Structure optimization of positive allosteric modulators of GABA<sub>B</sub> receptors led to the unexpected discovery of antagonists/potential negative allosteric modulators.
第一作者:
Claudia,Mugnaini
第一单位:
Department of Biotechnology, Chemistry, and Pharmacy, University of Siena, I-53100 Siena, SI, Italy. Electronic address: claudia.mugnaini@unisi.it.
作者:
主题词
别构调节(Allosteric Regulation);巴氯芬(Baclofen);苯呋喃类(Benzofurans);结合部位(Binding Sites);环化(Cyclization);环戊烷类(Cyclopentanes);药物评价, 临床前(Drug Evaluation, Preclinical);GABA调节剂(GABA Modulators);GABA-B受体激动剂(GABA-B Receptor Agonists);鸟苷5'-O-(3-硫代三磷酸)(Guanosine 5'-O-(3-Thiotriphosphate));人类(Humans);原冰片烷类(Norbornanes);蛋白质结合(Protein Binding);嘧啶类(Pyrimidines);受体, GABA-B(Receptors, GABA-B);构效关系(Structure-Activity Relationship)
DOI
10.1016/j.bmcl.2020.127443
PMID
32730942
发布时间
2021-06-03
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