阿片样肽。第十二部分。在第2位被D-丙氨酰残基修饰且在第2和4位被3-(2-萘基)-D-丙氨酰残基修饰的甲硫氨酸脑啡肽类似物的合成及某些生物学性质。
Opiate-like peptides. Part XII. Synthesis and some biological properties of Met-enkephalin analogues modified in position 2 by D-alanyl residue in positions 2 and 4 by 3-(2-naphthyl)-D-alanyl residue.
作者信息
Rolka K, Obuchowicz E, Kupryszewski G, Gołba K, Herman Z S
机构信息
Institute of Chemistry, University of Gdańsk, Kotowice, Poland.
出版信息
Pol J Pharmacol Pharm. 1989 Mar-Apr;41(2):147-56.
Nine Met-enkephalin analogues containing D-alanyl residue in position 2 and/or 3-(2-naphthyl)-D-alanyl residue in positions 2 and 4 have been obtained. Their biological activity has been determined after intracerebroventricular administration to rats. Almost all compounds appeared strongly toxic causing the death of the animals. Only [D-2-Nal2,4, Met5-OMe]--enkephalin exerted an analgesic effect after the administration in the form of fine suspension.
已获得9种在第2位含有D-丙氨酰残基和/或在第2位和第4位含有3-(2-萘基)-D-丙氨酰残基的甲硫氨酸脑啡肽类似物。在对大鼠进行脑室内给药后测定了它们的生物活性。几乎所有化合物都表现出很强的毒性，导致动物死亡。只有[D-2-Nal2,4, Met5-OMe]--脑啡肽以精细悬浮液形式给药后发挥了镇痛作用。
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