Receptor occupancy by ritanserin and risperidone measured using ex vivo autoradiography.

Brain Research
A SchotteJosée E Leysen

Abstract

In this study, autoradiographical techniques are introduced to investigate the occupancy of serotonin 5-HT2, dopamine D2 and alpha 1-adrenergic receptors after the in vivo administration of ritanserin, a selective, potent and long-acting 5-HT2 antagonist and of risperidone, a very potent 5-HT2 antagonist and potent D2 and alpha 1 antagonist. Unoccupied 5-HT2 and alpha 1-receptors were labelled with [125I]7-amino-8-iodoketanserin ([125I]AMIK) and D2 receptors with [125I]iodosulpride in horizontal rat brain section. Receptor occupancy by the drugs was quantified by image analysis of the autoradiograms. Ritanserin produced 50% occupancy of the 5-HT2 receptors at a dose of 0.02 mg/kg s.c., while at 40 mg/kg s.c. ritanserin still did not occupy 50% of the D2 and alpha 1 receptors. Risperidone occupied 50% of the 5-HT2, alpha 1 and D2 receptors at 0.0075, 0.32 and 2.5 mg/kg s.c., respectively. Ex vivo autoradiography was found to be applicable where radioligand binding techniques using brain homogenates had failed for the study of ex vivo receptor occupancy due to rapid drug dissociation. Ex vivo autoradiography is hitherto the sole technique which allowed the measurement of alpha 1 receptor occupancy by risperidone after in vivo adm...Continue Reading

Citations

Feb 1, 1994·Psychopharmacology·A A MegensJ E Leysen
Mar 1, 1996·Psychopharmacology·B J Kinon, J A Lieberman
Aug 6, 1992·European Journal of Pharmacology·A SchotteJ E Leysen
Jul 1, 1992·Pharmacology, Biochemistry, and Behavior·A D LevyL D Van de Kar
Dec 1, 1993·Pharmacology, Biochemistry, and Behavior·I PanockaM Massi
Mar 1, 1995·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·H HallG Sedvall
Mar 1, 1996·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·M M MarcusT H Svensson
Jun 29, 2000·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·M M MarcusT H Svensson
Mar 26, 2016·Progress in Neurobiology·Philippe De Deurwaerdère, Giuseppe Di Giovanni
Aug 1, 1995·Journal of Clinical Psychopharmacology·P CzoborR C Meibach
Feb 1, 1994·The British Journal of Psychiatry : the Journal of Mental Science·R W Kerwin

❮ Previous
Next ❯

Related Concepts

Related Feeds

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.