<?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%">Staniszewska,R.</style></author><author><style face="normal" font="default" size="100%">Fichna,J.</style></author><author><style face="normal" font="default" size="100%">Gach,K.</style></author><author><style face="normal" font="default" size="100%">Toth,G.</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%">A.E. Janecka</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Synthesis and biological activity of endomorphin-2 analogs incorporating piperidine-2-, 3- or 4-carboxylic acids instead of proline in position 24391</style></title><secondary-title><style face="normal" font="default" size="100%">Chem.Biol.Drug Des</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">0</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%">Aequorin</style></keyword><keyword><style  face="normal" font="default" size="100%">Amino Acid Substitution</style></keyword><keyword><style  face="normal" font="default" size="100%">Amino acids</style></keyword><keyword><style  face="normal" font="default" size="100%">an</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%">brain</style></keyword><keyword><style  face="normal" font="default" size="100%">Brain Chemistry</style></keyword><keyword><style  face="normal" font="default" size="100%">Calcium</style></keyword><keyword><style  face="normal" font="default" size="100%">Carboxylic Acids</style></keyword><keyword><style  face="normal" font="default" size="100%">chemistry</style></keyword><keyword><style  face="normal" font="default" size="100%">Comparison</style></keyword><keyword><style  face="normal" font="default" size="100%">electronic</style></keyword><keyword><style  face="normal" font="default" size="100%">Functional</style></keyword><keyword><style  face="normal" font="default" size="100%">im</style></keyword><keyword><style  face="normal" font="default" size="100%">Inhibitory Concentration 50</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%">medical</style></keyword><keyword><style  face="normal" font="default" size="100%">Oligopeptides</style></keyword><keyword><style  face="normal" font="default" size="100%">Piperidines</style></keyword><keyword><style  face="normal" font="default" size="100%">Proline</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,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%">SB - IM</style></keyword><keyword><style  face="normal" font="default" size="100%">stability</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%">2008</style></year><pub-dates><date><style  face="normal" font="default" size="100%">0/7/2008</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">94</style></number><volume><style face="normal" font="default" size="100%">72</style></volume><pages><style face="normal" font="default" size="100%">91 - 94</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">Novel endomorphin-2 (EM-2) analogs have been synthesized, incorporating unnatural amino acids with six-membered heterocyclic rings, such as piperidine-2-, 3- and 4-carboxylic acids (Pip, Nip and Inp, respectively) instead of Pro in position 2. [(R)-Nip(2)]EM-2 displayed an extremely high affinity for the mu-opioid receptor with IC(50) = 0.04 +/- 0.01 nM in comparison with IC(50) = 0.69 +/- 0.03 nM for EM-2. This analog was also very potent in the aequorin luminescence-based functional calcium assay and showed significantly enhanced stability in rat brain homogenate</style></abstract><issue><style face="normal" font="default" size="100%">1</style></issue><custom1><style face="normal" font="default" size="100%">4391</style></custom1><section><style face="normal" font="default" size="100%">91</style></section></record></records></xml>