title: Biological and Pharmacological Aspects of the NK1-Receptor.
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.
authors.affiliation: Laboratori d'Oncologia Molecular i Traslacional, Fundació Clínic per a la Recerca Biomèdica, 08036 Barcelona, Spain ; Departament de Medicina, Universitat de Barcelona, 08036 Barcelona, Spain.
authors.forename: Susana
authors.initials: S
authors.lastname: Garcia-Recio
authors.affiliation: Laboratori d'Oncologia Molecular i Traslacional, Fundació Clínic per a la Recerca Biomèdica, 08036 Barcelona, Spain ; Departament de Medicina, Universitat de Barcelona, 08036 Barcelona, Spain.
authors.forename: Pedro
authors.initials: P
authors.lastname: Gascón
mesh_terms: D000818:Animals; D006801:Humans; D008954:Models, Biological; D058990:Molecular Targeted Therapy; D018040:Receptors, Neurokinin-1 / Q000737:chemistry / Q000378:metabolism*; D015320:Tachykinins / Q000378:metabolism
chemical_list: D018040:Receptors, Neurokinin-1; D015320:Tachykinins