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.
Naloxone盐酸盐是阿片类拮抗剂,对阿片受体的IC50为3 nM。
MoreGW0742是一种有效的,选择性PPARβ/δ激动剂,IC50为1 nM,比作用于hPPARα和hPPARγ选择性高1000倍。
MoreBatimastat (BB-94)是一种广谱MMP(基质金属蛋白酶)抑制剂,作用于MMP-1, MMP-2, MMP-9, MMP-7和MMP-3,IC50分别为3 nM, 4 nM, 4 nM, 6 nM和20 nM。
MoreU0126-EtOH(U-0126)是MEK1和2选择性抑制剂,IC50分别为70nM和60nM,对ΔN3-S218E/S222D MEK的亲和力比PD098059强100倍。
MoreCaffeic acid phenethyl ester是一种强效的特异性NF-κB活化抑制剂,也能够表现出抗氧化、免疫调节和抗炎活性。
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