(S)-homoquisqualate: a potent agonist at the glutamate metabotropic receptor.
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 (EC50 = 50.2 +/- 1.6 microM), which, in common with responses to quisqualate and (1S,3R)-1-aminocyclopentane-1,3-dicarboxylate ((1S,3R)-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.
Porter
R H
RH
Department of Physiology & Pharmacology, University of Southampton.
Roberts
P J
PJ
Jane
D E
DE
Watkins
J C
JC
D000818:Animals; D001921:Brain / Q000187:drug effects*; D005971:Glutamates / Q000378:metabolism*; D006868:Hydrolysis; D016318:Quisqualic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D017470:Receptors, Glutamate; D017981:Receptors, Neurotransmitter / Q000187:drug effects*
D005971:Glutamates; D017470:Receptors, Glutamate; D017981:Receptors, Neurotransmitter; D016318:Quisqualic Acid