Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation

@article{Plvimki1998DeramciclaneAP,
  title={Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation},
  author={E. P{\"a}lvim{\"a}ki and H. Majasuo and M. Kuoppam{\"a}ki and P. M{\"a}nnist{\"o} and E. Syv{\"a}lahti and J. Hietala},
  journal={Psychopharmacology},
  year={1998},
  volume={136},
  pages={99-104}
}
Abstract Deramciclane (EGIS-3886) is a novel anxiolytic agent that binds with high affinity to 5-HT2A/2C receptors. The interactions of deramciclane with the serotonin 5-HT2C receptor were characterized further using receptor phosphoinositide hydrolysis assays and receptor autoradiography. Deramciclane antagonized 5-HT2C receptor mediated 5-HT-stimulated phosphoinositide hydrolysis with an IC50 value of 168 nM. Deramciclane also decreased basal phosphoinositide hydrolysis by up to 33% (EC50… Expand
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