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STRUCTURE‐ACTIVITY STUDIES WITH NEUROTENSIN: ANALYSIS OF POSITIONS 9, 10 and 11
Author(s) -
QUIRION R.,
REGOLI D.,
RIOUX F.,
STPIERRE S.
Publication year - 1980
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.1476-5381.1980.tb07923.x
Subject(s) - neurotensin , receptor , potency , neurotensin receptor , biology , guinea pig , hypothermia , neuropeptide , medicine , endocrinology , chemistry , pharmacology , biochemistry , in vitro
1 The stimulant effects of neurotensin (NT) and NT analogues modified in positions 9, 10 or 11 were evaluated and compared in two pharmacological preparations: the rat stomach strip and the isolated spontaneously beating atria of guinea‐pig. 2 The data derived from our structure‐activity study suggest that Arg 9 and Pro 10 mainly contribute to the affinity of neurotensin for its cardiac and smooth muscle receptors. Tyr 11 seems to be more closely involved in the process of receptor activation by NT. 3 The order of potency of some NT analogues modified in position 11 (e.g. [ d ‐Phe 11 ]‐NT, [ d ‐Tyr 11 ]‐NT) was strikingly different from that described in other systems (e.g. hypothermia test and specific mast cell binding). The importance of this observation is discussed.