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  • Title: [Preferential action of eptazocine, a novel analgesic, with opioid receptors in isolated guinea pig ileum and mouse vas deferens preparations].
    Author: Tamura T, Ogawa J, Taniguchi T, Waki I.
    Journal: Nihon Yakurigaku Zasshi; 1990 Jan; 95(1):41-6. PubMed ID: 2154395.
    Abstract:
    Actions of eptazocine, a novel analgesic, on isolated smooth muscle preparations were investigated. Eptazocine (10(-5) M) slightly inhibited electrically-driven twitch-tension in guinea pig ileum preparations sensitive to mu- and kappa-agonists, and this effect was antagonized by 10(-7) M naloxone. Eptazocine (10(-5)-10(-4) M) inhibited such an effect by the mu-agonist morphine. In mouse vas deferens preparations having delta-, mu- and kappa-receptors, eptazocine (10(-7) M-) inhibited the twitch-tension in a dose-dependent manner, being hardly inhibited by naloxone. On the other hand, MR-2266 (10(-6) M), a relatively selective kappa-receptor antagonist, inhibited the eptazocine effect. The Ke (equilibrium dissociation constant) value of naloxone against eptazocine was 325 nM and the Ke value of MR-2266 against eptazocine was 33.2 nM, showing that MR-2266 was 9.79-fold more effective than naloxone. These results suggest that eptazocine acted as a mu-receptor antagonist and as a kappa-receptor preferential agonist in isolated smooth muscle preparations.
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