The concept of selectivity in 5-HT receptor research.
Article Details
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van Wijngaarden I, Tulp MT, Soudijn W
The concept of selectivity in 5-HT receptor research.
Eur J Pharmacol. 1990 Jun 12;188(6):301-12.
- PubMed ID
- 2164935 [ View in PubMed]
- Abstract
Since the demonstration that serotonin (5-hydroxytryptamine, 5-HT) interacts with different (sub)types of membrane receptors, several compounds have been proposed as potent and selective ligands for one of these 5-HT subtypes. Unfortunately, specific and highly selective ligands (selectivity ratios greater than or equal to 1000) for the majority of 5-HT subtypes are still lacking. A few compounds are selective (ratios greater than or equal to 100), but most of the reputed 'selective' tools display affinities for other 5-HT subtypes and/or other (neuro-) transmitter receptors. Mainly due to different interpretations of the concept of selectivity, many of these nonselective compounds are still used to characterize 5-HT receptors. In this paper, we present the affinities (obtained by radioligand binding studies) of the most selective tools known today for each of the 5-HT subtypes and discuss the structure-activity relationships of some interesting series. The potential use of several of these selective ligands as pharmacological tools and therapeutics will be briefly reviewed.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Ondansetron 5-hydroxytryptamine receptor 1A Protein Humans UnknownOther/unknownDetails Ondansetron 5-hydroxytryptamine receptor 1B Protein Humans UnknownOther/unknownDetails Ondansetron 5-hydroxytryptamine receptor 4 Protein Humans UnknownAgonistDetails Ondansetron Mu-type opioid receptor Protein Humans UnknownOther/unknownDetails