In some cases, receptor activation caused by ligand binding to a receptor is directly coupled to the cell's response to the ligand. For example, the neurotransmitter GABA can activate a cell surface receptor that is part of an ion channel. GABA binding to a GABAA receptor on a neuron opens a chloride-selective ion channel that is part of the receptor. GABAA receptor activation allows negatively charged chloride ions to move into the neuron, which inhibits the ability of the neuron to produce action potentials.
Nicorandil 钾离子通道活化剂。
MoreLY2603618是Chk1蛋白激酶选择性抑制剂,IC50为7 nM,是第一个进入临床实验的Chk1选择性抑制剂。
MoreGW9508是一种有效的,选择性FFA1(GPR40)激动剂,pEC50为7.32,比作用于GPR120选择性高100倍,以葡萄糖敏感性方式刺激胰岛素的分泌。
MoreFenofibrate是PPARα激动剂,对小鼠和人的PPARα的EC50分别为18 μM和30 μM。
MoreMeclizine是H1组胺受体拮抗剂,可作用于晕动病。
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