Characteristics and localization of high-affinity kainate sites in slide-mounted sections of rat cerebellum.
The characteristics and localization of high-affinity, kainic acid (KA)-sensitive glutamate sites have been investigated using a radioreceptor procedure to provide insights into specific high-affinity KA receptors identified in molecular biological studies. Binding sites identified by employing [3H]KA. in the presence of the AMPA-selective antagonist NBQX (1 microM), and slide-mounted, coronal sections of rat cerebellum were of high-affinity (Kd 6 nM) and possessed an unique pharmacological profile. Specific binding was to a single population of sites and fully inhibited by kainoids and glutamate, but essentially insensitive to AMPA and willardiines. Autoradiography revealed that the high-affinity KA sites were localized to the granule cell layer of cerebellum. The KA site resembled both the KA receptor found on spinal motoneurones and the KA-2 type of receptor.
Ganakas
A M
AM
Department of Pharmacology, Monash University, Clayton, Vic., Australia.
Mercer
L D
LD
Shinozaki
H
H
Beart
P M
PM
D000818:Animals; D001345:Autoradiography; D001667:Binding, Competitive; D002531:Cerebellum / Q000166:cytology / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D018698:Glutamic Acid / Q000494:pharmacology; D007608:Kainic Acid / Q000031:analogs & derivatives / Q000378:metabolism* / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D011810:Quinoxalines / Q000494:pharmacology; D016318:Quisqualic Acid / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors; D018092:Kainic Acid Receptors / Q000032:analysis / Q000378:metabolism*; D014316:Tritium
D018698:Glutamic Acid; D007608:Kainic Acid; D011810:Quinoxalines; D016318:Quisqualic Acid; D018091:Receptors, AMPA; D018092:Kainic Acid Receptors; D014316:Tritium; C062865:2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline; C074250:4-(2-methoxyphenyl)-2-carboxy-3-pyrrolidineacetic acid; C056723:FG 9041