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ACPT-II is a general competitive antagonist of metabotropic glutamate (mGlu) receptors. The KB values for mGlu1a, mGlu2, and mGlu4a receptors are 115, 88, and 77 µM, respectively.1 It binds to the large extracellular domain called a Venus flytrap module, where agonists bind.2 ACPT-II is a stereoisomer of the group III mGlu receptor-selective antagonist, ACPT-I.1
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1. Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: New tools to discriminate between metabotropic glutamate receptor subtypes. J. Med. Chem. 40, 3119-3129 (1997).
2. Closure of the Venus flytrap module of mGlu8 receptor and the activation process: Insights from mutations converting antagonists into agonists. Proc. Natl. Acad. Sci. USA 99(17), 11097-11102 (2002).