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Contribution of spinal m1-opioid receptors and dynorphin B to the antinociception induced by Tyr-D-Arg-Phe-Sar

All Rights Reserved. Contribution of spinal m1-opioid receptors and dynorphin B to the antinociception induced by Tyr-D-Arg-Phe-Sar. Mizoguchi, Hirokazu; Ito, Kanenori; Watanabe, Hiroyuki; Watanabe, Chizuko; Katsuyama, Sou; Fujimura, Tsutomu; Sakurada, Tsukasa; Sakurada, Shinobu (Department of Physiology and Anatomy, Tohoku Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, Japan). Peptides (New York, NY, United States), 27(11), 2786-2793 (English) 2006 Elsevier Inc. CODEN: PPTDD5. ISSN: 0196-9781. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The antinociceptive effect of Tyr-D-Arg-Phe-Sar (TAPS) at the spinal level was characterized with the mouse tail-flick test. Intrathecal (i.t. 90549-86-3 and 85006-82-2 which are cas registry numbers are also used here.) administration of TAPS produced a dose-dependent antinociception. The antinociception induced by TAPS was completely blocked by i.t. pretreatment with the m-opioid receptor antagonist b-funaltrexamine, the m1-opioid receptor antagonist naloxonazine or the k-opioid receptor antagonist nor-binaltorphimine, but not with the d-opioid receptor antagonist naltrindole. Moreover, TAPS-induced antinociception was dose-dependently attenuated by i.t. pretreatment with an antiserum against dynorphin B, but not against dynorphin A, a-neo-endorphin, [Met5]enkephalin, or [Leu5]enkephalin. In mice lacking prodynorphin, TAPS-induced antinociception was significantly reduced compared to that in wild-type mice. These results suggest that TAPS mainly stimulates m1-opioid receptors, which subsequently induce the release of dynorphin B, which then acts on k-opioid receptors to produce antinociception. .