Nor-binaltorphimine (nor-BNI) k receptor antagonist

Figure 24.5 • Selective K-receptor ligands.

in some situations.50 The carboxy-terminal half of the receptor may serve as the portion that excludes binding to the ¡¿-, 8-, and K-opioid ligands. The functional role of the receptor is still being investigated, but selective agonists have been shown to delay gastric emptying and decrease gastric secretory functions in rats.51 In addition, this receptor is found on airway nerves, and agonists decrease bronchospasms in guinea pigs and cats. This receptor is a target for the design of novel peripherally acting antitussive agents, although no compounds are on the market at present.

receptors to multiple chemical backbones and tolerance for divergent functional groups. The reader is referred to reviews of the k- and 8-receptor for detailed SARs for ligands at those receptors.41 A summary review of the SARs of the ^-receptor compounds is included in the drug monograph section below. For the purpose of this chapter, the drug classes covered will be 4,5-epoxymorphinans, morphinans, benzomorphans, 4-phenylpiperidines/4-anilidopiperidines, diphenylheptanes, and the miscellaneous category.

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