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SPINAL ANTINOCICEPTION BY TYR-D-SER(OTBU)-GLY-PHE-LEU-THR, A SELECTIVE DELTA-OPIOID RECEPTOR AGONIST

KALSO, EA; SULLIVAN, AF; MCQUAY, HJ; DICKENSON, AH; (1992) SPINAL ANTINOCICEPTION BY TYR-D-SER(OTBU)-GLY-PHE-LEU-THR, A SELECTIVE DELTA-OPIOID RECEPTOR AGONIST. EUR J PHARMACOL , 216 (1) 97 - 101.

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Abstract

The spinal antinociceptive potency of the delta-opioid receptor agonist, Tyr-D-Ser(otbu)-Gly-Phe-Leu-Thr (DSTBULET), was studied in rats. The tail flick test was used as nociceptive stimulus and the rotarod test was used to detect any motor or sedative effects. A dose-response curve was also made for the mu-opioid receptor agonist, morphine. The ED50) for DSTBULET was 0.3-mu-g (0.4 nmol) and a near 100% maximum effect was achieved with 5-mu-g (7.5 nmol). No motor or sedative effects were detected. Antinociception by DSTBULET was antagonized by s.c. naltrindole (I mg/kg), a selective delta-opioid receptor antagonist, and naloxone (1 mg/kg), a non-selective opioid receptor antagonist. The ED50 for morphine was 0.5-mu-g (1.0 nmol) and the antinociceptive effects were not antagonized by naltrindole (1 mg/kg). The results evidence further the important role of the delta-opioid receptor in spinal nociceptive processing.

Type: Article
Title: SPINAL ANTINOCICEPTION BY TYR-D-SER(OTBU)-GLY-PHE-LEU-THR, A SELECTIVE DELTA-OPIOID RECEPTOR AGONIST
Keywords: ANTINOCICEPTION, TAIL-FLICK (SPINAL), DELTA-OPIOID RECEPTORS, DSTBULET (TYR-D-SER(OTBU)-GLY-PHE-LEU-THR), MORPHINE, SYSTEMS MEDIATING ANTINOCICEPTION, RAT DORSAL HORN, OPIATE RECEPTORS, INVIVO EVIDENCE, BINDING SITES, MU-RECEPTOR, CORD, ANALGESIA, MORPHINE, MOUSE
UCL classification: UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences > Neuro, Physiology and Pharmacology
URI: http://discovery.ucl.ac.uk/id/eprint/132481
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