[3H]clonidine binds at multiple high affinity states in human prefrontal cortex

Mark A. Carlson, Anne C. Andorn

Research output: Contribution to journalArticle

13 Scopus citations

Abstract

[3H]Clonidine binds at particulate membrane fractions of human prefrontal cortex in a process that demonstrates high affinity, saturability, reversebility, α2-adrenergic selectivity and the existence of multiple affinity states. At 37°C maximal specific [3H]clonidine binding was briefly attained at 10 and lasted only until 15 min, while at 21°C maximal binding was maintained from 20 to 90 min. At 21°C, rate dissociation studies and saturation analyses were at least biphasic, and adrenergic competitors decreased [3H]clonidine binding with Hill coefficients <0.70. Analysis of these data showed at least two affinity states with apparent KDs of 0.34 and 6.0 nM, and the order in which ligands decreased [3H]clonidine binding was clonidine > (-)-epinephrine > (-) > yohimbine > (+)-norepinephrine > (±) -isoproterenol > prazosin > serotonin.

Original languageEnglish (US)
Pages (from-to)73-78
Number of pages6
JournalEuropean Journal of Pharmacology
Volume123
Issue number1
DOIs
StatePublished - Apr 9 1986

Keywords

  • Human brain
  • [H]Clonidine
  • α-Adrenoceptors

ASJC Scopus subject areas

  • Pharmacology

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