U-50,488 and the к receptor: A personalized account covering the period 1973 to 1990

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Abstract
All clinically significant analgesics for severe pain derive from the morphine model. Morphine has provided a fertile area for medicinal chemistry research and received an additional stimulus in the 1970s with the appearance of the Opioid receptors. The background for the birth of U-50,488 is described herein. It occurred before the discovery of the K receptor and, thus, U-50,488 was classified originally as a non-μ compound, and only later as a K agonist. U-50,488 provided a succinct template for structural modifications and they are described for the period up to 1990. A description of the structural classes of K agonists is provided including a summary of K recognition sites based on known agonists.