Pharmacological properties of a series of alpha, omega-diamino-omega-phosphonocarboxylic acids and alpha, omega-diamino-alpha, omega-bis(phosphonic acids) on different excitatory amino acids mediated responses have been tested in CA1 rat hippocampal neurones, using intracellular recordings and current and voltage clamp techniques. In contrast with known antagonists as D(-)2-amino-5-phosphonopentanoic acid (AP-5) and 2-amino-4-oxo-5-phosphonopentanoic acid, which completely abolished the NMDA-response, no antagonistic activity was found. We conclude that the introduction of an omega-amino function abolishes the NMDA-antagonistic activity of alpha-amino-omega-phosphonocarboxylic acids.

Animals↗

PubMedDate not supplied

A contribution to the structure-activity relationship in glutamate receptor ligands: 2. Characterization of 2-amino-4-oxo-5-pentanoic acid as NMDA receptor antagonist.

Pharmacological properties of 2-amino-4-oxo-5-phosphonopentanoic acid (AOPA) on excitatory amino acids mediated responses have been tested in CA1 rat hippocampal neurones, using intracellular recordings and current and voltage clamp techniques. These properties were compared with those of the well-known NMDA antagonist, D(-)2-amino-5-phosphonopentanoic acid (AP-5). AOPA completely abolished the response to NMDA but had no effects on the responses to AMPA, quisqualate and kainate. In voltage clamp experiments AOPA antagonized NMDA-induced currents and produced a parallel shift of the NMDA concentration-response curve. Schild analysis gave a Kd value of 26 microM. AP-5 also produced a similar shift in this curve with a Kd of 6.9 mu.

Amino Acids↗

PubMedDate not supplied

[Changes in the Hoffman reflex during wakefulness and sleep in children with cerebral paralysis].

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Cerebral Palsy↗