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.
GW9508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。
MoreRivaroxaban是一种口服具有直接作用的Factor Xa抑制剂,Ki值为0.4 nM,IC50值为0.7 nM。
MorePiperine是一种生物碱,是造成黑胡椒和长胡椒辛辣的原因,也用于一些传统医学领域,且作为杀虫剂。
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