Functional Selectivity and Antidepressant Activity of Serotonin 1A Receptor Ligands
AbstractSerotonin (5-HT) is a monoamine neurotransmitter that plays an important role in physiological functions. 5-HT has been implicated in sleep, feeding, sexual behavior, temperature regulation, pain, and cognition as well as in pathological states including disorders connected to mood, anxiety, psychosis and pain. 5-HT1A receptors have for a long time been considered as an interesting target for the action of antidepressant drugs. It was postulated that postsynaptic 5-HT1A agonists could form a new class of antidepressant drugs, and mixed 5-HT1A receptor ligands/serotonin transporter (SERT) inhibitors seem to possess an interesting pharmacological profile. It should, however, be noted that 5-HT1A receptors can activate several different biochemical pathways and signal through both G protein-dependent and G protein-independent pathways. The variables that affect the multiplicity of 5-HT1A receptor signaling pathways would thus result from the summation of effects specific to the host cell milieu. Moreover, receptor trafficking appears different at pre- and postsynaptic sites. It should also be noted that the 5-HT1A receptor cooperates with other signal transduction systems (like the 5-HT1B or 5-HT2A/2B/2C receptors, the GABAergic and the glutaminergic systems), which also contribute to its antidepressant and/or anxiolytic activity. Thus identifying brain specific molecular targets for 5-HT1A receptor ligands may result in a better targeting, raising a hope for more effective medicines for various pathologies. View Full-Text
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Chilmonczyk, Z.; Bojarski, A.J.; Pilc, A.; Sylte, I. Functional Selectivity and Antidepressant Activity of Serotonin 1A Receptor Ligands. Int. J. Mol. Sci. 2015, 16, 18474-18506.
Chilmonczyk Z, Bojarski AJ, Pilc A, Sylte I. Functional Selectivity and Antidepressant Activity of Serotonin 1A Receptor Ligands. International Journal of Molecular Sciences. 2015; 16(8):18474-18506.Chicago/Turabian Style
Chilmonczyk, Zdzisław; Bojarski, Andrzej J.; Pilc, Andrzej; Sylte, Ingebrigt. 2015. "Functional Selectivity and Antidepressant Activity of Serotonin 1A Receptor Ligands." Int. J. Mol. Sci. 16, no. 8: 18474-18506.