Shinkai Koji, Toyohira Yumiko, Yoshimura Reiji, Tsutsui Masato, Ueno Susume, Nakamura Jun, Yanagihara Nobuyuki
Department of Psychiatry, University of Occupational and Environmental Health, School of Medicine, Kitakyushu, 807-8555, Japan.
Naunyn Schmiedebergs Arch Pharmacol. 2007 Mar;375(1):65-72. doi: 10.1007/s00210-006-0128-4. Epub 2007 Jan 9.
Milnacipran is a serotonin noradrenaline reuptake inhibitor (SNRI) and is used clinically as an antidepressant. We report here the effect of milnacipran on catecholamine synthesis in cultured bovine adrenal medullary cells. Incubation of adrenal medullary cells with milnacipran (300 ng/ml, 1,065 nM) for 20 min resulted in a significant increase in 14C-catecholamine synthesis from [14C]tyrosine, but not from [14C]DOPA, whereas the selective serotonin reuptake inhibitors (SSRIs), paroxetine (300 ng/ml, 800 nM) and fluvoxamine (300 ng/ml, 691 nM), had little effect. Milnacipran, but not paroxetine or fluvoxamine, increased the activity of tyrosine hydroxylase, the rate-limiting step of catecholamine biosynthesis, in a concentration-dependent manner (100-300 ng/ml, 355-1,065 nM). U0126 (1 microM), an inhibitor of p44/42 mitogen-activated protein kinase (MAPK) kinase, abolished the stimulatory effects of milnacipran on tyrosine hydroxylase activity. Furthermore, incubation of cells with milnacipran (30-100 ng/ml) for 5 min activated p44/42 MAPK, whereas paroxetine and fluvoxamine did not. The present findings suggest that milnacipran activates tyrosine hydroxylase and then stimulates catecholamine synthesis through a p44/42 MAPK-dependent pathway in cultured bovine adrenal medullary cells.
米那普明是一种5-羟色胺去甲肾上腺素再摄取抑制剂(SNRI),在临床上用作抗抑郁药。我们在此报告米那普明对培养的牛肾上腺髓质细胞中儿茶酚胺合成的影响。用米那普明(300 ng/ml,1065 nM)孵育肾上腺髓质细胞20分钟,导致从[14C]酪氨酸合成14C-儿茶酚胺显著增加,但从[14C]多巴合成的儿茶酚胺没有增加,而选择性5-羟色胺再摄取抑制剂(SSRI)帕罗西汀(300 ng/ml,800 nM)和氟伏沙明(300 ng/ml,691 nM)几乎没有影响。米那普明而非帕罗西汀或氟伏沙明以浓度依赖性方式(100 - 300 ng/ml,355 - 1065 nM)增加了儿茶酚胺生物合成限速步骤酪氨酸羟化酶的活性。U0126(1 microM),一种p44/42丝裂原活化蛋白激酶(MAPK)激酶抑制剂,消除了米那普明对酪氨酸羟化酶活性的刺激作用。此外,用米那普明(30 - 100 ng/ml)孵育细胞5分钟可激活p44/42 MAPK,而帕罗西汀和氟伏沙明则不能。目前的研究结果表明,米那普明在培养的牛肾上腺髓质细胞中通过p44/42 MAPK依赖性途径激活酪氨酸羟化酶,进而刺激儿茶酚胺合成。