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  • Title: [Comparison of pharmacological profile of selective kappa-opioid agonist K-II and U-50488].
    Author: Lu SN, Ma SC, Zhang KG, Dong YX, Cui YY, Li JG, Wang CQ.
    Journal: Yao Xue Xue Bao; 1991; 26(3):171-4. PubMed ID: 1957656.
    Abstract:
    K-II is an analogue of U-50488, a selective kappa-opioid agonist. Comparison of pharmacological profile of K-II and U-50488 was studied using in vitro and in vivo methods. The results showed that the IC50 values of K-II and U-50488 on electrically induced contraction of the rabbit vas deferens were 0.42 nmol/L and 26.5 nmol/L, respectively. ED50 values of K-II and U-50488 in impairing motor function of mouse in the horizontal screen test were 1.7 and 15.3 mg/kg, respectively. The effect of K-II in reducing spontaneous activity of mouse was 6 times as potent as U-50488. These results suggest that K-II is a more potent kappa agonist in pharmacological effects than U-50488.
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