Isomers of 2-amino-7-phosphonoheptanoic acid as antagonists of neuronal excitants.
The D(-)-isomer of 2-amino-7-phosphonoheptanoic acid ( (-)APH) was active as an antagonist of N-methyl-D-aspartate (NMDA) excitation of central neurones. The L(+)-isomer was inactive. The antagonism was also selective, kainate and glutamate responses being relatively unaffected. Excitatory responses to ibotenic acid, a neurotoxic amino acid analogue, were less susceptible to blockade by (-)APH than NMDA, but more so than kainic acid. Ibotenate may therefore act partly on NMDA receptors.
D015763:2-Amino-5-phosphonovalerate / Q000031:analogs & derivatives*; D000596:Amino Acids / Q000494:pharmacology*; D000818:Animals; D001224:Aspartic Acid / Q000031:analogs & derivatives / Q000494:pharmacology; D002540:Cerebral Cortex / Q000187:drug effects / Q000502:physiology*; D006624:Hippocampus / Q000187:drug effects / Q000502:physiology*; D007051:Ibotenic Acid / Q000494:pharmacology; D007608:Kainic Acid / Q000494:pharmacology; D016202:N-Methylaspartate; D009474:Neurons / Q000187:drug effects / Q000502:physiology*; D051381:Rats
D000596:Amino Acids; D007051:Ibotenic Acid; D001224:Aspartic Acid; D016202:N-Methylaspartate; D015763:2-Amino-5-phosphonovalerate; C031231:2-amino-7-phosphonoheptanoic acid; D007608:Kainic Acid