Molecular, pharmacological and functional diversity of 5-HT receptors

@article{Hoyer2002MolecularPA,
  title={Molecular, pharmacological and functional diversity of 5-HT receptors},
  author={Daniel Hoyer and Jason P. Hannon and Graeme R. Martin},
  journal={Pharmacology Biochemistry and Behavior},
  year={2002},
  volume={71},
  pages={533-554}
}
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Molecular biology of 5-HT receptors

Serotonin receptors nomenclature

5-HT3 receptors.

The 5-HT(3) receptor is a member of the Cys-loop family of ligand-gated ion channels that is located in both the peripheral and central nervous systems and the pharmacophore is reasonably well understood.

5-HT1A receptors and memory

5-HT2A Receptors in the Central Nervous System

A thorough pharmacological analysis of the available data arguing in favour of the involvement of constitutive activity of 5-HT2A receptors, mostly in learning tasks is proposed and the functional significance of such an activity is discussed.

5-Hydroxytryptamine Receptors

5-HT 7 Receptors as Favorable Pharmacological Targets for Drug Discovery

Hypotheses driving current research strongly indicate an involvement in mood regulation, suggesting the 5-HT7 receptor as a putative target in the treatment of depression.

Distribution of 5-HT Receptors in the Central Nervous System

Pharmacological Analysis in Favour of a Physiological Role for the Constitutive Activity of 5-HT 2A Receptors in Learning

A thorough pharmacological analysis of the available data arguing in favour of the involvement of constitutive activity of 5-HT2A receptors, mostly in learning tasks is proposed and the functional significance of such an activity is discussed.

Functional, molecular and pharmacological advances in 5-HT7 receptor research.

...

References

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International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin).

It is evident that in the last decade or so, a vast amount of new information has become available concerning the various 5-HT receptor types and their characteristics, and it is important to rationalise in concert all of the available data from studies involving both operational approaches of the classical pharmacological type and those from molecular and cellular biology.

5-Hydroxytryptamine (5-HT)4 receptors and central nervous system function: an update.

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The 5-hydroxytryptamine (5-HT; serotonin)4 receptor is one of three 5-HT receptor subtypes that couple positively to adenylyl cyclase, the others being the 5- HT6 and 5-ht7 receptors, which are distinct and have differing distributions and function.

Molecular biology of 5-HT receptors

Characterization of human serotonin 1D and 1B receptors using [ 3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist

The binding properties of [3H]-GR-125743, a new radiolabelled derivative of a compound that exhibits selective antagonistic properties with respect to the serotonin human (h5-HT1D) and human ( h5- HT1B) receptors are described.

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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.

The 5-HT3B subunit is a major determinant of serotonin-receptor function

Surprisingly, the M2 region of the 5-HT3B subunit lacks any of the structural features that are known to promote the conductance of related receptors, and will be a valuable resource for defining the molecular mechanisms of ion-channel function.

Molecular biology and potential functional role of 5-HT5, 5-HT6, and 5-HT7 receptors

This review focuses on the structural features, binding properties, and mRNA distribution of these novel 5-HT receptor subtypes, as well as an evaluation of the tool sets available to link these cloned receptors to function and therapeutic potential.

The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists.

A number of substituted indole carbazimidamides were prepared and evaluated as 5-HT4 receptor agonists by using the isolated field-stimulated guinea pig ileum preparation and several selective and highly potent full as well as partial agonists emerged.

Medicinal Chemistry of 5-HT4 Receptor Ligands

This chapter describes the significant progress made in the medicinal chemistry of 5-HT4 receptor ligands subsequent to the identification of these early leads which has resulted in the discovery of potent and selective 5- HT4 receptor agonists and antagonists, several of which are currently undergoing clinical evaluation.
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