase in the number of -CH(2) in a benzene ring, as seen in the inhibitory actions of tramadol and M1. Cocaine reduced CAP peak amplitudes with an IC(50) value of 0.80 mM. It is concluded that opioids reduce CAP peak amplitudes in a manner being independent of opioid-receptor activation and with an efficacy being much less than that of cocaine. It is suggested that the substituted groups of -OH bound to the benzene ring of morphine, codeine and ethylmorphine as well as of tramadol and M1, the structures of which are quite different from those of the opioids, may play an important role in producing nerve conduction block.
机译：阿片类曲马多比其代谢产物单-O-去甲基-曲马多（M1）更有效地抑制复合作用电位（CAPs）。为了进一步解决这个问题，我们通过将气隙方法应用于青蛙坐骨神经，研究了阿片类药物（吗啡，可待因，乙基吗啡和二氢可待因）和可卡因对CAP的影响。所有浓度低于10 mM的阿片类药物均以可逆和剂量依赖的方式降低了CAP的峰值幅度。 CAP峰幅度降低的顺序为乙基吗啡>可待因>二氢可待因>或=吗啡;乙吗啡的半数最大抑制有效浓度（IC（50））为4.6 mM。阿片类药物对CAP的所有抑制作用均对非特异性阿片受体拮抗剂纳洛酮有抵抗力。由吗啡，可待因和乙基吗啡产生的CAP峰幅度降低与它们的化学结构有关，这样的程度随苯环中-CH（2）数量的增加而增强，如曲马多和M1。可卡因降低了CAP峰幅度，IC（50）值为0.80 mM。结论是，阿片类药物以与阿片类药物受体活化无关的方式降低CAP峰幅度，且功效远低于可卡因。建议与吗啡，可待因和乙基吗啡的苯环以及曲马多和M1的苯环结合的-OH取代基的结构与阿片类药物的结构有很大不同，这可能在神经产生中起重要作用。传导阻滞。

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