Excitatory Amino Acid Receptor Interactions of a Novel α-Phosphinic Acid Analogue of α-Methylaspartic Acid

• Published in: Journal of pharmaceutical sciences 1984-11, Vol.73 (11), p.1550-1553
• Main Authors: Cates, L.A., Li, V-S., Hu, Z-S., Lehmann, J., Coyle, J.T., Ferkany, J.W.
• Format: Article
• Language: English
• Subjects: Acetylcholine - metabolism; Alanine - analogs & derivatives; Alanine - chemical synthesis; Alanine - pharmacology; Animals; anticonvulsant activity; Anticonvulsants - chemical synthesis; Anticonvulsants-in vitro; Anticonvulsants—in vitro, rats, excitatory amino acids; Aspartic Acid - metabolism; Biological and medical sciences; Cerebellum - metabolism; Corpus Striatum - metabolism; Electroshock; Excitatory amino acid receptors-N-methyl-D-aspartate; Excitatory amino acid receptors—N-methyl-D-aspartate, glutamate, kainate; excitatory amino acids; General pharmacology; glutamate; Glutamates - metabolism; Glutamic Acid; In Vitro Techniques; kainate; Medical sciences; Organophosphorus Compounds - chemical synthesis; Organophosphorus Compounds - pharmacology; Pentylenetetrazole - pharmacology; Pharmacology. Drug treatments; Phosphinic acids-excitatory amino acid receptors; Phosphinic acids—excitatory amino acid receptors, anticonvulsant activity; Physicochemical properties. Structure-activity relationships; Rats; Receptors, Amino Acid; Receptors, Cell Surface - metabolism; Synaptosomes - metabolism
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.2600731115

An α-phosphino analogue of α-methylaspartate has been synthesized. The compound may not interact with excitatory amino acid receptors directly, as assessed by direct in vitro radioreceptor binding methods; however, it possesses weak anticonvulsant activity and exhibits an excitant action in vitro that is apparently not mediated by a N-methyl-D-aspartate receptor.