Synthesis and opioid activity of dermorphin tetrapeptides bearing D-methionine S-oxide at position 2

S Salvadori, M Marastoni, G Balboni…

文献索引：Salvadori, Severo; Marastoni, Mauro; Balboni, Gianfranco; Sarto, Gian Pietro; Tomatis, Roberto Journal of Medicinal Chemistry, 1986 , vol. 29, # 6 p. 889 - 894

全文：HTML全文

被引用次数: 17

摘要

Eight new dermorphin tetrapeptides, X-Tyr-D-MetO-Phe-aa-Y (X= H, H2N= C (NH); aa= Gly, 2-aminoethanol, sarcosine; Y= NHz, NH--11, were prepared and teated for opioid activity. They show doee-related naloxone-reversible opioid effects in vitro and in vivo. H-Tyr-D- MetO-Phe-Gly-NH2 (I)(guinea pig ileum ICw= 13.6 n M tail-flick EDM= 1.97 pmol/mouse, icv, and 0.65 pmol/kg, sc), though less effective in the pheriphery, has central activities higher ...