SB 242084, a Selective and Brain Penetrant 5-HT2C Receptor Antagonist
@article{Kennett1997SB2A, 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}, journal={Neuropharmacology}, year={1997}, volume={36}, pages={609-620} }
511 Citations
SB 242084: A Selective 5‐HT2C Receptor Antagonist
- Biology, Psychology
- 2006
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
- Biology, PsychologyPsychopharmacology
- 2008
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.
SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety
- Psychology, BiologyNeuropharmacology
- 2001
m-CPP hypolocomotion is selectively antagonized by compounds with high affinity for 5-HT receptors but not
- Biology, Psychology
- 2001
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.
Antiobesity-like effects of the 5-HT2C receptor agonist WAY-161503
- Biology, ChemistryBrain Research
- 2006
Studies on the role of 5-HT2C and 5-HT2B receptors in regulating generalised seizure threshold in rodents.
- Biology, ChemistryEuropean journal of pharmacology
- 1998
m-CPP hypolocomotion is selectively antagonized by compounds with high affinity for 5-HT2C receptors but not 5-HT2A or 5-HT2B receptors
- Biology, PsychologyBehavioural pharmacology
- 2001
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-HT3- and 5-HT2C-antagonist properties of cyamemazine: significance for its clinical anxiolytic activity
- Biology, PsychologyPsychopharmacology
- 2000
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
- BiologyNaunyn-Schmiedeberg's Archives of Pharmacology
- 2004
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.
References
SHOWING 1-10 OF 36 REFERENCES
Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes
- Biology, ChemistryThe 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
- Biology, PsychologyBritish journal of pharmacology
- 1996
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
- Biology, ChemistryNature
- 1983
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
- Biology, ChemistryBritish journal of pharmacology
- 1995
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
- Biology, PsychologyBritish journal of pharmacology
- 1994
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
- Biology, ChemistryJournal of neurochemistry
- 1996
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.
- Biology, ChemistryProceedings 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.
- BiologyMolecular pharmacology
- 1991
Findings may help clarify several ambiguities in the classification and action of serotonin receptor subtypes.
Distribution of the serotonin 5-HT2 receptor family mRNAs: comparison between 5-HT2A and 5-HT2C receptors.
- BiologyBrain research. Molecular brain research
- 1994
International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin).
- BiologyPharmacological reviews
- 1994
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.