Gulati O D, Shah N S
Eur J Pharmacol. 1977 Nov 15;46(2):135-45. doi: 10.1016/0014-2999(77)90249-7.
The amine releasing action of mescaline was investigated in rat isolated hypothalamus labeled with 3H-metaraminol. Mescaline had no effect on the uptake of 3H-metaraminol but produced its release in a concentration-related manner. 4 x 10(-4) M mescaline, which produced submaximal effects was used for subsequent experiments. 3 x 10(-5) M cocaine had no effect on the 3H-metaraminol releasing action of mescaline. Mescaline was fully effective in Ca2+-free medium while 6 x 10(-2) M KCl was ineffective. 3 x 10(-7) M tetrodotoxin or 6 x 10(-5) M lidocaine partially blocked mescaline-induced release but substantially or completely blocked 3 x 10(-2) M KCl-induced release. Prior exposure of hypothalamus to 3 x 10(-4) M tyramine reduced the releasing action of mescaline. Thus, mescaline appears to release 3H-metaraminol both by Ca2+-independent (tyramine-like) and Ca2+-dependent (lidocaine-sensitive) mechanisms. 3 x 10(-4) M tyramine and 6 x 10(-2) M KCl released 14C from control hypothalamus labelled with 14C-mescaline, but not from reserpinized hypothalamus. The amounts of 14C recovered in 14C-mescaline labeled control and reserpinized hypothalamus at the end of 50 min of efflux were similar suggesting a poor retention of 14C-mescaline by storage particles.
在以3H - 间羟胺标记的大鼠离体下丘脑上研究了三甲氧苯乙胺的胺释放作用。三甲氧苯乙胺对3H - 间羟胺的摄取没有影响，但以浓度相关的方式使其释放。产生次最大效应的4×10（-4）M三甲氧苯乙胺用于后续实验。3×10（-5）M可卡因对三甲氧苯乙胺的3H - 间羟胺释放作用没有影响。三甲氧苯乙胺在无钙培养基中完全有效，而6×10（-2）M氯化钾无效。3×10（-7）M河豚毒素或6×10（-5）M利多卡因部分阻断了三甲氧苯乙胺诱导的释放，但基本上或完全阻断了3×10（-2）M氯化钾诱导的释放。预先将下丘脑暴露于3×10（-4）M酪胺可降低三甲氧苯乙胺的释放作用。因此，三甲氧苯乙胺似乎通过不依赖钙（类似酪胺）和依赖钙（对利多卡因敏感）的机制释放3H - 间羟胺。3×10（-4）M酪胺和6×10（-2）M氯化钾从以14C - 三甲氧苯乙胺标记的对照下丘脑释放14C，但不从利血平化的下丘脑释放。在流出50分钟结束时，在以14C - 三甲氧苯乙胺标记的对照和利血平化下丘脑回收的14C量相似，表明储存颗粒对14C - 三甲氧苯乙胺的保留较差。
