Up-regulation of striatal adenosine A(2A) receptors in schizophrenia

Neuroreport. 2003 Mar 3;14(3):313-6. doi: 10.1097/00001756-200303030-00003.

Abstract

Adenosine A (2A) receptors have been implicated in the pathophysiology of schizophrenia by clinical, anatomical, biochemical and genetic studies. We hypothesized that a genetically determined low number of adenosine A (2A) receptors could be a vulnerability factor for the development of the disease. The density of adenosine A (2A) receptors was investigated in human postmortem striatum of patients with schizophrenia (n = 9) and matched controls ( n= 9) using [ H)CGS 21680 as a radioligand probe. The maximum number of binding sites (B) (max) was 70% higher in patients with schizophrenia than in matched controls (609.4 +/- 259.1 354.0 +/- 156.4 fmol/mg protein, p=0.04). No significant difference could be discerned for the affinity of caffeine for adenosine A receptors between patients and controls. The increase in receptor density correlated with the dose of antipsychotic medication in chlorpromazine equivalents (r =0.61, = 0.014). We failed to provide evidence for a genetically determined reduction of adenosine A 2(A) receptors in schizophrenia. Instead, consistent with findings from animal experiments, our observation supports a role of adenosine A (2A) receptors in the molecular effects of antipsychotic drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / metabolism
  • Aged
  • Aged, 80 and over
  • Antipsychotic Agents / therapeutic use
  • Cadaver
  • Caffeine / metabolism
  • Control Groups
  • Corpus Striatum / metabolism*
  • Female
  • Humans
  • Male
  • Middle Aged
  • Phenethylamines / metabolism
  • Purinergic P1 Receptor Agonists
  • Receptor, Adenosine A2A
  • Receptors, Purinergic P1 / metabolism*
  • Schizophrenia / drug therapy
  • Schizophrenia / metabolism*
  • Up-Regulation

Substances

  • Antipsychotic Agents
  • Phenethylamines
  • Purinergic P1 Receptor Agonists
  • Receptor, Adenosine A2A
  • Receptors, Purinergic P1
  • 2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine
  • Caffeine
  • Adenosine