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Centrally active 5-HT receptor agonists and antagonists
D N Middlemiss1, M D Tricklebank
1Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK.
Neuroscience and Biobehavioral Reviews
|January 1, 1992
Summary
Selective serotonin (5-HT) receptor agonists and antagonists are discussed, focusing on their potency and selectivity. This review covers key findings for various 5-HT receptor subtypes, aiding in understanding their pharmacological profiles.
Area of Science:
- Neuroscience
- Pharmacology
- Molecular Biology
Background:
- Eleven central serotonin (5-HT) receptor subtypes have been proposed.
- Four subtypes (5-HT1A, 5-HT1C, 5-HT1D, 5-HT2) have been cloned, and one (5-HT3) purified.
Purpose of the Study:
- To review agonists and antagonists acting on central 5-HT receptor subtypes.
- To evaluate the selectivity and in vivo potency of these agents.
Main Methods:
- Literature review of existing studies on 5-HT receptor pharmacology.
- Analysis of data on agonist and antagonist activity at various 5-HT receptor subtypes.
Main Results:
- Selective agonists are available for 5-HT1A, 5-HT1B, and 5-HT3 receptors.
- Selective antagonists have been identified for 5-HT2 and 5-HT3 receptors.
Conclusions:
- Pharmacological tools with varying selectivity and potency exist for several 5-HT receptor subtypes.
- These selective agents are crucial for further research into 5-HT receptor function.