Molecular biology of 5-HT receptors

  title={Molecular biology of 5-HT receptors},
  author={Frank Boess and Ian L. Martin},

Pharmacology of 5-HT1A Receptors: Critical Aspects

The serotonin 1A (5-HT1A) receptor may play a far more complex role than previously believed and at least two possibilities exist to explain the diversity of pharmacology of 5-HT receptors.

Neurochemical Consequences Following Pharmacological Manipulation of Central 5-HT4 Receptors

The present chapter focuses on the neurochemical functions of central 5-HT4 receptors, a group of receptors comparable to receptor groups responsive to glutamate, GABA and acetylcholine.

5-HT3 receptors

5-HT4 Receptors: An Update

A clear biphasic doseactivation curve was obtained only with 5-carboxamidotryptamine (5-CT), which had high (13nM) and low (3000 nM) affinities for 5- HT (RH) and 5-HT (RL) receptors, respectively.

5-HT(4) receptor antagonists: structure-affinity relationships and ligand-receptor interactions.

This article will review the development of the most important classes of 5-HT(4R) antagonists with an emphasis on benzimidazole derivatives, their structure-affinity relationships, ligand-receptor interactions and pharmacological applications.

In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors.

This review was undertaken to summarize the results of structure-activity relationship studies with ligands of 5-HT5, 5- HT6 and5-HT7 receptors and some data on localization, pharmacological properties and the functional role of those receptors were reported.

Pharmacological and molecular characterization of 5-hydroxytryptamine(7) receptors in the rat adrenal gland.

Correlation analysis between the potencies of the different compounds in the model and those previously reported for various recombinant 5-HT receptors showed that the rat adrenal 5- HT receptor exhibits the same pharmacological profile as the5-HT(7) receptor transiently expressed in COS-7 cells.

Neuropharmacology of 5-HT3 Receptor Ligands

The present chapter reviews the beginnings of a pharmacological understanding of this receptor and the therapeutic implications of drugs which have affinity for it.

Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity.

The results suggest that these compounds (including the widely used 5- HT2 agonists DOB and DOI) are 5-HT1C/5-HT2 agents.



The pharmacology and function of 5-HT3receptors

Distribution of Serotonin Receptors

The results obtained with autoradiographic techniques in the analysis of 5- HT receptors in the brain and their contribution to the understanding of the multiplicity of receptors where 5-HT acts to produce its diverse effects are reviewed.

Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.

The affinity of a compound for the 5-HT2F receptor at 37 degrees versus 0 degree was shown to be useful for predicting agonist or antagonist activity, and information is provided about some of the structural requirements for the affinity of certain tryptamines at the 4-HT/1C receptor family.

5-HT3 receptors are membrane ion channels

The first recordings of currents through single ion channels activated by 5-HT3 receptors are reported, in excised membrane patches from neurons of the guinea pig submucous plexus, implying a role for 5- HT, and perhaps other amines, as a 'fast' synaptic transmitter.

Pharmacological characterization of two 5-hydroxytryptamine receptors coupled to adenylate cyclase in guinea pig hippocampal membranes.

The characteristics of RH suggest that it is a functional correlate of the 5-HT1A-binding site in brain, and the relatively low affinities of the selective 5- HT antagonists ketanserin and MDL 72222 for RH and RL indicate that neither receptor may be classified as the5-HT2 or as the 4-HT3 (i.e., peripheral neuronal) type.

Identification and distribution of 5-HT3 receptors in rat brain using radioligand binding

Direct evidence for the existence of 5-HT3 receptors in rat brain tissue and their distribution is reported, based on high affinity binding of the potent 5- HT3 receptor antagonist 3H-GR65630 to homogenates of rat entorhinal cortex.

Pharmacological characterization of 5-hydroxytryptamine4(5-HT4) receptors positively coupled to adenylate cyclase in adult guinea pig hippocampal membranes: effect of substituted benzamide derivatives.

It is shown that 4-amino-5-chlor-2-methoxy-benzamide derivatives are agonists of 5-HT4 receptors in guinea pig hippocampal membranes, and their effects on the adenylate cyclase of these membranes are not additive with those of5-HT but are additive with Those of RU 24969, a typical 5- HT1 agonist.

5-Hydroxytryptamine4-like receptors mediate the slow excitatory response to serotonin in the rat hippocampus.

Clear differences are established between the 5-HT receptor(s) mediating the depolarization and reduction in the afterhyperpolarization in the hippocampus and the5-HT3 and 5- HT1p receptors and its classification in the 5 -HT4 class is suggested.

Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization.

The 5-HT5A gene colocalized with the mouse mutation reeler and the human mutation holoprosencephaly type 3, which both result in abnormal brain development, raising the possibility that the 5- HT5A receptor plays a role in brain development.

Identification of presynaptic serotonin autoreceptors using a new ligand: 3H-PAT

3H-PAT seems to be a useful ligand for studying the biochemical and pharmacological characteristics of presynaptic autoreceptors in selected regions of rat brain.