Comparison of [3H]clonidine and [3H]guanfacine binding to α2 adrenoceptors in membranes from rat cerebral cortex

R. J. Summers, B. Jarrott, W. J. Louis

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Abstract

[3H]Clonidine and a new phenylacylguanidine antihypertensive drug, [3H]guanfacine, bind with a high affinity to α2 adrenoceptors in membranes from rat cerebral cortex. Dissociation curves for [3H]clonidine binding indicated the presence of high and low affinity binding sites, whereas with [3H]guanfacine, two components could be distinguished only with difficulty; the major part of the binding being to a high affinity component. Saturation experiments revealed that both ligands bind with similar high affinity but that [3H]guanfacine labels twice the number of sites labeled by [3H]clonidine.

Original languageEnglish
Pages (from-to)31-36
Number of pages6
JournalNeuroscience Letters
Volume25
Issue number1
DOIs
Publication statusPublished - 7 Aug 1981

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