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.
Cilomilast是一种有效的PDE4抑制剂,IC50为110 nM,具有抗炎活性和弱的中枢神经系统活性。
MoreEntacapone是特异的外周活性的邻苯二酚-O-甲基转移酶(COMT)抑制剂,IC50为151 nM。
MorePF-2545920是一种有效的,选择性的PDE10A抑制剂,IC50为0.37 nM,比作用于PDE选择性高1000倍以上。
MorePracinostat是广泛的HDAC抑制剂,对HDAC1,3,4,5,9,和10的IC50分别是49 nM,43 nM,56 nM,47 nM,70 nM和40 nM。
MoreWHI-P154是JAK3抑制剂,IC50为1.8 μM,还能抑制EGFR,Src,Abl,VEGFR和MAPK,对JAK1和JAK2无活性。
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