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Studies on the binding of [^3^H]flumazenil and [^3^H]sarmazenil in post‐mortem human brain by H. Hall; J.‐E. Litton; C. Halldin; J. Kopp; G. Sedvall is a Medicine article available to read on EtoBox.

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Two benzodiazepine analogues, [3H]flumazenil and [3H]sarmazenil, were used to study the GABA,/benzodiazepine receptor complex in human post-mortem brain using in vitro receptor assays on homogenates and whole hemisphere autoradiography. Both radioligands bound in a saturable manner to single binding sites in the tissue preparations from any brain region. The highest levels of binding were found in the cortical regions and in cortex cerebelli. Both [3H]flumazenil and [3H]sarmazenil were excellent radioligands for autoradiography with high binding in cerebral and cerebellar cortex with no or very low binding in areas with white matter. The addition of a high concentration of flumazenil or clonazepam did not inhibit the binding of [3H]sarmazenil to granule cells in the cerebellum while the binding of [3H]flumazenil was abolished completely in all regions. The results show that with the two different radioligands, one an antagonist and one a partial inverse agonist, the binding pattern to GABA&enzodiazepine receptor complex is approximately similar in most brain regions. The additional binding seen in the cerebellum with [3H]sarmazenil is suggested to be due to binding to an a,-contain

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Author

H. Hall; J.‐E. Litton; C. Halldin; J. Kopp; G. Sedvall

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0885-6222)

Published

1992

Language

EN

Field

Medicine (Health Sciences)