The concept of selectivity in 5-HT receptor research.

Article Details

Citation

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
DrugTargetKindOrganismPharmacological ActionActions
Ondansetron5-hydroxytryptamine receptor 1AProteinHumans
Unknown
Other/unknown
Details
Ondansetron5-hydroxytryptamine receptor 1BProteinHumans
Unknown
Other/unknown
Details
Ondansetron5-hydroxytryptamine receptor 4ProteinHumans
Unknown
Agonist
Details
OndansetronMu-type opioid receptorProteinHumans
Unknown
Other/unknown
Details