Overview
- Møller, E.H. et al. (1999) Chirality 11, 752.
Alomone Labs (S)-ATPO inhibits GluA1 receptors expressed in Xenopus oocytes.Time course of GluA1 currents, activated by a continuous application (top dotted line) of 1 µM (S)-AMPA (#A-267), and reversibly inhibited by 10 µM and 100 µM (S)-ATPO (#A-330), as indicated (bars), at a holding potential of -60 mV.
ATPO, a phosphono amino acid, is a structural hybrid between the NMDA antagonist (RS)-2-amino-7-phosphonoheptanoic acid (AP7) and the AMPA and GluR5 agonist, (RS)-2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl) propionic acid (ATPA).
(S)-ATPO acts as a potent and selective AMPA and kainate receptor antagonist. ATPO has the ability to competitively reduce peak responses evoked by semi-rapid applications of AMPA1. It antagonizes AMPA-induced depolarization in the cortical wedge preparation with an IC50 value of 15 µM1.
AMPA receptors are the principal glutamate receptors that mediate fast excitatory neurotransmission. This function is essential for synaptic plasticity and cellular correlate of learning and memory. Antagonists of AMPA receptors are good drug candidates for potential treatment of several neurological disorders such as epilepsy, stroke and amyotrophic lateral sclerosis (ALS)2,3.
