Differential Binding of Ergot Compounds to Human versus Rat 5-HT2 Cortical Receptors
Study at a glance
AI-extracted from the abstract| Characteristics | In vitro receptor binding study Peer reviewed |
|---|---|
| Population | Rat and human cortex tissue (5-HT2 receptors) |
| Measures | [3H]-ketanserin binding |
| Citations | 11 |
| Key points | Four of eleven ergot compounds (mesulergine, methysergide, nicergoline, metergoline) showed selectivity for rat 5-HT2 receptors, while seven others showed selectivity for human 5-HT2 receptors. The authors propose that a methyl substitution on the indole nitrogen marks rat-selective ergots and a hydrogen at that position marks human-selective ones, a structural feature that may allow the two groups to differentiate between the species' receptors. |
Abstract
Eleven ergot compounds were competed against [3H]-ketanserin-labelled 5-HT2 receptors in rat and human cortex. Four of the ergots are selective for rat 5-HT2 receptors--mesulergine, methysergide, nicergoline and metergoline, whereas pergolide, d-lysergic acid, ergonovine, ergotamine, d-lysergic acid diethylamide, lisuride and dihydroergotamine display selectivity for human 5-HT2 receptors. Rat-selective compounds contain a methyl substitution on the indole nitrogen, whereas human-selective compounds contain a hydrogen. This structural feature may allow the two groups of ergots to differentiate between the two species of receptors.