A. Shafiee , M. Amanlou , H. Farsam , A.R. Dehpour , F. Mir-Ershadi , A.R. Mani
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引用次数: 9
Abstract
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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