The Structure and Function of Neurotransmitter Receptors and Transporters: From Molecular Biology to Translational Research

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Biomacromolecules: Proteins, Nucleic Acids and Carbohydrates".

Deadline for manuscript submissions: 31 May 2026 | Viewed by 12639

Special Issue Editor


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Guest Editor
Department of Biomedical Sciences, Humanitas University, Pieve Emanuele, 20072 Milan, Italy
Interests: quantal release of neurotransmitters through electrophysiological recording and signal processing; the activity of neurotransporters through the analysis of the the currents generated by charge movements in the transporter molecule

Special Issue Information

Dear Colleagues,

Transmembrane proteins are essential to perform two main functions for the cell: (i) preserving cellular homoeostasis by handling the translocation of relevant molecules, and (ii) detecting extracellular factors or signaling molecules and initiating appropriate intracellular responses. Neurotransmitter receptors and transporters are among the most relevant instances of this category of molecules. The first molecular structures of membrane proteins were reported in the 1980s; since then, the number of clarified structures has been growing exponentially. In the meantime, the patch clamp technique (developed in the late 1970s) has made it possible to study the functional properties of receptors and transporters and monitor the conformational changes of single molecules in real time. An ever-growing number of neurotransmitter receptor and transporter types and subgroups have been identified, pharmacologically characterized, and sequenced; polymorphisms and mutations have been spotted and characterized; and molecular dynamic studies have elucidated the details of drug interaction with these vital proteins. Altogether, a wide field of neurobiology and medicine has been generated that certainly deserves to be targeted by a collection of up-to-date contributions.

Prof. Dr. Riccardo Fesce
Guest Editor

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Keywords

  • neurotransmitters
  • receptors
  • neurotransporters
  • structure–function relationship
  • neuropharmacology

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Published Papers (2 papers)

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Research

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13 pages, 8750 KB  
Article
Type II Cells in the Human Carotid Body Display P2X7 Receptor and Pannexin-1 Immunoreactivity
by Marcos Anache, Ramón Méndez, Olivia García-Suárez, Patricia Cuendias, Graciela Martínez-Barbero, Elda Alba, Teresa Cobo, Iván Suazo, José A. Vega, José Martín-Cruces and Yolanda García-Mesa
Biomolecules 2025, 15(11), 1523; https://doi.org/10.3390/biom15111523 - 29 Oct 2025
Viewed by 910
Abstract
The carotid body is a peripheral chemoreceptor that consists of clusters of chemoreceptive type I cells, glia-like type II cells, afferent and efferent nerves, and sinusoidal capillaries and arterioles. Cells and nerves communicate through reciprocal chemical synapses and electrical coupling that form a [...] Read more.
The carotid body is a peripheral chemoreceptor that consists of clusters of chemoreceptive type I cells, glia-like type II cells, afferent and efferent nerves, and sinusoidal capillaries and arterioles. Cells and nerves communicate through reciprocal chemical synapses and electrical coupling that form a “tripartite synapse,” which allows for the process of sensory stimuli within the carotid body involving neurotransmission, autocrine, and paracrine pathways. In this network there are a variety of neurotransmitters and neuromodulators including adenosine 5′-triphosphate (ATP). Carotid body cells and nerve fibre terminals express ATP receptors, i.e., purinergic receptors. Here we used double immunofluorescence associated with laser confocal microscopy to detect the ATP receptor P2X7 and pannexin 1 (an ATP permeable channel) in the human carotid body, as well as the petrosal and cervical sympathetic ganglia. Immunofluorescence for P2X7r and pannexin 1 forms a broad cellular network within the glomeruli of the carotid body, whose pattern corresponds to that of type II cells. Moreover, both P2X7r and pannexin 1 were also detected in nerve profiles. In the petrosal ganglion, the distribution of P2X7r was restricted to satellite glial cells, whereas in the cervical sympathetic ganglion, P2X7r was found in neurons and glial satellite cells. The role of this purinergic receptor in the carotid body, if any, remains to be elucidated, but it probably provides new evidence for gliotransmission. Full article
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Review

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23 pages, 1936 KB  
Review
Enkephalins and Pain Modulation: Mechanisms of Action and Therapeutic Perspectives
by Mario García-Domínguez
Biomolecules 2024, 14(8), 926; https://doi.org/10.3390/biom14080926 - 30 Jul 2024
Cited by 15 | Viewed by 11079
Abstract
Enkephalins, a subclass of endogenous opioid peptides, play a pivotal role in pain modulation. Enkephalins primarily exert their effects through opioid receptors located widely throughout both the central and peripheral nervous systems. This review will explore the mechanisms by which enkephalins produce analgesia, [...] Read more.
Enkephalins, a subclass of endogenous opioid peptides, play a pivotal role in pain modulation. Enkephalins primarily exert their effects through opioid receptors located widely throughout both the central and peripheral nervous systems. This review will explore the mechanisms by which enkephalins produce analgesia, emotional regulation, neuroprotection, and other physiological effects. Furthermore, this review will analyze the involvement of enkephalins in the modulation of different pathologies characterized by severe pain. Understanding the complex role of enkephalins in pain processing provides valuable insight into potential therapeutic strategies for managing pain disorders. Full article
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