【摘 要】
：
Analogues of endomorphin(Dmt-Pro-Xaa-Xaa-NH2)modified at position 4 or at position 4 and 3,and tripeptides(Dmt-Pro-Xaa-NH2)modified at position 3,with vario
【机 构】
：
SchoolofPharmacy,NanjingMedicalUniversity,Nanjing211166,ChinaCenterforIntegratedPreclinicalDrugDevel
论文部分内容阅读
Analogues of endomorphin(Dmt-Pro-Xaa-Xaa-NH2)modified at position 4 or at position 4 and 3,and tripeptides(Dmt-Pro-Xaa-NH2)modified at position 3,with various phenylalanine analogues(Xaa = Trp,1-Nal,2-Nal,Tmp,Dmp,Dmt)were synthesized and their effects on in vitro opioid activity were investigated.Most of the peptides exhibited high μ-opioid(MOP)receptor binding affinity(KiMOP = 0.13-0.81 nM),modest MOP-selectivity(Kiδ-opioid(DOP)/KiMOP = 3.5-316),and potent functional MOP agonism(GPI,IC50 = 0.274-249 nM)without DOP and κ-opioid(KOP)receptor agonism.Among them,compounds 7(Dmt-Pro-Tmp-Tmp-NH2)and 9(Dmt-Pro-1-Nal-NH2)were opioids with potent mixed MOP receptor agonism/DOP receptor antagonism and devoid of β-arrestin2 recruitment activity[1].They may offer a unique template for the discovery of potent analgesics that produce less respiratory depression,less gastrointestinal dysfunction and that have a lower propensity to induce tolerance and dependence compared with morphine[2].
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