PMID: 9551765Apr 29, 1998Paper

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

Psychopharmacology
E P PälvimäkiJ Hietala

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 = 93 nM) in a physiological system in the choroid plexus, suggesting that deramciclane possesses inverse agonist properties at this receptor. Administration of single doses of 0.5 mg/kg and 10 mg/kg resulted in a maximal 5-HT2C receptor occupancy of up to 45% and 79%, respectively, in the choroid plexus. Chronic (14 days) treatment with 0.5 mg/kg or 10 mg/kg deramciclane did not alter [125I]DOI (agonist) or [3H]mesulergine (antagonist) binding to 5-HT2C receptors in the choroid plexus compared to saline-treated controls, as determined by quantitative receptor autoradiography. In comparison, the effects of deramciclane on 5-HT2A binding characteristics and receptor occupancy were also studied. Deramciclane treatment resulted in 5-HT2A receptor occupan...Continue Reading

Citations

Nov 11, 1999·European Journal of Pharmacology·I KovácsJ Kardos
Mar 13, 2002·Pharmacology, Biochemistry, and Behavior·Brian J Jones, Thomas P Blackburn
Apr 26, 2000·Brain Research Bulletin·I KovácsJ Kardos
Feb 19, 2002·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Samar Al-BehaisiImre Klebovich
Feb 19, 2002·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Kálmán MagyarImre Klebovich
Nov 20, 1998·The Journal of Pharmacy and Pharmacology·H KanervaT Nevalainen
Jul 2, 2004·American Journal of Respiratory and Critical Care Medicine·Sigrid C VeaseyDomenico Pratico
Jul 5, 2005·Expert Opinion on Investigational Drugs·F JenckJ L Moreau
Sep 29, 2004·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Sándor DrabantImre Klebovich
Mar 15, 2000·The Journal of Pharmacy and Pharmacology·K B NemesI Klebovich
Apr 13, 2000·Biopharmaceutics & Drug Disposition·H KanervaA Urtti
Jan 15, 2004·Molecular Pharmacology·Terry Kenakin
Aug 25, 2005·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Katalin MonostoryLászló Kóbori

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