A novel kainate receptor ligand : Pharmacological characterization in rabbit brain membranes
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Cited by (27)
In vivo seizure induction and pharmacological preconditioning by domoic acid and isodomoic acids A, B and C
2008, NeuropharmacologyCitation Excerpt :Thus it is entirely possible that Iso-B has virtually zero potency. Our affinity results for KA and DA are consistent with numerous radioligand binding studies of KA receptors in mammalian brain (Hampson et al., 1992; Smith and McIlhinney, 1992; Hawkins et al., 1995; Toms et al., 1997; Crawford et al., 2000). Binding studies have also been used to characterize several stereoisomers of domoic acid (including Iso-D, Iso-E and Iso-F) and indicate that the conformation of the side chain at position C-4 of the prolyl ring critically affects the high affinity interaction of domoic acid and its isomers at kainic acid binding sites (Hampson et al., 1992).
Reduction in functional potency of the neurotoxin domoic acid in the presence of cadmium and zinc ions
2005, Environmental Toxicology and PharmacologyCitation Excerpt :Of particular concern is the possibility that Ca2+ and Mg2+, which are naturally present in millimolar concentrations in cerebrospinal fluid, may also interact with DA to form low-affinity complexes. A number of laboratories have utilized radioligand binding techniques to assess the affinity of DA at AMPA and KA receptors and have consistently reported DA binding constants in the low nanomolar range (Hampson et al., 1992; Hawkins et al., 1995; Nielsen et al., 1995; Toms et al., 1997; Crawford et al., 2000). At the same time numerous electrophysiological studies of DA have shown that the neuroexcitatory effects of DA are most readily observed at in vitro concentrations in the high nanomolar to low micromolar range.
SYM 2081, an agonist that desensitizes kainate receptors, attenuates capsaicin and inflammatory hyperalgesia
2003, Brain ResearchCitation Excerpt :Thus, SYM 2081 is highly selective for kainate receptors but at higher concentrations binds to other glutamate receptors and may have other effects. SYM 2081’s pharmacology of binding in rabbit whole brain membranes suggested that it binds to GluR5 and GluR6 kainate receptor subunits [70], and SYM 2081 has been used to map GluR5 and GluR6 kainate receptor subunits in mouse [5] and monkey [9] brains. At higher concentrations, SYM 2081 has been shown to be a potent agonist, selective for GluR5 and GluR6 kainate receptor subunits [10,20,83].
Regional mapping of low-affinity kainate receptors in mouse brain using [<sup>3</sup>H](2S,4R)-4-methylglutamate autoradiography
2001, European Journal of Pharmacology