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.
TAK-875是一种选择性GPR40激动剂,EC50为14 nM,比油酸有效400倍。
MoreAtorvastatin calcium, a hydrophilic inhibitor, inhibits the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Atorvastatin hemicalcium salt 是高活性HMG-CoA还原酶抑制剂,IC50为8 nM。
MoreGo6976 is a potent protein kinase C (PKC) inhibitor (IC50 = 7.9 nM), selectively inhibits PKCα, and PKCβ1 (IC50 values are 2.3 and 6.2 nM respectively).
MoreTacrolimus (FK506)是一种免疫抑制剂和大环内酯类抗生素,用于同种异体的器官移植,可以降低病人的免疫系统的作用。
MoreDexamethasone (DEX), a synthetic glucocorticoid, is widely used in clinical settings for its anti-inflammatory effect. Dexamethasone (DHAP)是一种抗炎剂和免疫抑制剂。
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