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.
Loratadine是H1受体反向激动剂,IC50>32 μM。
MoreBafetinib (INNO-406)是一种有效的,选择性的,Bcr-Abl/Lyn双重抑制剂,IC50为5.8 nM/19 nM,对T315I突变型的磷酸化没有抑制作用,对PDGFR和c-Kit的作用效果稍弱。
MoreSafinamide Mesylate是Safinamide的甲磺酸盐,是一种选择性的且可逆的MAO-B抑制剂,IC50为98 nM,比作用于MAO-A选择性高5918倍。
MoreFexofenadine是第三代抗组胺药,用于治疗过敏症状,如花粉热,鼻塞和荨麻疹,抑制H1受体IC50值为246 nM。
MoreAZD2461是新型PARP抑制剂,能够避免由Pgp介导的olaparib抗性。
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