Department of Synthesis and Chemical Technology of Pharmaceutical Substances with Computer Modeling Laboratory, Faculty of Pharmacy, Medical University of Lublin, 4A Chodźki St., PL-20093 Lublin, Poland.
School of Pharmacy, University of Eastern Finland, Yliopistonranta 1, P.O. Box 1627, FI-70211 Kuopio, Finland.
Molecules. 2022 Dec 25;28(1):178. doi: 10.3390/molecules28010178.
Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays a hot topic in medicinal chemistry. Allosteric modulators, i.e., compounds which bind in a receptor site topologically distinct from orthosteric sites, exhibit a number of advantages. They are more selective, safer and display a ceiling effect which prevents overdosing. Allosteric modulators of dopamine D receptor are potential drugs against a number of psychiatric and neurological diseases, such as schizophrenia and Parkinson's disease. In this review, an insightful summary of current research on D receptor modulators is presented, ranging from their pharmacology and structural aspects of ligand-receptor interactions to their synthesis.
变构调节 G 蛋白偶联受体（GPCRs）是当今药物化学的热门话题。变构调节剂，即结合在与正位点拓扑上不同的受体部位的化合物，具有许多优点。它们更具选择性、更安全，并具有防止过量用药的上限效应。多巴胺 D 受体的变构调节剂是治疗多种精神和神经疾病（如精神分裂症和帕金森病）的潜在药物。在这篇综述中，对 D 受体调节剂的当前研究进行了深入总结，从配体-受体相互作用的药理学和结构方面到它们的合成。
