Golub M S, Berger M E, Powell M
Prostaglandins Leukot Med. 1985 Dec;20(3):299-311. doi: 10.1016/0262-1746(85)90152-0.
The release of prostacyclin (PGI2) as measured by the production of 6-keto-PGF1 alpha was assessed in vitro in rat tail artery segments after exposure to norepinephrine (NE). Time course studies demonstrated a three fold increase in 6-keto-PGF1 alpha production in response to 6 X 10(-5) M NE that persisted for approximately one hour. This production was almost completely prevented by the cyclooxygenase inhibitors indomethacin and ibuprofen and the phospholipase inhibitor mepacrine. Vigorous rubbing of the vessel intima did not prevent the response to NE. Previously stimulated tissues were unresponsive to further addition of NE. However, the addition of arachidonic acid following NE resulted in further increases in PGI2 production which exceeded that of the addition of arachidonic acid alone. NE stimulation was significantly inhibited by phentolamine and prazosin pretreatment of the tissues but was not affected by yohimbine or propranolol. Alpha-1 adrenergic agonists (cirazoline, methoxamine, and phenylephrine) were stimulatory whereas alpha-2 agonists in high doses (tramazoline, BHT-920, xylazine, and UK-14304) were without effect. It is concluded that norepinephrine stimulates PGI2 production in the rat tail artery via an alpha-1 adrenergic receptor. NE also enhances the conversion of arachidonic acid to PGI2. Exhaustion of the response appears to be due to consumption of available arachidonic acid. The fact that procedures which generally remove most of the endothelium did not prevent NE-induced stimulation points to the vascular smooth muscle as the likely source of adrenergically mediated prostacyclin generation in this tissue.
通过测量6-酮-前列环素F1α(6-keto-PGF1α)的生成来评估去甲肾上腺素(NE)作用后大鼠尾动脉段中前列环素(PGI2)的释放。时间进程研究表明,对6×10⁻⁵ M NE的反应中,6-酮-前列环素F1α的生成增加了三倍,并持续约一小时。环氧化酶抑制剂吲哚美辛和布洛芬以及磷脂酶抑制剂米帕林几乎完全抑制了这种生成。剧烈摩擦血管内膜并不能阻止对NE的反应。先前受到刺激的组织对进一步添加NE无反应。然而,NE后添加花生四烯酸导致PGI2生成进一步增加,超过单独添加花生四烯酸的情况。酚妥拉明和哌唑嗪预处理组织可显著抑制NE刺激,但育亨宾或普萘洛尔对此无影响。α-1肾上腺素能激动剂(可乐唑啉、甲氧明和去氧肾上腺素)具有刺激作用,而高剂量的α-2激动剂(曲马唑嗪、BHT-920、赛拉嗪和UK-14304)则无作用。结论是,去甲肾上腺素通过α-1肾上腺素能受体刺激大鼠尾动脉中PGI2的生成。NE还增强花生四烯酸向PGI2的转化。反应耗尽似乎是由于可用花生四烯酸的消耗。一般能去除大部分内皮的操作并不能阻止NE诱导的刺激,这一事实表明血管平滑肌可能是该组织中肾上腺素介导的前列环素生成的来源。