Cyclothiazide decreases [3HAMPA binding to rat brain membranes: evidence that AMPA receptor desensitization increases agonist affinity
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Use of [<sup>3</sup>H]fluorowillardiine to study properties of AMPA receptor allosteric modulators
2006, Brain ResearchCitation Excerpt :As expected, the drug increased the apparent affinities for the radioligands about three-fold but did not significantly alter Bmax values (receptor densities). Similar tests with other drugs, including CTZ, found that the drug-induced change in binding in each instance reflects a change in agonist affinity and not in Bmax (Hall et al., 1993a; Suzuki et al., 2004). 2,3-Benzodiazepines and related compounds, which include GYKI 52466, GYKI 53655 and SYM2206 (Fig. 1), effectively inhibit AMPA receptor currents, but their site of action and the nature of their impact on receptor kinetics are not yet clear.
Cyclothiazide binding to functionally active AMPA receptor reveals genuine allosteric interaction with agonist binding sites
2004, Neurochemistry InternationalInteractions between recording technique and AMPA receptor modulators
2002, Brain ResearchCitation Excerpt :This is not entirely unexpected. Binding studies have shown that AMPA receptor kinetics, and the degree to which they are affected by cyclothiazide [16], are uncommonly sensitive to membrane variables (e.g. Ref. [25]). As hypothesized above, changes in the activity of protein kinases and/or phosphatases brought about by whole cell clamp recording could affect AMPA receptors.
5′-Alkyl-benzothiadiazides: A new subgroup of AMPA receptor modulators with improved affinity
2002, Bioorganic and Medicinal ChemistryCitation Excerpt :This may also account for the observations that cyclothiazide and D1 produced very different changes in many receptor properties. For one, D1 increased binding of [3H]AMPA nearly 3-fold whereas cyclothiazide reduces binding under the same assay conditions by up to 90%.34 D1 also prolonged the rate at which responses to 1-ms glutamate pulses deactivate receptors by more than 4-fold, whereas cyclothiazide had relatively small effects.24
This work was supported by a Grant from the Air Force Office of Scientific Research (AFOSR 92-J-0307) to G.L.
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The authors wish to thank Eli Lilly Corp. for a generous donation of cyclothiazide, Dr. Gary Rogers for graciously providing the initial cyclothiazide samples, and Jackie Porter and Marla Lay for secretarial assistance.