Autoradiographic characterization of alpha(2C)-adrenoceptors in the human striatum

Synapse
Veronica FagerholmJarmo Hietala

Abstract

Indirect experimental evidence suggests that drugs acting on the alpha(2C)-adrenoceptor could be useful in the treatment of neuropsychiatric disorders such as depression and schizophrenia. In rodent brain, the highest levels of alpha(2C)-adrenoceptors are found in the striatum, with lower levels in cerebral cortex and hippocampus. In human brain, because of the poor subtype-selectivity of the available alpha(2)-adrenoceptor ligands, the localization of alpha(2C)-adrenoceptors has remained unknown. Recently, a selective alpha(2C)-adrenoceptor antagonist, JP-1302, was characterized, and to assess the presence of alpha(2C)-adrenoceptors in human brain, we performed competition binding in vitro receptor autoradiography with JP-1302 and the alpha(2)-adrenoceptor subtype nonselective antagonist [ethyl-(3)H]RS79948-197 on rat and human postmortem brain sections. In striatum of both species, JP-1302 vs. [ethyl-(3)H]RS79948-197 competition binding was biphasic, identifying high- and low-affinity binding sites, whereas in cortex and cerebellum, only low-affinity binding sites were detected. The results indicate that a significant portion of the alpha(2)-adrenoceptors in striatum is of the alpha(2C) subtype, whereas non-alpha(2C)-adreocne...Continue Reading

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Citations

Feb 4, 2014·Psychopharmacology·Jan BrosdaHeinz H Pertz
Sep 10, 2014·European Journal of Nuclear Medicine and Molecular Imaging·Jussi LehtoJuha O Rinne
Apr 30, 2015·Psychopharmacology·Sjoerd J FinnemaSarah Grimwood
Dec 19, 2014·The International Journal of Neuropsychopharmacology·Sjoerd J FinnemaChrister Halldin
Mar 20, 2018·Molecular Neurobiology·Marta Sánchez-SotoSergi Ferré
Dec 8, 2020·Stress : the International Journal on the Biology of Stress·Jiayin LuYulan Dong
May 7, 2014·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Eveliina ArponenOlof Solin

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