Clement J G
Can J Physiol Pharmacol. 1980 Mar;58(3):265-70. doi: 10.1139/y80-045.
It has been noted that the analgesic property of ethanol bears a marked resemblance to that of morphine. The purpose of this study was to determine if the mechanism of action of morphine and ethanol was similar using the guinea pig ileal longitudinal muscle strip (GPI-LMS). Ethanol (35-260 mM) depressed the twitch response and the acetylcholine- (ACh-), KCl-, and BaCl2-induced contractions to the same extent while having no significant effect on the binding of [3H]quinuclidinyl benzilate ([3H]QNB) to muscarinic receptors. Morphine (53-530 nM) inhibited the twitch response and to a lesser extent BaCl2- and KCl-induced contractions while having no significant effect on either ACh-induced contractions or the binding of [3H]QNB to muscarinic receptors. Naloxone and increased [Ca2+] reversed the inhibitory effects of morphine but not ethanol. Ethanol appears to inhibit a site after interaction of ACh with the receptor. Mechanism of inhibition of BaCl2 response is also different as naloxone and increased [Ca2+] reverse morphine but not ethanol inhibition Ethanol inhibition in GPI-LMS does not involve the opiate receptor.
已经注意到乙醇的镇痛特性与吗啡的镇痛特性有显著相似之处。本研究的目的是使用豚鼠回肠纵肌条(GPI-LMS)来确定吗啡和乙醇的作用机制是否相似。乙醇(35 - 260 mM)同等程度地抑制抽搐反应以及乙酰胆碱(ACh)、氯化钾(KCl)和氯化钡(BaCl₂)诱导的收缩,而对[³H]喹核醇基苯甲酸酯([³H]QNB)与毒蕈碱受体的结合没有显著影响。吗啡(53 - 530 nM)抑制抽搐反应,并在较小程度上抑制BaCl₂和KCl诱导的收缩,而对ACh诱导的收缩或[³H]QNB与毒蕈碱受体的结合均无显著影响。纳洛酮和增加的[Ca²⁺]可逆转吗啡的抑制作用,但不能逆转乙醇的抑制作用。乙醇似乎在ACh与受体相互作用后抑制一个位点。BaCl₂反应的抑制机制也不同,因为纳洛酮和增加的[Ca²⁺]可逆转吗啡的抑制作用,但不能逆转乙醇的抑制作用。GPI-LMS中乙醇的抑制作用不涉及阿片受体。