[3H]SCH 23390 labels a novel 5-hydroxytryptamine binding site in human blood platelet membranes
| Autor: | G. Ebinger, Hilde Walraevens, André Convents, Jacques De Keyser, G. Vauquelin |
|---|---|
| Přispěvatelé: | Gerontology |
| Rok vydání: | 1989 |
| Předmět: |
Blood Platelets
Serotonin/drug effects/*metabolism Stereochemistry receptors Mianserin Biology In Vitro Techniques Binding Competitive chemistry.chemical_compound Radioligand Assay Dopamine medicine Humans heterocyclic compounds Spiperone/pharmacology Binding site Receptor Blood Platelets/drug effects/*metabolism 5-HT receptor Pharmacology Cerebral Cortex SCH-23390 Cell Membrane/drug effects/metabolism Mianserin/pharmacology Antipsychotic Agents/*pharmacology organic chemicals Benzazepines/*pharmacology Cell Membrane Cerebral Cortex/drug effects/metabolism in vitro Biological membrane Binding Benzazepines Membrane nervous system chemistry Spiperone Receptors Serotonin Serotonin Competitive/drug effects Human medicine.drug Antipsychotic Agents |
| Zdroj: | European journal of pharmacology. 162(3) |
| ISSN: | 0014-2999 |
| Popis: | In human blood platelet membranes, 5-HT displaced the binding of the putative selective D-1 dopamine receptor antagonist [ 3 H]SCH 23390 in a competitive manner with a K i value of 5.7 ± 0.8 nM, which was about 1000-fold lower than the K i value for dopamine (K i = 4400 ± 150 nM. Thus the ‘D-1 dopamine-like’ site in human blood platelet membranes described previously corresponds to a 5-HT 1 -type site. [ 3 H]SCH 23390 competition experiments with a number of serotonergic drugs disclosed a pharmacological profile that was distinct from the four 5-HT 1 site subtypes reported previously. We therefore propose that this novel 5-HT site be designated the 5-HT 1E site. Binding of [ 3 H]SCH 23390 to 5-HT 1 -type sites could not be detected in several regions of the human brain. In some regions, however, 5-HT displaced part of the [ 3 H]SCH 23390 binding with a K 1 value of 320–380 nM. These sites correspond to 5-HT 2 receptors. |
| Databáze: | OpenAIRE |
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