A. Shafiee , M. Amanlou , H. Farsam , A.R. Dehpour , F. Mir-Ershadi , A.R. Mani
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引用次数: 9
摘要
通过底贝恩与n -芳基马来酰亚胺的反应合成了底贝恩衍生的μ-阿片激动剂，并对其进行了阿片活性测试。以吗啡为对照物。我们的研究结果表明，芳基琥珀酰亚胺基团与苯胺的结合产生了一系列具有μ-阿片激动剂活性的化合物。平滑肌制剂中活性最高的化合物为化合物6,IC50值为δ/μ=248.69，热板试验ED50值为26.65 mg kg - 1 i.p.，与吗啡药效相当，具有良好的抗伤感受活性。
Synthesis and pharmacological activity of thebaine-derived μ-opioid receptor agonists
Thebaine-derived μ-opioid agonists were synthesized through the reaction of thebaine with N-aryl maleimide and tested for opioid activity. Morphine was used as reference compound. Our results show that an attachment of aryl succinimide group to thebaine produced series of compounds with μ-opioid agonist activity. The most active compound in smooth muscle preparation was compound 6 with an IC50 ratio of δ/μ=248.69 and was as potent as morphine with ED50 value 26.65 mg kg−1 i.p. in hot-plate test and showed good antinociceptive activity.
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