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- W2315690076 abstract "The synthesis of a new series of nonpeptide derivatives of interleukin-l β sequence is described. Compounds have been investigated for their relative activity regarding antinociception and suppression of inflammation. Several compounds with R<sub>1</sub>(R)Lys [CH<sub>2</sub> N]-Pro structure showed better efficacy in the inflamed paw pressure test than indometacin and morphine. In terms of the relative potencies the above mentioned products (i.e. compounds <b>2, 4, 5, 6;</b> ED<sub>50</sub> values of 0.002, 0.0035, 0.0032, 0.0074 mg/kg i.p. respectively) were 10-100 times more potent than indometacin and morphine (ED<sub>50</sub> values of 0.22 and 0.75 mg/kg). Compounds <b>1–14</b> were not able to inhibit binding of labeled interleukin-l β to EL 4-6.1 murine cells, since they had no affinity for interleukin-l β receptors. The antinociceptive activity elicited by compound <b>4</b> in the rat inflamed paw pressure test was inhibited by naloxone, but the compound was inactive in the mouse hot plate and rat paw pressure tests. These results suggest that compound <b>4</b> exerts its antinociceptive activity through a mechanism which is based on the local release of endogenous opioids in injured tissue." @default.
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- W2315690076 date "2011-12-28" @default.
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- W2315690076 title "Synthesis and Antinociceptive Activity of Some Novel Nonpeptide Derivatives of interleukin-1β (193–195) Sequence" @default.
- W2315690076 doi "https://doi.org/10.1055/s-0031-1300374" @default.
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