Non-adrenoceptor [3H]idazoxan binding sites (I2-imidazoline sites) are increased in postmortem brain from patients with Alzheimer's disease

Neurosci Lett. 1993 Sep 17;160(1):109-12. doi: 10.1016/0304-3940(93)90925-b.

Abstract

The I2-imidazoline site (a non-adrenergic mitochondrial site for which a glial location has been proposed and that is associated with the B-form of the enzyme monoamine oxidase) was evaluated in postmortem cortical membranes from 9 subjects with Alzheimer's disease (AD) and 9 matched-controls by using [3H]idazoxan (0.6-30 nM) in the presence of 10(-6) M (-)-adrenaline to prevent binding to alpha 2-adrenoceptors. In AD the density (Bmax) of I2-imidazoline sites was significantly higher (+63%) than in controls whereas no differences were apparent in affinity values (Kd). The results support the hypothesis that the I2 imidazoline site has a major location on glial (astrocyte) cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-Antagonists / metabolism*
  • Adrenergic alpha-Antagonists / pharmacology
  • Aged
  • Aged, 80 and over
  • Alzheimer Disease / metabolism*
  • Autoradiography
  • Dioxanes / metabolism*
  • Dioxanes / pharmacology
  • Epinephrine / pharmacology
  • Female
  • Humans
  • Idazoxan
  • Imidazoline Receptors
  • Kinetics
  • Male
  • Membranes / drug effects
  • Membranes / metabolism
  • Prefrontal Cortex / metabolism
  • Receptors, Drug / metabolism*

Substances

  • Adrenergic alpha-Antagonists
  • Dioxanes
  • Imidazoline Receptors
  • Receptors, Drug
  • Idazoxan
  • Epinephrine