PET-characterization of [carbonyl-11C]WAY-100635 binding to 5-HT1A receptors in the primate brain

Psychopharmacology (Berl). 1997 Sep;133(2):196-202. doi: 10.1007/s002130050391.


[carbonyl-11C]WAY-100635 is a new radioligand which can be used with positron emission tomography (PET) to provide high contrast delineation of human brain regions that are rich in 5-HT1A receptors. In the present PET study, the binding of [carbonyl-11C]WAY-100635 was characterized in the cynomolgus monkey brain. Pretreatment with each of the two reference compounds, WAY-100635 and 8-OH-DPAT, as well as the drugs buspirone and pindolo, induced a marked inhibition of [carbonyl-11C]WAY-100635 binding in the neocortex and the raphe nuclei. A preliminary Scatchard analysis yielded 5-HT1A receptor density values of the same order as those that have been reported in vitro. The study shows that [carbonyl-11C]WAY-100635 binds specifically to 5-HT1A receptors in the primate brain and has potential for determination of 5-HT1A receptor occupancy and density in psychiatric patients.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin / metabolism
  • Animals
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Buspirone / metabolism
  • Carbon Radioisotopes
  • Cerebellum / metabolism
  • Macaca fascicularis
  • Male
  • Neocortex / metabolism
  • Pindolol / metabolism
  • Piperazines / metabolism*
  • Pyridines / metabolism*
  • Raphe Nuclei / metabolism
  • Receptors, Serotonin / metabolism*
  • Receptors, Serotonin, 5-HT1
  • Tomography, Emission-Computed


  • Carbon Radioisotopes
  • Piperazines
  • Pyridines
  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT1
  • N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • Pindolol
  • Buspirone