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In investigating the development of compounds with potent analgesic effects after oral administration, 74 C-terminal analogues (N(alpha)-amidino-Tyr-D-Arg-Phe-X), based on the structure of N(alpha)-amidino-Tyr-D-Arg-Phe-Me beta Ala-OH (ADAMB), were synthesized. Their analgesic activity was evaluated using the mouse-tail pressure test after both subcutaneous and oral administration, and the structure-activity relationships (SAR) were examined in detail. The results clearly indicated that compounds containing beta-amino acid without a side chain at the X position are preferable for expression of potent analgesic activity, and that the free carboxyl group is superior in its analgesic activity to that of the esterified or amidated carboxy group at the C-terminal. In addition, N-methylation of the amide bond at the 4th position contributed to improved analgesic activity. These results indicated that the strong and long-lasting analgesic effect of ADAMB is expressed by the synergistic effects of N(alpha)-amidination, the N-methylation of the amide bond at the 4th position and the carbon chain length (beta-Ala) of the residue at the 4th position, and that this is the most suitable structure.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Structure&amp;ndash;Activity Relationships (SAR) of [&lt;small&gt;D&lt;/small&gt;-Arg&lt;sup&gt;2&lt;/sup&gt;]Dermorphin(1&amp;mdash;4) Analogues, &lt;i&gt;N&lt;sup&gt;&amp;alpha;&lt;/sup&gt;&lt;/i&gt;-Amidino-Tyr-&lt;small&gt;D&lt;/small&gt;-Arg-Phe-X