Pharmacological characterization of a substance P antagonist, [D-Arg1, D-Pro2, D-Trp79, Leu11]-substance P

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Abstract
1 The substance P antagonist [D-Arg1, D-Pro2, D-Trp7,9, Leu11]-substance P produced parallel log dose-response curve shifts to both substance P and eledoisin on five in vitro smooth muscle preparations. 2 The slope values of Arunlakshana-Schild plots were not significantly different from unity suggesting that it acts as a simple competitive antagonist on all five preparations with an association constant (Ka) in the range of 0.3–1.5 × 106M−1. 3 The Ka value of the antagonist was always slightly greater when tested against eledoisin than against substance P; however, this difference appears too small to suggest that these two agonists are acting on different receptor sub-types.

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