This study examined the binding of (S)-( 3 H)AMPA , the radiolabelled active isomer of AMPA, to rat brain synaptic membranes. Under non-chaotropic conditions specific binding of 10 nM (S)-( 3 H)AMPA represented 33 ± 2% of the total; this increased to 74 ± 1% in the presence of 100 mM KSCN. (S)-( 3 H)AMPA binding was inhibited by non-NMDA receptor agonists and the antagonists NBQX and CNQX, with the following rank order of potency: NBQX > ( S )-AMPA ⩾ quisqualate > CNQX > l -glutamate > domoate ⩾ kainate > ( R )-AMPA. NMDA, and the metabotropic glutamate receptor agonist (1 S ,3 R )-ACPD, up to 100 μM, did not inhibit (S)-( 3 H)AMPA binding. A number of willardiine analogues all effectively inhibited (S)-( 3 H)AMPA binding with the rank order of potency: ( S )-5-fluorowillardiine > ( S )-5-nitrowillardiine > ( S )-5-trifluoromethylwillardiine > ( S )-5-bromowillardiine ≈ ( S )-5-chlorowillardiine > ( S )-5-cyanowillardiine > ( S )-willardiine > ( S )-5-iodowillardiine > ( S )-6-methylwillardiine > ( S )-5-methylwillardiine. This rank order closely reflects data from equilibrium measurements made, under voltage clamp, on cultured hippocampal neurons. In contrast the respective ( R )-enantiomers and the racemate mixtures of ( R , S )-3, 5 and 6-isowillardiine were relatively inactive. Similar IC 50 values and thus rank orders of potency for the willardiines were observed in the presence of 100 mM KSCN.
Neuropharmacology – Elsevier
Published: Apr 1, 1995
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