Karl-August Ackermann

EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists

Abstract K opiate agonists like (−)-U 50488H, (−)-PD 117302, etc. contain an acetamido group which is mono substituted in the α-position by an aromatic moiety. In contrast, EMD 61 753 is di substituted in this position by two phenyl rings and is thus the first representative of the new class of diarylacetamide-type κ opiates. Derivatives of EMD 61 753 are described and structure-activity relationships are discussed. In the formalin test in mice EMD 61 753 shows a profile similar to that of the antiinflammatory drugs rather than that of the centrally acting opiates.