Prokai Laszlo, Zharikova Alevtina D, Juhasz Attila, Prokai-Tatrai Katalin
Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL 32610-0485, USA.
Peptides. 2006 May;27(5):1015-9. doi: 10.1016/j.peptides.2005.06.032. Epub 2006 Feb 21.
The neuropeptide FF (NPFF) antagonist desaminotyrosyl-Phe-Leu-Phe-Gln-Pro-Gln-Arg-NH2 dose-dependently reversed NPFF-induced elevation of blood pressure in anesthetized rats after intravenous injection without causing a significant change of blood pressure and heart rate by itself. However, another antagonist dansyl-Pro-Gln-Arg-NH2 produced a significant drop of the mean arterial pressure only at a large dose (10 micromol/kg body weight), but reversal of the NPFF-induced hypertension was modest. Consequently and contrary to the conclusions of a previous study, NPFF antagonists cannot be identified simply by measuring the changes in the hemodynamic parameters upon the injection of the compounds alone and without a subsequent NPFF challenge.
神经肽FF(NPFF)拮抗剂去氨基酪氨酰 - 苯丙氨酸 - 亮氨酸 - 苯丙氨酸 - 谷氨酰胺 - 脯氨酸 - 谷氨酰胺 - 精氨酸 - 氨基在静脉注射后可剂量依赖性地逆转NPFF诱导的麻醉大鼠血压升高,而其本身不会引起血压和心率的显著变化。然而,另一种拮抗剂丹磺酰 - 脯氨酸 - 谷氨酰胺 - 精氨酸 - 氨基仅在大剂量(10微摩尔/千克体重)时才会使平均动脉压显著下降,但对NPFF诱导的高血压的逆转作用较弱。因此,与先前一项研究的结论相反,不能仅通过测量单独注射化合物时的血流动力学参数变化而不进行后续NPFF激发来鉴定NPFF拮抗剂。