Amenta F, De Rossi M, Mione M C, Geppetti P
Eur J Pharmacol. 1985 Jun 7;112(2):181-6. doi: 10.1016/0014-2999(85)90494-7.
The in vitro uptake of tritiated serotonin ([3H]5HT) was studied in a preparation of rat extracerebral arteries. The uptake of [3H]5HT was time- and temperature-dependent and of high affinity; linear regression analysis gave a Km value of 6.48 X 10(-7) M for the specific uptake. Bilateral superior cervical ganglionectomy was without effect on [3H]5HT uptake while it significantly reduced the uptake of tritiated norepinephrine by the preparation of rat extracerebral arteries. The serotonergic neurotoxin 5,7-dihydroxytryptamine and lesions to both the medial and the dorsal raphe nuclei caused a marked loss of [3H]5HT uptake but did not change the uptake of tritiated norepinephrine. Competition studies with norepinephrine, desimipramine (a noradrenergic uptake blocker), nomifensine (a dopaminergic uptake blocker) and fluoxetine (a 5HT uptake blocker) confirmed the specificity of the [3H]5HT uptake mechanism. Histoautoradiographic studies showed the highest density of silver grains at the level of the adventitial-medial border of the basilar artery. Fluoxetine inhibited the accumulation of silver grains within the adventitial-medial border in the blood vessel studied. The present data further support the view that a neuronal serotonergic system may play a role in the control of blood flow in the cerebrovascular tree.
在大鼠脑外动脉制备物中研究了氚标记的血清素([3H]5HT)的体外摄取。[3H]5HT的摄取具有时间和温度依赖性,且亲和力高;线性回归分析得出特异性摄取的Km值为6.48×10(-7)M。双侧颈上神经节切除术对[3H]5HT的摄取没有影响,而它显著降低了大鼠脑外动脉制备物对氚标记去甲肾上腺素的摄取。血清素能神经毒素5,7 - 二羟基色胺以及内侧和背侧中缝核的损伤导致[3H]5HT摄取明显丧失,但未改变氚标记去甲肾上腺素的摄取。用去甲肾上腺素、地昔帕明(一种去甲肾上腺素能摄取阻滞剂)、诺米芬辛(一种多巴胺能摄取阻滞剂)和氟西汀(一种5HT摄取阻滞剂)进行的竞争研究证实了[3H]5HT摄取机制的特异性。组织放射自显影研究显示,在基底动脉外膜 - 中膜边界水平银颗粒密度最高。在所研究的血管中,氟西汀抑制了外膜 - 中膜边界内银颗粒的积累。目前的数据进一步支持了神经元血清素能系统可能在脑血管树血流控制中起作用的观点。