Bi-affinity α1-adrenoceptor binding in normal rat brain in vivo

A. Gjedde, S. Dyve, Y. J. Yang, M. McHugh, H. M. Pappius

Research output: Contribution to journalArticle

Abstract

The specific binding in rat brain in vivo of [125I]HEAT ([125I]iodo-2-[β-(4-hydroxyphenyl)ethylamino methyl), a selective α1-adrenoceptor ligand, was analyzed by a method designed to distinguish sites with different affinities. The data indicate at least two sites with different affinities for the α1-adrenoreceptor in normal rat brain in vivo: a high-affinity site with K(d) (half-saturation constant) of 3.6 ± 0.7 nM (AV ± SD), and a low-affinity site with K(d) of 668 ± 552 nM. The density (B(max)) of the high-affinity site in nine brain regions - auditory, visual, sensorimotor (four layers) and frontal cortex and lateral thalamic and medial geniculate nuclei - varied from 2.2 ± 0.8 to 14.6 ± 0.6 pmole/g, while the low-affinity range was 149 ± 44 to 577 ± 30 pmole/g. The results also revealed a very dynamic relationship between the two sites regulated by the concentration of the ligand ranging from 80% preponderance of the high-affinity sites at low ligand concentrations to more than 95% preponderance of the low-affinity sites at high ligand concentrations.

Original languageEnglish (US)
Pages (from-to)1-6
Number of pages6
JournalSynapse
Volume9
Issue number1
DOIs
StatePublished - 1991
Externally publishedYes

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Adrenergic Receptors
Geniculate Bodies
Ligands
Brain
Frontal Lobe

ASJC Scopus subject areas

  • Neuroscience(all)
  • Physiology
  • Pharmacology

Cite this

Gjedde, A., Dyve, S., Yang, Y. J., McHugh, M., & Pappius, H. M. (1991). Bi-affinity α1-adrenoceptor binding in normal rat brain in vivo. Synapse, 9(1), 1-6. https://doi.org/10.1002/syn.890090102

Bi-affinity α1-adrenoceptor binding in normal rat brain in vivo. / Gjedde, A.; Dyve, S.; Yang, Y. J.; McHugh, M.; Pappius, H. M.

In: Synapse, Vol. 9, No. 1, 1991, p. 1-6.

Research output: Contribution to journalArticle

Gjedde, A, Dyve, S, Yang, YJ, McHugh, M & Pappius, HM 1991, 'Bi-affinity α1-adrenoceptor binding in normal rat brain in vivo', Synapse, vol. 9, no. 1, pp. 1-6. https://doi.org/10.1002/syn.890090102
Gjedde, A. ; Dyve, S. ; Yang, Y. J. ; McHugh, M. ; Pappius, H. M. / Bi-affinity α1-adrenoceptor binding in normal rat brain in vivo. In: Synapse. 1991 ; Vol. 9, No. 1. pp. 1-6.
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