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

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 o...

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Published inNeuropharmacology Vol. 32; no. 12; pp. 1325 - 1331
Main Authors BUFTON, K. E, STEWARD, L. J, BARBER, P. C, BARNES, N. M
Format Journal Article
LanguageEnglish
Published Oxford Elsevier 01.12.1993
Subjects
Aged
Aged, 80 and over
Amygdala - metabolism
Animals
Binding, Competitive
Biological and medical sciences
Caudate Nucleus - metabolism
Digestive system
Female
Granisetron - metabolism
Hippocampus - metabolism
Humans
Kinetics
Male
Medical sciences
Middle Aged
Nucleus Accumbens - metabolism
Organ Specificity
Pharmacology. Drug treatments
Prosencephalon - metabolism
Putamen - metabolism
Receptors, Serotonin - analysis
Receptors, Serotonin - metabolism
Tumor Cells, Cultured
Vagus Nerve - metabolism
Human
Serotonin antagonist
Central nervous system
S3 receptor
Basal ganglion
Vagus nerve
Pharmacokinetics
In vitro
Putamen
Antiemetic
Brain (vertebrata)
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Summary: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.
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ISSN:0028-3908
1873-7064
DOI:10.1016/0028-3908(93)90027-Z