Distribution and characterization of the [3H]granisetron-labelled 5-HT3 receptor in the human forebrain

Neuropharmacology. 1993 Dec;32(12):1325-31. doi: 10.1016/0028-3908(93)90027-z.


The present study has demonstrated the distribution of [3H]granisetron-labelled 5-HT3 receptors in the human forebrain with relatively high levels of this receptor in homogenates of hippocampus, caudate nucleus, putamen, nucleus accumbens and amygdala. Lower levels of 5-HT3 receptors were found in other brain regions and the cervical vagus nerve. Pharmacological characterization of the labelled 5-HT3 receptor in human putamen homogenates identified a relatively low affinity for d-tubocurarine compared to the 5-HT3 receptor in NG108-15 neuroblastoma-glioma cell homogenates. In contrast, the affinities of 19 other 5-HT3 receptor ligands were not significantly different for the [3H]granisetron-labelled receptor in these two preparations. Such findings indicate that the human putamen 5-HT3 receptor displays a unique pharmacology which may have significance given the reported clinical potential of compounds active at this receptor when assessed in animal models of disease.

MeSH terms

  • Aged
  • Aged, 80 and over
  • Amygdala / metabolism
  • Animals
  • Binding, Competitive
  • Caudate Nucleus / metabolism
  • Female
  • Granisetron / metabolism*
  • Hippocampus / metabolism
  • Humans
  • Kinetics
  • Male
  • Middle Aged
  • Nucleus Accumbens / metabolism
  • Organ Specificity
  • Prosencephalon / metabolism*
  • Putamen / metabolism
  • Receptors, Serotonin / analysis*
  • Receptors, Serotonin / metabolism*
  • Tumor Cells, Cultured
  • Vagus Nerve / metabolism


  • Receptors, Serotonin
  • Granisetron