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Structure‐antinociceptive activity studies with neurotensin
Author(s) -
Furuta Seiichi,
Kisara Kensuke,
Sakurada Shinobu,
Sakurada Tsukasa,
Sasaki Yusuke,
Suzuki Kenji
Publication year - 1984
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.1476-5381.1984.tb10117.x
Subject(s) - neurotensin , nociception , (+) naloxone , pharmacology , chemistry , potency , opioid , antagonist , neuropeptide , endocrinology , medicine , receptor , in vitro , biochemistry
1 The antinociceptive effects of synthetic neurotensin (NT), its fragments and analogues administered into the lateral cerebroventricle have been compared in the conscious mouse. 2 Intracerebroventricular (i.c.v.) administration of NT produced a dose‐dependent antinociceptive effect in the tail pressure test. 3 The NT fragments and analogues, NT(8–13), NT(8–10), NT(9–13), NT(9–11), NT(8–11) NHEt and NT(9–11) NHEt were also effective antinociceptive peptides. 4 The potency of NT(8–13) and the duration of its effects were found to be approximately equal to those of NT. 5 The antinociceptive effects produced by NT, NT(8–13) and NT(9–13) were significantly reversed by the opioid antagonist naloxone but not by thyrotropin releasing hormone. 6 It is concluded that NT(8–13) is required for the full expression of the antinociceptive effects of NT which may be mediated in part through the brain opioid system.