The main features of central 5-HT1 receptors.

Article Details

Citation

Hamon M, Lanfumey L, el Mestikawy S, Boni C, Miquel MC, Bolanos F, Schechter L, Gozlan H

The main features of central 5-HT1 receptors.

Neuropsychopharmacology. 1990 Oct-Dec;3(5-6):349-60.

PubMed ID
2078271 [ View in PubMed
]
Abstract

The 5-HT1 receptor family comprises five different pharmacologic subtypes, designated 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, and 5-HT1E, whose common property is to bind 5-HT with nanomolar affinity. Recent investigations with molecular biology approaches led to the cloning and sequencing of 5-HT1A receptors in the rat and in the human, and of the 5-HT1C receptor in the rat. Although the 5-HT1A and 5-HT1C protein binding subunits exhibit the same structure with seven hydrophobic transmembrane domains, an extracellular N terminal and an intracellular C tail, their respective amino-acid sequences are markedly different. Indeed, a higher degree of sequence homology is found between the 5-HT1C and 5-HT2 receptors than between the former and 5-HT1A receptors, suggesting that the 5-HT1C subtype in fact belongs to the 5-HT2 class of central 5-HT receptors. All other 5-HT1 receptor subtypes are negatively coupled to adenylyl cyclase, whereas the 5-HT1C subtype, like 5-HT2 receptors, is positively coupled to phospholipase C. The respective regional distributions and regulatory properties, as well as pending questions regarding the ultrastructural localization, synthesis, mutual interactions, and axonal flow of 5-HT1 receptor subtypes, are also discussed.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
Buspirone5-hydroxytryptamine receptor 1AKi (nM)30N/AN/ADetails
Lesopitron5-hydroxytryptamine receptor 1AKi (nM)50N/AN/ADetails
Pindolol5-hydroxytryptamine receptor 1AKi (nM)15N/AN/ADetails
Propranolol5-hydroxytryptamine receptor 1AKi (nM)55N/AN/ADetails