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• W1537367071 abstract "Serotonin (5-HT)2C receptors play a major role in the regulation of mood, and alteration of their functional status has been implicated in the etiology of affect disorders. Correspondingly, they represent an important target for various antidepressant categories, including tricyclics, tetracyclics, mCPP derivatives, specific serotonin reuptake inhibitors, and agomelatine, which exhibit medium to high affinities for 5-HT2C receptors and behave as antagonists. Antidepressant effects of 5-HT2C antagonists have been attributed to a disinhibition of mesocorticolimbic dopaminergic pathways, which exert a beneficial influence upon mood and cognitive functions altered in depression. However, recent experimental evidence revealed a prominent role of constitutive activity in the tonic inhibitory control of dopaminergic transmission exerted by 5-HT2C receptors in specific brain areas such as the nucleus accumbens. Accordingly, alteration in the constitutive activity of 5-HT2C receptors might participate in the induction of depressed states and drugs with inverse agonist properties should themselves be effective antidepressant agents and, possibly, more active than neutral antagonists. This highlights the relevance of systematically evaluating inverse agonist versus neutral antagonist activities of antidepressants acting at 5-HT2C receptors. Here, we provide a detailed description of a palette of cellular assays exploiting constitutive activity of 5-HT2C receptor expressed in heterologous cells (such as HEK-293 cells) toward Gq-operated signaling or their constitutive association with β-arrestins to evaluate inverse agonist activity of antidepressants. We also describe an approach allowing discrimination between inverse agonist and neutral antagonist activities of antidepressants at native constitutively active receptors expressed in cultured cortical neurons, based on previous findings indicating that prolonged treatments with inverse agonists, but not with neutral antagonists, induce functional 5-HT2C receptor-operated Ca2+ responses in neurons." @default.
• W1537367071 created "2016-06-24" @default.
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• W1537367071 date "2010-01-01" @default.
• W1537367071 modified "2023-10-03" @default.
• W1537367071 title "Techniques for Studying Inverse Agonist Activity of Antidepressants at Recombinant Nonedited 5-HT2C-INI Receptor and Native Neuronal 5-HT2C Receptors" @default.
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• W1537367071 doi "https://doi.org/10.1016/b978-0-12-381296-4.00004-x" @default.
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