Helmeste D M, Tang S W
Department of Psychiatry, Veterans Administration Medical Center, Long Beach, CA 90822.
Eur J Pharmacol. 1994 Apr 15;267(2):239-42. doi: 10.1016/0922-4106(94)90176-7.
Effects of kinase inhibitors and activators on the binding of tritiated imipramine and inhibition of serotonin uptake were tested in platelets. The majority of compounds inhibited specific [3H]imipramine binding and serotonin uptake with affinities similar to those reported for their action on protein kinases themselves. Many of these compounds are derivatives with modified naphthalenesulfonamide or isoquinolinesulfonamide structures, which appear to compete directly with imipramine for binding to the serotonin transporter. This is of great importance for studies involving kinase regulation since at these concentrations, the inhibitors and activators were previously thought to interact virtually exclusively with protein kinases.
在血小板中测试了激酶抑制剂和激活剂对氚化丙咪嗪结合及5-羟色胺摄取抑制的影响。大多数化合物抑制特异性[3H]丙咪嗪结合和5-羟色胺摄取，其亲和力与报道的它们对蛋白激酶自身的作用相似。这些化合物中有许多是具有修饰的萘磺酰胺或异喹啉磺酰胺结构的衍生物，它们似乎直接与丙咪嗪竞争结合5-羟色胺转运体。这对于涉及激酶调节的研究非常重要，因为在这些浓度下，抑制剂和激活剂以前被认为几乎只与蛋白激酶相互作用。
