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(S)‐homoquisqualate: a potent agonist at the glutamate metabotropic receptor
Author(s) -
Porter Richard H.P.,
Roberts Peter J.,
Jane David E.,
Watkins Jeffrey C.
Publication year - 1992
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1992.tb14366.x
Subject(s) - metabotropic glutamate receptor 2 , metabotropic receptor , metabotropic glutamate receptor , metabotropic glutamate receptor 5 , agonist , metabotropic glutamate receptor 1 , metabotropic glutamate receptor 7 , metabotropic glutamate receptor 6 , metabotropic glutamate receptor 4 , chemistry , acpd , glutamate receptor , neuroscience , pharmacology , receptor , biochemistry , biology
The synthetic quisqualate analogue, ( S )‐homoquisqualate was examined for activity at the glutamate metabotropic receptor, in relation to its ability to stimulate phosphoinositide hydrolysis in rat pup cerebro‐cortical slices. The compound produced a robust increase in hydrolysis (EC 50 = 50.2 ± 1.6 μ m ), which, in common with responses to quisqualate and (1 S ,3 R )‐1‐aminocyclopentane‐1,3‐dicarboxylate ((1 S ,3 R )‐ACPD), was antagonized uncompetitively by l ‐2‐amino‐3‐phosphonopropionate ( l ‐AP3). In contrast to quisqualate which exhibits low efficacy, ( S )‐homoquisqualate behaves as a full agonist at the metabotropic receptor.