Bent S, Fehling U, Braam U, Schunack W, Schmutzler W
Institut für Pharmakologie und Toxikologie, Medizinische Fakultät der RWTH Aachen.
Agents Actions. 1991 May;33(1-2):67-70. doi: 10.1007/BF01993129.
The effects of the H3-agonist R-alpha-methylhistamine (R-alpha-MeHA) and the H3-antagonist thioperamide on the spontaneous and concanavalin A (ConA) induced histamine release from human mast cells were tested and compared with the effect of some H1- and H2-receptor active substances. R-alpha-MeHA (10(-9)-10(-7) M) exerted no effect on histamine release whereas thioperamide increased the spontaneous release at 10(-6)-10(-4) M but inhibited the ConA induced release in a narrow concentration range (10(-6)-10(-5) M). This enhancement might be taken as an indication of the existence of H3-receptor dependent autoregulation although presently other mechanism cannot be excluded.
测试了H3激动剂R-α-甲基组胺(R-α-MeHA)和H3拮抗剂硫代酰胺对人肥大细胞自发释放和伴刀豆球蛋白A(ConA)诱导的组胺释放的影响,并与一些H1和H2受体活性物质的作用进行了比较。R-α-MeHA(10^(-9)-10^(-7) M)对组胺释放无影响,而硫代酰胺在10^(-6)-10^(-4) M时增加自发释放,但在狭窄浓度范围(10^(-6)-10^(-5) M)内抑制ConA诱导的释放。这种增强可能表明存在H3受体依赖性自调节,尽管目前不能排除其他机制。