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.
CH-223191是选择性AhR受体拮抗剂。
MoreElvitegravir (EVG, JTK-303/GS-9137)是HIV整合酶抑制剂,对HIV-1 IIIB,HIV-2 EHO和HIV-2 ROD的IC50分别为0.7 nM,2.8 nM和1.4 nM。
MoreOSI-420 (Desmethyl Erlotinib,CP-473420)是erlotinib的活性代谢物,是口服活性的EGFR抑制剂,对人EGFR和EGFR自磷酸化的IC50分别为2和20 nM。
MoreNeostigmine Bromide是胆碱酯酶抑制剂,可作用于重症肌无力。
MoreEdoxaban是factor Xa选择性抑制剂,也是具有口服效应的抗凝药物。
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