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混合激动剂-拮抗剂镇痛药的动物及分子药理学

Animal and molecular pharmacology of mixed agonist-antagonist analgesic drugs.

作者信息

Rance M J

出版信息

Br J Clin Pharmacol. 1979;7 Suppl 3(Suppl 3):281S-286S. doi: 10.1111/j.1365-2125.1979.tb04701.x.

DOI:10.1111/j.1365-2125.1979.tb04701.x
PMID:223616
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1429313/
Abstract

1 The pharmacology of analgesic drugs with mixed agonist-antagonist action is reviewed in the light of the theory of drug action at single and multiple receptors. 2 Evidence for a heterogeneous population of opiate receptors in mammalian brain and in isolated tissue preparations is discussed. 3 The unusual pharmacological and pharmacokinetic profiles of the oripavine derivative buprenorphine are discussed in relation to the action of the drug at a molecular level.

摘要
  1. 根据药物在单一和多个受体上的作用理论，对具有混合激动 - 拮抗作用的镇痛药的药理学进行综述。2. 讨论了哺乳动物脑和离体组织制剂中阿片受体异质群体的证据。3. 结合丁丙诺啡在分子水平上的作用，讨论了阿片碱衍生物丁丙诺啡不同寻常的药理学和药代动力学特征。

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1
Animal and molecular pharmacology of mixed agonist-antagonist analgesic drugs.混合激动剂-拮抗剂镇痛药的动物及分子药理学
Br J Clin Pharmacol. 1979;7 Suppl 3(Suppl 3):281S-286S. doi: 10.1111/j.1365-2125.1979.tb04701.x.
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Opiate receptor pharmacology: mixed agonist/antagonist narcotics.阿片受体药理学：混合激动剂/拮抗剂类麻醉药
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Simple in vivo tests that differentiate prototype agonists at opiate receptors.区分阿片受体原型激动剂的简单体内试验。
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History and development of mixed opioid agonists, partial agonists and antagonists.混合阿片类激动剂、部分激动剂和拮抗剂的历史与发展
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HS-599: a novel long acting opioid analgesic does not induce place-preference in rats.HS-599：一种新型长效阿片类镇痛药不会在大鼠中诱发位置偏爱。
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Quantum chemical studies of molecular features and receptor interactions that modulate opiate agonist and antagonist activity.调节阿片类激动剂和拮抗剂活性的分子特征及受体相互作用的量子化学研究。
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Some pharmacological properties of a newly synthesized 3-acetoxy-6 beta-acetylthio-10-oxo-N-cyclopropylmethyl-dihydronormorphine (KT-95).一种新合成的3-乙酰氧基-6β-乙酰硫基-10-氧代-N-环丙基甲基-二氢去甲吗啡（KT-95）的一些药理学特性
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Drug discrimination in human post-addicts: agonist/antagonist opioids.
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In vivo and in vitro investigation of naltrindole, a delta-opioid antagonist.
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引用本文的文献

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Behavioral Effects of Opioid Full and Partial Agonists During Chronic Buprenorphine Treatment.阿片类药物完全激动剂和部分激动剂在慢性丁丙诺啡治疗期间的行为效应。
J Pharmacol Exp Ther. 2019 Nov;371(2):544-554. doi: 10.1124/jpet.119.259010. Epub 2019 Aug 14.
2
The effects of maternally administered methadone, buprenorphine and naltrexone on offspring: review of human and animal data.美沙酮、丁丙诺啡和纳曲酮对母婴的影响：人类和动物数据综述。
Curr Neuropharmacol. 2008 Jun;6(2):125-50. doi: 10.2174/157015908784533842.
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Buprenorphine: a unique drug with complex pharmacology.丁丙诺啡：一种具有复杂药理学的独特药物。
Curr Neuropharmacol. 2004 Oct;2(4):395-402. doi: 10.2174/1570159043359477.
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Pharmacokinetic and pharmacodynamic principles of illicit drug use and treatment of illicit drug users.非法药物使用的药代动力学和药效学原理以及非法药物使用者的治疗
Clin Pharmacokinet. 1997 Nov;33(5):344-400. doi: 10.2165/00003088-199733050-00003.
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Propiram. A review of its pharmacodynamic and pharmacokinetic properties, and clinical use as an analgesic.丙哌卡因。对其药效学和药代动力学特性以及作为镇痛药的临床应用的综述。
Drugs. 1993 Sep;46(3):428-445. doi: 10.2165/00003495-199346030-00008.
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Differential effects of opiate agonists-antagonists on morphine-induced hyperexcitability and analgesia in mice.阿片类激动剂-拮抗剂对小鼠吗啡诱导的过度兴奋和镇痛的不同作用。
Psychopharmacology (Berl). 1981;73(2):134-6. doi: 10.1007/BF00429203.
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Stimulation of avoidance behavior by buprenorphine in rats.
Psychopharmacology (Berl). 1983;80(1):19-23. doi: 10.1007/BF00427487.
8
Reversal by beta-funaltrexamine of the antinociceptive effect of opioid agonists in the rat.β-芬基曲马胺对大鼠阿片类激动剂镇痛作用的逆转作用
Br J Pharmacol. 1986 Aug;88(4):867-72. doi: 10.1111/j.1476-5381.1986.tb16260.x.
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Opioid agonist-antagonist drugs in acute and chronic pain states.阿片类激动剂-拮抗剂药物在急慢性疼痛状态中的应用。
Drugs. 1991 Mar;41(3):326-44. doi: 10.2165/00003495-199141030-00002.
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Mixed agonist-antagonist opiates and physical dependence.混合激动剂-拮抗剂阿片类药物与身体依赖性
Br J Clin Pharmacol. 1979;7 Suppl 3(Suppl 3):291S-296S. doi: 10.1111/j.1365-2125.1979.tb04703.x.

本文引用的文献

1
A comparison of heat and pressure analgesiometric methods in rats.大鼠热和压力镇痛测量方法的比较。
Br J Pharmacol Chemother. 1951 Dec;6(4):572-85. doi: 10.1111/j.1476-5381.1951.tb00668.x.
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Analgesimetry and ranking of analgesic drugs by the receptacle method.
Arch Int Pharmacodyn Ther. 1959 Nov 1;122:434-47.
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Antagonism of the frequency of phenylquinone-induced writhing in the mouse by weak analgesics and nonanalgesics.弱镇痛药和非镇痛药对苯醌诱发小鼠扭体反应频率的拮抗作用。
J Pharmacol Exp Ther. 1959 Mar;125(3):237-40.
4
The analgesic effectiveness of nalorphine and nalorphine-morphine combinations in man.烯丙吗啡及烯丙吗啡 - 吗啡组合对人体的镇痛效果。
J Pharmacol Exp Ther. 1954 Nov;112(3):356-63.
5
Agonist and antagonist actions of morphine-like drugs on the guinea-pig isolated ileum.吗啡样药物对豚鼠离体回肠的激动剂和拮抗剂作用。
Br J Pharmacol Chemother. 1966 Sep;27(3):514-27. doi: 10.1111/j.1476-5381.1966.tb01864.x.
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Opioid antagonists.阿片类拮抗剂。
Pharmacol Rev. 1967 Dec;19(4):463-521.
7
Stereospecific interaction between narcotic analgesics and a synaptic plasm a membrane fraction of rat cerebral cortex.麻醉性镇痛药与大鼠大脑皮质突触质膜部分之间的立体特异性相互作用。
Acta Pharmacol Toxicol (Copenh). 1973;32(3):317-20. doi: 10.1111/j.1600-0773.1973.tb01477.x.
8
Opiate receptor: demonstration in nervous tissue.阿片受体：在神经组织中的显示
Science. 1973 Mar 9;179(4077):1011-4. doi: 10.1126/science.179.4077.1011.
9
A new example of a morphine-sensitive neuro-effector junction: adrenergic transmission in the mouse vas deferens.吗啡敏感型神经效应器连接的一个新实例：小鼠输精管中的肾上腺素能传递。
Br J Pharmacol. 1972 Dec;46(4):764-6. doi: 10.1111/j.1476-5381.1972.tb06901.x.
10
Stereospecific binding of the potent narcotic analgesic (3H) Etorphine to rat-brain homogenate.强效麻醉性镇痛药（3H）埃托啡与大鼠脑匀浆的立体特异性结合。
Proc Natl Acad Sci U S A. 1973 Jul;70(7):1947-9. doi: 10.1073/pnas.70.7.1947.