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A highly selective nonpeptidic δ opioid receptor agonist TAN-67, (4aS*, 12aR*)-4a-(3-hydroxyphenyl)-2-methyl-1,2,3,4,4a,5,12,12a-octahydropyrido[3,4-b]acridine was designed on the basis of the message-address concept and the accessory site theory. (−)-TAN-67 is a potent and selective δ1 opioid receptor agonist and shows strong antinociceptive, cardioprotective, and...
We designed the nonpeptidic highly selective δ opioid receptor agonist on the basis of message address concept and the accessory site theory and synthesized (+/-) TAN-67. In spite of highly potent agonistic activity in in vitro assay, (+/-) TAN-67 (racemate) afforded a weak antinociceptive effect in the mouse tail-flick test. This result led us to separate (+/-) TAN-67 to optical pure compounds, (+)...
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