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  • Title: Involvement of spinal mu1-opioid receptors on the Tyr-d-Arg-Phe-sarcosine-induced antinociception.
    Author: Mizoguchi H, Nakayama D, Watanabe H, Ito K, Sakurada W, Sawai T, Fujimura T, Sato T, Sakurada T, Sakurada S.
    Journal: Eur J Pharmacol; 2006 Jul 01; 540(1-3):67-72. PubMed ID: 16730704.
    Abstract:
    The involvement of spinal mu-opioid receptor subtypes on the antinociception induced by i.t.-administered Tyr-D-Arg-Phe-sarcosine (TAPS), a N-terminal tetrapeptide analog of dermorphin, was determined in mice tail-flick test. Intrathecal administration of TAPS produced the marked inhibition of the tail-flick response in a dose-dependent manner. The antinociception induced by TAPS was completely eliminated by i.t.-co-administration of Tyr-D-Pro-Phe-Phe-NH2 (D-Pro2-endomorphin-2), the mu1-opioid receptor antagonist, whereas i.t. co-treatment with Tyr-D-Pro-Trp-Phe-NH2 (D-Pro2-endomorphin-1) or Tyr-D-Pro-Trp-Gly-NH2 (D-Pro2-Tyr-W-MIF-1), the mu2-opioid receptor antagonists, did not affect the TAPS-induced antinociception. In contrast, the antinociception induced by i.t.-administered [D-Ala2,N-MePhe4,Gly-ol5]enkephalin was significantly attenuated by i.t.-co-administration of D-Pro2-endomorphin-1 or D-Pro2-Tyr-W-MIF-1, but not D-Pro2-endomorphin-2. These results suggest that TAPS may stimulate spinal mu1-opioid receptors to produce the antinociception.
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