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Int. J. Mol. Sci. 2015, 16(8), 18474-18506; doi:10.3390/ijms160818474

Functional Selectivity and Antidepressant Activity of Serotonin 1A Receptor Ligands

1
National Medicines Institute, Chełmska 30/34, 00-725 Warszawa, Poland
2
Institute of Nursing and Health Sciences, University of Rzeszów, W. Kopisto 2A, 35-310 Rzeszów, Poland
3
Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31-343 Kraków, Poland
4
Faculty of Health Sciences, University of Tromsø—The Arctic University of Norway, No-9037 Tromsø, Norway
*
Author to whom correspondence should be addressed.
Academic Editor: Kenji Hashimoto
Received: 2 July 2015 / Revised: 29 July 2015 / Accepted: 31 July 2015 / Published: 7 August 2015
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Abstract

Serotonin (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
Keywords: serotonin 1A receptors; receptor trafficking; antidepressant activity serotonin 1A receptors; receptor trafficking; antidepressant activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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.

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