Quantification of 5-HT2A receptors in the human brain using [18F]altanserin-PET and the bolus/infusion approach

J Cereb Blood Flow Metab. 2003 Aug;23(8):985-96. doi: 10.1097/01.WCB.0000074092.59115.23.


The aim of the present study is to describe and validate a method for accurate quantification of 5-hydroxytryptamine (5-HT)(2A) receptors using [18F]altanserin-positron emission tomography (PET) and the bolus/infusion approach. A bolus/infusion ratio of 1.75 h aimed at attaining rapid steady state in blood and brain was predicted from previous bolus studies performed in our laboratory. The infusion schedule was tested in normal subjects (n = 10) using dynamic PET and frequent plasma sampling for 6 h. Steady state was attained in brain and plasma within 2 h, and time-activity curves remained constant for another 3 h. To represent free and nonspecifically bound [18F]altanserin and its radiolabeled metabolites only, cerebellum must show no displacement in 5-HT(2A) displacement studies. To validate this, saturating doses of cold ketanserin were administered and it was found that specific binding of [18F]altanserin decreased uniformly to the level of the cerebellum and no change in the cerebellar time-activity curve was found after ketanserin administration. A shorter experimental setup was tested in a second group (n = 20) including patients with neuropsychiatric disorders. Dynamic PET (five frames of 8 minutes each) and venous blood sampling at midscan time started 2 h after [18F]altanserin administration. The mean percentage rate of change per hour in the outcome parameter, DV(3)', was low (mean -0.3% h-1; range -7.3-7.2% h-1) and no correlation of DV(3)' versus time was demonstrated. It is concluded that 5-HT(2A) receptor studies can be conducted within 2 h of [18F]altanserin infusion, yielding reliable results.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Brain Chemistry*
  • Cerebellum / chemistry
  • Fluorine Radioisotopes* / administration & dosage
  • Humans
  • Injections
  • Ketanserin / administration & dosage
  • Ketanserin / analogs & derivatives*
  • Middle Aged
  • Radiochemistry
  • Receptors, Serotonin / analysis*
  • Tomography, Emission-Computed*


  • Fluorine Radioisotopes
  • Receptors, Serotonin
  • altanserin
  • Ketanserin