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2015-04-25

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cc-by (c) Garcia-Recio, S. et al., 2015
Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/97661

Biological and Pharmacological aspects of the NK1-Receptor.

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http://dx.doi.org/10.1155/2015/495704

Abstract

The neurokinin 1 receptor (NK-1R) is the main receptor for the tachykinin family of peptides. Substance P (SP) is the major mammalian ligand and the one with the highest affinity. SP is associated with multiple processes: hematopoiesis, wound healing, microvasculature permeability, neurogenic inflammation, leukocyte trafficking, and cell survival. It is also considered a mitogen, and it has been associated with tumorigenesis and metastasis. Tachykinins and their receptors are widely expressed in various human systems such as the nervous, cardiovascular, genitourinary, and immune system. Particularly, NK-1R is found in the nervous system and in peripheral tissues and are involved in cellular responses such as pain transmission, endocrine and paracrine secretion, vasodilation, and modulation of cell proliferation. It also acts as a neuromodulator contributing to brain homeostasis and to sensory neuronal transmission associated with depression, stress, anxiety, and emesis. NK-1R and SP are present in brain regions involved in the vomiting reflex (the nucleus tractus solitarius and the area postrema). This anatomical localization has led to the successful clinical development of antagonists against NK-1R in the treatment of chemotherapy-induced nausea and vomiting (CINV). The first of these antagonists, aprepitant (oral administration) and fosaprepitant (intravenous administration), are prescribed for high and moderate emesis.

Subject

Pèptids, Sistema nerviós, Farmacologia molecular, Biologia molecular

Subject (English)

Peptides, Nervous system, Molecular pharmacology, Molecular biology

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Articles publicats en revistes (Medicina)

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GARCIA RECIO, Susana and GASCÓN, Pere. Biological and Pharmacological aspects of the NK1-Receptor. BioMed Research International. 2015. Vol. 2015, num. 495704. ISSN 2314-6133. [consulted: 10 of August of 2026]. Available at: https://hdl.handle.net/2445/97661

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