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Molecular Biology, Pharmacology, and Genetics of the Serotonin Transporter: Psychobiological and Clinical Implications

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Serotoninergic Neurons and 5-HT Receptors in the CNS

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 129))

Abstract

Serotonin (5-HT), which acts at multiple pre- and postsynaptic receptor sites, fulfills the criteria for a neurotransmitter and modulator of synaptic signal transduction in many functional systems of the brain. As a consequence of this enormous versatility, brainstem 5-HT systems affect many diverse functions, such as mood, cognition, appetite and satiation, sleep, motor behavior, neuroendocrine and circadian rhythms, social and reproductive behavior. By determining the magnitude and duration of postsynaptic receptor-mediated signaling, carrier-facilitated 5-HT transport into and release from the presynaptic neuron plays a key role in the spatiotemporal fine-tuning of 5-HT neurotransmission (Fig. 1). Recent advances have resulted from the molecular and functional characterization of the serotonin transporter (5-HTT), from pharmacological and neurochemical studies relating the actions of psychoactive drugs (e.g., tricyclics, selective 5-HT reuptake inhibitors, psychostimulants) to discrete effects on 5-HT uptake and release, and from the molecular dissection of the complex changes in functional expression as a consequence of altered gene transcription. On the basis of its molecular structure and anatomical distribution, substrate specificity, electrophysiological properties, and drug-binding profiles the 5-HTT has been placed in the extended gene family of Na+/C1--dependent cell surface transport proteins.

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Lesch, KP. (2000). Molecular Biology, Pharmacology, and Genetics of the Serotonin Transporter: Psychobiological and Clinical Implications. In: Baumgarten, H.G., Göthert, M. (eds) Serotoninergic Neurons and 5-HT Receptors in the CNS. Handbook of Experimental Pharmacology, vol 129. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-60921-3_26

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