Plech A, Rykaczewska-Czerwińska M, Bartosz-Bechowski H, Lombarska-Sliwińska D, Małota M, Szewczyk M, Brus R, Konopińska D
Department of Pharmacology, Silesian Medical Academy, Zabrze, Poland.
Pol J Pharmacol. 1997 Mar-Jun;49(2-3):119-26.
The insect myotropic octapeptide leucopyrokinin Glp-Thr-Ser-Phe-Thr-Pro-Arg-Leu-amide (LPK or Lem-PK) (1) and its truncated analogues without the first N-terminal amino acids [2-8]-LPK (2) as well as devoid of the first, second and third N-terminal amino acids [4-8]-LPK (3) were prepared together with a series of the following modified [2-8]-LPK heptapetides such as: [Ala2] (4)-, [Ala3] (6)-, [D-Phe4] (7)-, [Ala5] (8)-, [D-Ala5] (9)-, [D-Thr5] (10)-, [Ser5] (11)-, [D-Pro6] (12)-, [Ala6] (13)- and [D-Arg7]-[2-8]-LPK (14) and [Pro1]-LPK (5). Bioassays were carried out by means of a hot-plate and a tail immersion tests in rats after i.c.v. and i.p. injections. Peptides 1 and 2 revealed prolonged high antinociceptive effects, while other peptides were practically inactive. [2-8]-LPK (2) probably crosses the blood-brain barrier in rats.
昆虫亲肌八肽亮氨焦激肽Glp-Thr-Ser-Phe-Thr-Pro-Arg-Leu-酰胺（LPK或Lem-PK）（1）及其不含前N端氨基酸的截短类似物[2-8]-LPK（2）以及不含前三个N端氨基酸的[4-8]-LPK（3），与以下一系列修饰的[2-8]-LPK七肽一起制备，例如：[Ala2]（4）-、[Ala3]（6）-、[D-Phe4]（7）-、[Ala5]（8）-、[D-Ala5]（9）-、[D-Thr5]（10）-、[Ser5]（11）-、[D-Pro6]（12）-、[Ala6]（13）-和[D-Arg7]-[2-8]-LPK（14）以及[Pro1]-LPK（5）。通过在大鼠脑室内和腹腔注射后进行热板和尾浸试验进行生物测定。肽1和2显示出延长的高镇痛作用，而其他肽实际上无活性。[2-8]-LPK（2）可能在大鼠中穿过血脑屏障。
