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Pharmacological characterization of a substance P antagonist, [D‐Arg 1 , D‐Pro 2 , D‐Trp 7 9 , Leu 11 ]‐substance P
Author(s) -
Watson Stephen P.
Publication year - 1983
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1983.tb11067.x
Subject(s) - chemistry , radiochemistry
1 The substance P antagonist [D‐Arg 1 , D‐Pro 2 , D‐Trp 7,9 , Leu 11 ]‐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 ( K a ) in the range of 0.3–1.5 × 10 6 M −1 . 3 The K a 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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