反激动剂
γ-氨基丁酸受体
部分激动剂
变构调节
内在活性
药理学
化学
苯二氮卓
受体
加巴能
兴奋性突触后电位
神经科学
兴奋剂
生物
生物化学
出处
期刊:PubMed
日期:1988-01-01
卷期号:45: 275-92
被引量:9
摘要
The BZR is an allosteric modulatory site of the GABAA receptor, which is unique insofar as it mediates both a positive (facilitatory) and a negative (inhibitory) modulation of the GABA-mediated gating of the chloride channel. Ligands acting as positive modulators are called BZR agonists; ligands producing negative modulation, inverse BZR agonists. The effects of both classes of ligands are blocked by antagonists. A large number of compounds belonging to these three groups of ligands are known. Concepts are presented here that could explain the modulatory function of the BZR, and a number of factors are proposed to determine the pharmacological and therapeutic profile of BZR ligands: intrinsic efficacy at the BZR, density of GABAA-BZR on neurons, functional reserve in GABAA-BZRs, the intensity of the GABAergic input to a neuron, and the excitatory neuronal state. The effect of these factors on the pharmacology of full agonists, partial agonists, antagonists, partial inverse agonists, and inverse agonists is illustrated.
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