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.
Orteronel (TAK-700) is an inhibitor of the steroidogenic enzyme CYP17A1. It has higher specificity for the 17,20 lyase activity of CYP17A1 with IC50 of 38 nM. Phase III.
MoreICI 162,846是活性的 H2 拮抗剂, 体内有效。
MoreICI 204,448 hydrochloride是κ 激动剂, 作用于外周(acts peripherally)。
MoreHX 531是活性的 RXR 拮抗剂。
MoreHX 630是RXR synergist。
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