HYDIA explained

HYDIA is a drug that is used in neuroscience research, which acts as a potent and selective antagonist for the group II metabotropic glutamate receptors (mGluR_2/3). It has been useful in the mapping of the group II mGluR receptor proteins and their molecular modeling.^[1] HYDIA is similar in structure to group II mGluR agonists such as eglumetad and pomaglumetad, but the addition of the 3-hydroxy group reverses the activity to a competitive antagonist. Other derivatives such as the 3-benzyloxy ether are more potent antagonists than HYDIA itself.^[2]

Notes and References

1. Lundström L, Kuhn B, Beck J, Borroni E, Wettstein JG, Woltering TJ, Gatti S . Mutagenesis and molecular modeling of the orthosteric binding site of the mGlu2 receptor determining interactions of the group II receptor antagonist (3)H-HYDIA . ChemMedChem . 4 . 7 . 1086–94 . July 2009 . 19402024 . 10.1002/cmdc.200900028 . 9062937 .
2. Woltering TJ, Adam G, Huguenin P, Wichmann J, Kolczewski S, Gatti S, Bourson A, Kew JN, Richards G, Kemp JA, Mutel V, Knoflach F . Asymmetric synthesis and receptor pharmacology of the group II mGlu receptor ligand (1S,2R,3R,5R,6S)-2-amino-3-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid-HYDIA . ChemMedChem . 3 . 2 . 323–35 . February 2008 . 18058780 . 10.1002/cmdc.200700226 . 1695024 .