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1-α-乙酰美沙多的外周交感神经阻滞作用

Peripheral sympatholytic effects of 1-alpha-acetylmethadol.

作者信息

Stickney J L, Eikenburg D C

出版信息

J Cardiovasc Pharmacol. 1981 Mar-Apr;3(2):369-80. doi: 10.1097/00005344-198103000-00014.

DOI:10.1097/00005344-198103000-00014
PMID:6166807
Abstract

1-alpha-Acetylmethadol (LAAM), 1.4 mg/kg or greater, decreased the response of the cat nictitating membrane to pre- and postganglionic sympathetic nerve stimulation. LAAM had a greater effect on the low-frequency (0.5 Hz) than on the high-frequency (5-20 Hz) responses. No difference was observed between the effects of LAAM on the pre- as opposed to the postganglionic responses. The responses ot the nictitating membranes to intravenous epinephrine were not affected by LAAM. LAAM appears to act at the nerve terminal. The minimum dose of LAAM (1.4 mg/kg) which decreased the nictitating membrane responses also decreased blood pressure and heart rate. Naltrexone, 300 micrograms/kg, s.c., antagonized the effects of LAAM on the nictitating membrane responses and the cardiovascular actions of the drug. In anesthetized dogs, naltrexone completely blocked the blood pressure response to LAAM and partially blocked the effects of LAAM on heart rate and contractile force. The data suggest that LAAM may produce its cardiovascular effects, in part, by an action on the peripheral sympathetic nervous system which involves opiate binding sites. LAAM also appears to have direct actions on the heart to decrease heart rate and contractile force that do not involve opiate binding sites.

摘要

1-α-乙酰美沙多(LAAM),剂量为1.4毫克/千克或更高时,可降低猫瞬膜对节前和节后交感神经刺激的反应。LAAM对低频(0.5赫兹)反应的影响大于对高频(5 - 20赫兹)反应的影响。未观察到LAAM对节前反应和节后反应的影响之间存在差异。LAAM不影响瞬膜对静脉注射肾上腺素的反应。LAAM似乎作用于神经末梢。降低瞬膜反应的LAAM最小剂量(1.4毫克/千克)也会降低血压和心率。皮下注射300微克/千克的纳曲酮可拮抗LAAM对瞬膜反应和该药物心血管作用的影响。在麻醉犬中,纳曲酮完全阻断了对LAAM的血压反应,并部分阻断了LAAM对心率和收缩力的影响。数据表明,LAAM可能部分通过作用于涉及阿片类结合位点的外周交感神经系统而产生其心血管效应。LAAM似乎还对心脏有直接作用,可降低心率和收缩力,且不涉及阿片类结合位点。

相似文献

1
Peripheral sympatholytic effects of 1-alpha-acetylmethadol.1-α-乙酰美沙多的外周交感神经阻滞作用
J Cardiovasc Pharmacol. 1981 Mar-Apr;3(2):369-80. doi: 10.1097/00005344-198103000-00014.
2
l-alpha-Acetylmethadol (LAAM) attenuates sympathetic function by a peripheral mechanism.
Proc West Pharmacol Soc. 1981;24:237-9.
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Cardiac and autonomic nervous system effects of L-alphacetylmethadol (LAAM).左旋α-乙酰美沙醇(LAAM)对心脏及自主神经系统的影响。
Arch Int Pharmacodyn Ther. 1982 Oct;259(2):250-8.
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l-alpha-Acetylmethadol, l-alpha-acetyl-N-normethadol and l-alpha-acetyl-N,N-dinormethadol: comparisons with morphine and methadone in suppression of the opioid withdrawal syndrome in the dog.左旋α-乙酰美沙多、左旋α-乙酰-N-去甲美沙多和左旋α-乙酰-N,N-二去甲美沙多:与吗啡和美沙酮在抑制犬类阿片戒断综合征方面的比较。
J Pharmacol Exp Ther. 1997 Nov;283(2):833-42.
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Discriminative stimulus effects of l-alpha-acetylmethadol (LAAM), buprenorphine and methadone in morphine-treated rhesus monkeys.左旋 - α - 乙酰美沙多(LAAM)、丁丙诺啡和美沙酮在吗啡治疗的恒河猴中的辨别性刺激效应。
J Pharmacol Exp Ther. 1997 Aug;282(2):574-84.
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General cardiovascular pharmacology of 1-alpha-acetylmethadol (LAAM).1-α-乙酰美沙醇(LAAM)的一般心血管药理学
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Effects of levo-alpha-acetylmethadol (LAAM) on morphine self-administration in the rat.左旋 -α- 乙酰美沙醇(LAAM)对大鼠吗啡自我给药的影响。
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Effect of autonomic blocking agents on chronotropic actions of 1-alpha-acetylmethadol.自主神经阻滞剂对1-α-乙酰美沙多心率作用的影响。
Arch Int Pharmacodyn Ther. 1978 Jan;231(1):70-80.
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L-alphacetylmethadol (LAAM) effects on cardiac muscarinic receptors.左旋α-乙酰美沙多(LAAM)对心脏毒蕈碱受体的影响。
Arch Int Pharmacodyn Ther. 1989 Jul-Aug;300:140-8.
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Modification of drug effects by l-alpha-acetylmethadol.左旋 -α- 乙酰美沙醇对药物作用的修饰
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