kappa-Opioid activity of the four stereoisomers of the peripherally selective kappa-agonists, EMD 60,400 and EMD 61,753.
The four stereoisomers of the two peripherally selective kappa-opioid agonists EMD 60,400 and EMD 61,753 were synthesized, tested for stereoisomeric purity, and examined for affinity to the kappa opioid receptor. The relationships between the configuration of these molecules and their biological activity are discussed.
Department of Medicinal Chemistry, E. Merck, Darmstadt, Germany.
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Gottschlich
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Krug
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Barber
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Devant
D000081:Acetamides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D017473:Receptors, Opioid, kappa / Q000819:agonists* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000081:Acetamides; D011759:Pyrrolidines; D017473:Receptors, Opioid, kappa; C088120:EMD 60400; C092095:asimadoline