SB 242084, a Selective and Brain Penetrant 5-HT2C Receptor Antagonist

  title={SB 242084, a Selective and Brain Penetrant 5-HT2C Receptor Antagonist},
  author={Guy A. Kennett and Martyn D. Wood and F. Bright and Brenda K Trail and Graham J. Riley and Valerie Holland and K Y Avenell and Tania O. Stean and Neil Upton and Steven Mark Bromidge and Ian Thomson Forbes and Arthur M. Brown and Derek N. Middlemiss and Thomas P Blackburn},

SB 242084: A Selective 5‐HT2C Receptor Antagonist

In vivo studies have shown that SB 242084 is a very effective antagonist of behavioral responses mediated by 5-HT2C receptors such as penile erections, and the hypophagic and hypolocomotor effect of mCPP in rats, and this compound has anxiolytic-like properties.

S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models

In vitro and in vivo, the novel benzourea derivative, S32006 is a potent 5-HT2C receptor antagonist, and possesses antidepressant and anxiolytic properties in diverse rodent models.

m-CPP hypolocomotion is selectively antagonized by compounds with high affinity for 5-HT receptors but not

A detailed pharmacological evaluation with selective antagonists for the 5-HT family of receptors supports a primary role for the 1m-chlorophenyl piperazine receptor in mediating the hypolocomotion produced by m-CPP.

m-CPP hypolocomotion is selectively antagonized by compounds with high affinity for 5-HT2C receptors but not 5-HT2A or 5-HT2B receptors

A detailed pharmacological evaluation with selective antagonists for the 5-HT2 family of receptors supports a primary role for the 1-(m-chlorophenyl)piperazine receptor in mediating the hypolocomotion produced by m-CPP.

5-HT-2B Receptor

5-HT3- and 5-HT2C-antagonist properties of cyamemazine: significance for its clinical anxiolytic activity

5-HT3- and 5-HT2C-antagonistic actions of cyamemazine can be involved, at least in part, in its beneficial therapeutic actions in anxiety disorders.

Pharmacological characterisation of the agonist radioligand binding site of 5-HT2A, 5-HT2B and 5-HT2C receptors

The results indicate the importance of defining the selectivity of pharmacological tools, which may have been over-estimated in the past, and highlights the need to find more selective agonists to investigate 5-HT2 receptor pharmacology.



Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes

  • R. E. HeuringS. Peroutka
  • Biology, Chemistry
    The Journal of neuroscience : the official journal of the Society for Neuroscience
  • 1987
The data demonstrate the presence of a homogeneous class of 5- HT1 binding sites in bovine caudate that is pharmacologically distinct from previously defined 5-HT1A, 5-ht1B, 5 - HT1C, 4-HT2, 3-HT3 receptor subtypes.

In vitro and in vivo profile of SB 206553, a potent 5‐HT2C/5‐HT2B receptor antagonist with anxiolytic‐like properties

The results suggest that SB 206553 is a potent mixed 5‐HT2C/5-HT2B receptor antagonist with selectivity over the 5‐ HT2A and all other sites studied and possesses anxiolytic‐like properties.

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.

Characterization and distribution of putative 5‐ht7 receptors in guinea‐pig brain

The distribution of 5‐ht7 receptors in thalamocortical and limbic brain regions suggests a role for these receptors in sensory and affective behaviours in guinea‐pig brain.

In vivo properties of SB 200646A, a 5‐HT2C/2B receptor antagonist

The results indicate that SB 200646A has in vivo efficacy and that 5‐HT2C or 5‐ HT2B receptors are indeed likely to mediate mCPP‐induced hypolocomotion, hypophagia and anxiogenesis and suggest that5‐HT 2C/2B receptor blockade induces anxiolysis.

Characterisation of Human 5‐Hydroxytryptamine2A and 5‐Hydroxytryptamine2C Receptors Expressed in the Human Neuroblastoma Cell Line SH‐SY5Y: Comparative Stimulation by Hallucinogenic Drugs

Abstract: Stable transfection of the human neuroblastoma cell line SH‐SY5Y with the human 5‐hydroxytryptamine2A (5‐HT2A) or 5‐HT2C receptor cDNA produced cell lines demonstrating ligand affinities

Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.

  • N. AdhamH. Kao T. Branchek
  • Biology, Chemistry
    Proceedings of the National Academy of Sciences of the United States of America
  • 1993
Competition studies revealed the following rank order of potencies for serotonergic ligands: 5-HT > sumatriptan >> 5-carboxyamidotryptamine > 8-hydroxy-2(di-1-propylamino)tetralin > spiperone.

Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.

Findings may help clarify several ambiguities in the classification and action of serotonin receptor subtypes.

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.