<?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%">Perlikowska,R.</style></author><author><style face="normal" font="default" size="100%">Fichna,J.</style></author><author><style face="normal" font="default" size="100%">Wyrebska,A.</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%">Toth,G.</style></author><author><style face="normal" font="default" size="100%">Storr,M.</style></author><author><style face="normal" font="default" size="100%">J.C. do Rego</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%">Design, synthesis and pharmacological characterization of endomorphin analogues with non-cyclic amino acid residues in position 24386</style></title><secondary-title><style face="normal" font="default" size="100%">Basic Clin.Pharmacol.Toxicol.</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%">acid</style></keyword><keyword><style  face="normal" font="default" size="100%">Acids</style></keyword><keyword><style  face="normal" font="default" size="100%">Activity</style></keyword><keyword><style  face="normal" font="default" size="100%">ALL</style></keyword><keyword><style  face="normal" font="default" size="100%">Amino acids</style></keyword><keyword><style  face="normal" font="default" size="100%">Analgesics</style></keyword><keyword><style  face="normal" font="default" size="100%">Analgesics,Opioid</style></keyword><keyword><style  face="normal" font="default" size="100%">Animals</style></keyword><keyword><style  face="normal" font="default" size="100%">Antigens</style></keyword><keyword><style  face="normal" font="default" size="100%">Antigens,CD13</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%">brain</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%">Comparative Study</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%">Design</style></keyword><keyword><style  face="normal" font="default" size="100%">Dipeptidyl Peptidase 4</style></keyword><keyword><style  face="normal" font="default" size="100%">Disease Models,Animal</style></keyword><keyword><style  face="normal" font="default" size="100%">drug therapy</style></keyword><keyword><style  face="normal" font="default" size="100%">electronic</style></keyword><keyword><style  face="normal" font="default" size="100%">Enzymes</style></keyword><keyword><style  face="normal" font="default" size="100%">im</style></keyword><keyword><style  face="normal" font="default" size="100%">in vivo</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%">Lead</style></keyword><keyword><style  face="normal" font="default" size="100%">M</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%">Oligopeptides</style></keyword><keyword><style  face="normal" font="default" size="100%">pain</style></keyword><keyword><style  face="normal" font="default" size="100%">Peptides</style></keyword><keyword><style  face="normal" font="default" size="100%">pharmacology</style></keyword><keyword><style  face="normal" font="default" size="100%">physiopathology</style></keyword><keyword><style  face="normal" font="default" size="100%">profile</style></keyword><keyword><style  face="normal" font="default" size="100%">Profiles</style></keyword><keyword><style  face="normal" font="default" size="100%">Protein Binding</style></keyword><keyword><style  face="normal" font="default" size="100%">RATES</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%">SELECTED</style></keyword><keyword><style  face="normal" font="default" size="100%">series</style></keyword><keyword><style  face="normal" font="default" size="100%">study</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></keywords><dates><year><style  face="normal" font="default" size="100%">2010</style></year><pub-dates><date><style  face="normal" font="default" size="100%">0/2/2010</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">113</style></number><volume><style face="normal" font="default" size="100%">106</style></volume><pages><style face="normal" font="default" size="100%">106 - 113</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">A series of endomorphin-1 (EM-1) and endomorphin-2 (EM-2) analogues, containing non-cyclic amino acids (Ala, D-Ala, beta-Ala, NMeAla, D-NMeAla or Sar) instead of Pro in position 2 was synthesized, where NMeAla = N-methylalanine and Sar = N-methylglycine, sarcosine. The opioid activity profiles of these peptides were determined in mu and delta opioid receptor (MOR and DOR)-representative binding assays and bioassays in vitro, as well as in the mouse hot-plate test in vivo. Finally, the degradation rates of all analogues in the presence of either rat brain homogenate or selected proteolytic enzymes were determined. Analogues of EM-2 were generally more potent than the respective analogues of EM-1. EM-2 analogues with D-Ala or D-NMeAla were about twofold more potent than the parent peptide and were least prone to degradation by brain homogenate, dipeptydyl peptidase IV and aminopeptidase M. In the in vivo test, [D-Ala(2)]EM-2 and [D-NMeAla(2)]EM-2 showed much higher analgesic potency than EM-2 which confirmed the usefulness of structural modifications in obtaining new leads for pain-relief therapeutics</style></abstract><issue><style face="normal" font="default" size="100%">2</style></issue><custom1><style face="normal" font="default" size="100%">4386</style></custom1><section><style face="normal" font="default" size="100%">106</style></section></record></records></xml>