Studies on the mechanism of action of avermectin B1a: stimulation of release of gamma-aminobutyric acid from brain synaptosomes.
作者： Sheng-Shung Pong , Ching C. Wang , Lawrence C. Fritz
DOI: 10.1111/J.1471-4159.1980.TB06604.X
关键词:
摘要: : Avermectin B1a, a novel macrocyclic lactone antiparasitic agent, causes marked and sustained increase of γ-aminobutyric acid release from rat brain synaptosomes. A concentration 8-10 μM avermectin B1a produced the maximal effect (310 ± 30% control), while half-maximal level was achieved at 2-3 μM. The drug also stimulated (251 11% basal level) synaptosomes in calcium-free medium, which 28 4% lower than that 1.8 mm-Ca2+ medium. compound did not, however, affect synaptosomal glutamate. At lobster neuromuscular junction, reduced input resistance muscle fibers control Ringer's solution as well Co2+ substituted for Ca2+. This observation is accord with Ca2+ independent stimulation seen good correlation between activity acid-releasing has been found among various derivatives suggests ability to this neurotransmitter may be basis its action.
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