Analogue interactions with the brain receptor labeled by [3H]kainic acid

J. T. Slevin, J. F. Collins, J. T. Coyle

Research output: Contribution to journalArticlepeer-review

56 Scopus citations

Abstract

The kinetics of interaction of kainic acid analogues and reputed antagonists of acidic excitatory amino acids with a specific binding site for [3H]α-kainic acid were examined in washed cerebellar membranes incubated at 4°C. The avidity of both l-glutamate (1.5 μM) and quisqualate (0.6 μM) suggests that proper orientation of the two carboxyls in the amino group is essential for binding to one component of the receptor. The high affinity of domoate, α-kainate and α-keto-kainate as compared to the low affinity of dihydrokainate and α-allo-kainate indicate that a pi electron group with appropriate cis-planar orientation versus the C2-carboxyl group is essential for high affinity binding to the receptor. These studies provide additional evidence that the recognition site labeled by [3H]kainic acid represents the receptor mediating its neurophysiologic and neurotoxic effects.

Original languageEnglish
Pages (from-to)169-172
Number of pages4
JournalBrain Research
Volume265
Issue number1
DOIs
StatePublished - Apr 11 1983

Bibliographical note

Funding Information:
We thank Dorothea Stieff for excellent secretarial assistance and Karen Lindsley for technical assistance. This research was supported by USPHS Grants NS 13584, RSDA Type II MH00125, Postdoctoral Fellowship NS 06328 and a grant from the Surdna Foundation.

Keywords

  • analogue interactions
  • cerebellum
  • kainic acid

ASJC Scopus subject areas

  • Neuroscience (all)
  • Molecular Biology
  • Clinical Neurology
  • Developmental Biology

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