<?xml version="1.0" encoding="UTF-8"?><xml><records><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Fichna,J.</style></author><author><style face="normal" font="default" size="100%">do-Rego,J.C.</style></author><author><style face="normal" font="default" size="100%">Chung,N.N.</style></author><author><style face="normal" font="default" size="100%">Lemieux,C.</style></author><author><style face="normal" font="default" size="100%">Schiller,P.W.</style></author><author><style face="normal" font="default" size="100%">J Poels</style></author><author><style face="normal" font="default" size="100%">J. Vanden Broeck</style></author><author><style face="normal" font="default" size="100%">Costentin,J.</style></author><author><style face="normal" font="default" size="100%">A.E. Janecka</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2)4395</style></title><secondary-title><style face="normal" font="default" size="100%">J.Med.Chem.</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">0</style></keyword><keyword><style  face="normal" font="default" size="100%">a</style></keyword><keyword><style  face="normal" font="default" size="100%">Aequorin</style></keyword><keyword><style  face="normal" font="default" size="100%">Agent</style></keyword><keyword><style  face="normal" font="default" size="100%">Agents</style></keyword><keyword><style  face="normal" font="default" size="100%">agonists</style></keyword><keyword><style  face="normal" font="default" size="100%">Analgesics</style></keyword><keyword><style  face="normal" font="default" size="100%">Animals</style></keyword><keyword><style  face="normal" font="default" size="100%">antagonists &amp; inhibitors</style></keyword><keyword><style  face="normal" font="default" size="100%">article</style></keyword><keyword><style  face="normal" font="default" size="100%">AS</style></keyword><keyword><style  face="normal" font="default" size="100%">Binding Sites</style></keyword><keyword><style  face="normal" font="default" size="100%">brain</style></keyword><keyword><style  face="normal" font="default" size="100%">Calcium</style></keyword><keyword><style  face="normal" font="default" size="100%">chemical synthesis</style></keyword><keyword><style  face="normal" font="default" size="100%">chemistry</style></keyword><keyword><style  face="normal" font="default" size="100%">Cho Cells</style></keyword><keyword><style  face="normal" font="default" size="100%">Cricetinae</style></keyword><keyword><style  face="normal" font="default" size="100%">Cricetulus</style></keyword><keyword><style  face="normal" font="default" size="100%">drug effects</style></keyword><keyword><style  face="normal" font="default" size="100%">Functional</style></keyword><keyword><style  face="normal" font="default" size="100%">Guinea Pigs</style></keyword><keyword><style  face="normal" font="default" size="100%">Ileum</style></keyword><keyword><style  face="normal" font="default" size="100%">im</style></keyword><keyword><style  face="normal" font="default" size="100%">Institute</style></keyword><keyword><style  face="normal" font="default" size="100%">IS</style></keyword><keyword><style  face="normal" font="default" size="100%">journal</style></keyword><keyword><style  face="normal" font="default" size="100%">Laboratories</style></keyword><keyword><style  face="normal" font="default" size="100%">Luminescent Agents</style></keyword><keyword><style  face="normal" font="default" size="100%">Male</style></keyword><keyword><style  face="normal" font="default" size="100%">medical</style></keyword><keyword><style  face="normal" font="default" size="100%">metabolism</style></keyword><keyword><style  face="normal" font="default" size="100%">mice</style></keyword><keyword><style  face="normal" font="default" size="100%">Muscle Contraction</style></keyword><keyword><style  face="normal" font="default" size="100%">Muscle,Smooth</style></keyword><keyword><style  face="normal" font="default" size="100%">Oligopeptides</style></keyword><keyword><style  face="normal" font="default" size="100%">ON</style></keyword><keyword><style  face="normal" font="default" size="100%">pharmacology</style></keyword><keyword><style  face="normal" font="default" size="100%">physiology</style></keyword><keyword><style  face="normal" font="default" size="100%">Print</style></keyword><keyword><style  face="normal" font="default" size="100%">rats</style></keyword><keyword><style  face="normal" font="default" size="100%">Receptor</style></keyword><keyword><style  face="normal" font="default" size="100%">receptors</style></keyword><keyword><style  face="normal" font="default" size="100%">Receptors,Opioid,delta</style></keyword><keyword><style  face="normal" font="default" size="100%">Receptors,Opioid,mu</style></keyword><keyword><style  face="normal" font="default" size="100%">Research</style></keyword><keyword><style  face="normal" font="default" size="100%">Research Support</style></keyword><keyword><style  face="normal" font="default" size="100%">Residue</style></keyword><keyword><style  face="normal" font="default" size="100%">SB - IM</style></keyword><keyword><style  face="normal" font="default" size="100%">series</style></keyword><keyword><style  face="normal" font="default" size="100%">Structure-Activity Relationship</style></keyword><keyword><style  face="normal" font="default" size="100%">Test</style></keyword><keyword><style  face="normal" font="default" size="100%">Universities</style></keyword><keyword><style  face="normal" font="default" size="100%">university</style></keyword><keyword><style  face="normal" font="default" size="100%">Vas Deferens</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2007</style></year><pub-dates><date><style  face="normal" font="default" size="100%">8/2/2007</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">520</style></number><volume><style face="normal" font="default" size="100%">50</style></volume><pages><style face="normal" font="default" size="100%">512 - 520</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">To synthesize potent antagonists of the mu-opioid receptor, we prepared a series of endomorphin-1 and endomorphin-2 analogues with 3-(1-naphthyl)-d-alanine (d-1-Nal) or 3-(2-naphthyl)-d-alanine (d-2-Nal) in position 4. Some of these analogues displayed weak antagonist properties. We tried to strengthen these properties by introducing the structurally modified tyrosine residue 2,6-dimethyltyrosine (Dmt) in place of Tyr1. Among the synthesized compounds, [Dmt1, d-2-Nal4]endomorphin-1, designated antanal-1, and [Dmt1, d-2-Nal4]endomorphin-2, designated antanal-2, turned out to be highly potent and selective mu-opioid receptor antagonists, as judged on the basis of two functional assays, the receptor binding assay and the hot plate test of analgesia. Interestingly, another analogue of this series, [Dmt1, d-1-Nal4]endomorphin-1, turned out to be a moderately potent mixed mu-agonist/delta-antagonist</style></abstract><issue><style face="normal" font="default" size="100%">3</style></issue><custom1><style face="normal" font="default" size="100%">4395</style></custom1><section><style face="normal" font="default" size="100%">512</style></section></record></records></xml>