(S)-3,5-DHPG

(S)-3,5-DHPG, known more commonly as DHPG, is an agonist of the group I metabotropic glutamate receptors (mGluRs), binding both mGluR1a and mGluR5a (K_i = 0.9 and 3.9 µM, respectively) but not ionotropic glutamate receptors.¹ The (S)-enantiomer is about ten times more potent than the (R)-enantiomer.² (S)-3,5-DHPG is commonly used to evaluate the roles of group I mGluRs in neuronal signaling.^3,4

WARNING This product is not for human or veterinary use.

1. Mutel, V., Ellis, G.J., Adam, G., et al. Characterization of [³H]quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections. J. Neurochem. 75(6), 2590-2601 (2000).

2. Baker, S.R., Goldsworthy, J., Harden, R.C., et al. Enzymatic resolution and pharmacological activity of the enantiomers of 3,5-dihydroxyphenylglycine, a metabotropic glutamate receptor agonist. Bioorg. Med. Chem. Lett. 5(3), 223-228 (1995).

3. Clements, M.A., Swapna, I., and Morikawa, H. Inositol 1,4,5-triphosphate drives glutamatergic and cholinergic inhibition selectively in spiny projection neurons in the striatum. J. Neurosci. 33(6), 2697-2708 (2013).

4. Grolla, A.A., Sim, J.A., Lim, D., et al. Amyloid-β and Alzheimer’s disease type pathology differentially affects the calcium signalling toolkit in astrocytes from different brain regions. Cell Death Dis. (2013).