ACTIONS OF ETORPHINE HYDROCHLORIDE (M99) - A POTENT MORPHINE LIKE AGENT
ACTIONS OF ETORPHINE HYDROCHLORIDE (M99) - A POTENT MORPHINE LIKE AGENT
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DOI：
10.1111/j.1476-5381.1967.tb02108.x
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发表时间：
1967-01-01
期刊：
影响因子：
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通讯作者：
LISTER, RE
中科院分区：
文献类型：
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作者：
BLANE, GF;BOURA, ALA;LISTER, RE
研究了埃托啡（Propylorvinol; M99，7a-（1-（R）-羟基-1-甲基丁基）-6，14-endoethenotetrahydro-oripavine，一种强吗啡样剂）的作用，并与吗啡进行了比较。剪下，根据测试情况，埃托啡的效力是吗啡的1000- 80，000倍。在啮齿类动物、猫、狗和猴中，埃托啡与吗啡相似，可引起镇痛、紧张症、条件反射阻滞、呼吸抑制、胃肠推进减少和抗利尿作用。它也类似于吗啡，引起小鼠和猫的兴奋，以及大鼠，狗，猫和猴子的心动过缓和低血压。埃托啡抑制中枢神经系统的低级中枢的程度大于吗啡。这种药物在大鼠、豚鼠和兔子身上引起了更大的呼吸抑制。它更容易阻断大鼠的条件反射，并在大鼠和豚鼠中引起更大程度的紧张症。低剂量的埃托啡不能引起狗的兴奋和呕吐。纳洛啡和强效吗啡拮抗剂M285 [N-环丙基-甲基-7a-（1-羟基-1-甲基乙基）-6，14-1内乙烯基四氢-去甲东罂粟碱]满足埃托啡竞争性拮抗作用的常规标准。
The effects of etorphine (Propylorvinol; M99, 7a-(l-(R)-hydroxy-l-methylbutyl)-6,14-endoethenotetrahydro-oripavine, a powerful morphine-like agent, were investigated and compared with morphine. Subcut., etorphine was 1000-80,000 times more potent than morphine depending on the test situation. Etorphine resembled morphine in rodents, cats, dogs and monkeys by causing analgesia, catatonia, blockade of conditioned reflexes, respiratory depression, reduction of gastro-intestinal propulsion and an anti-diuretic effect. It also resembled morphine by causing excitement in mice and cats, and bradycardia and hypotension in rats, dogs, cats and monkeys. Etorphine depressed the lower centers of the central nervous system to a greater extent than morphine. The drug caused greater respiratory depression in rats, guinea-pigs and rabbits. It blocked more readily conditioned reflexes in the rat and caused a greater degree of catatonia in the rat and guinea-pig. Low doses of etorphine failed tq cause excitement and emesis in the dog. Nalorphine and the potent morphine antagonist M285 [N-cyclopropyl-methyl-7a-(l-hydroxy-l-methylethyl)-6,14-1 endoethenotetrahydro-nororipavine] fulfilled conventional criteria for competitive antagonism of etorphine.