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}
}
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511 Citations
Highly Influential Citations
58
Background Citations
185
Methods Citations
49
Results Citations
19

511 Citations

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.

SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety

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.

Antiobesity-like effects of the 5-HT2C receptor agonist WAY-161503

Studies on the role of 5-HT2C and 5-HT2B receptors in regulating generalised seizure threshold in rodents.

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.
...

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