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ABSTRACT
Introduction
The tachykinin family of peptides (substance P, neurokinin A) via the neurokinin-1 (NK-1), NK-2, and NK-3 receptors is involved in many physiological/physiopathological actions. Antagonists of these receptors may be used to treat many human pathologies.
Areas covered
This review offers an overview (from 2014 to present) of the actions exerted by NK receptor (NK-R) antagonists on emesis, pruritus, cardiomyopathy, respiratory tract diseases, bacterial infection, cancer, ocular pain, corneal neovascularization, excess of body fat/weight, conditioned fear, social isolation stress, hot flush, melanogenesis, follicle development, fish reproduction, and sex-hormone-dependent diseases.
Expert opinion
From 2014, no invention has been published using NK-2R antagonists. Although the tachykinin/NK receptor system is involved in a great number of mechanisms, to date, the use of only five NK-1R antagonists have been approved in humans but no NK-2R or NK-3R antagonist. NK receptor antagonists are safe in human trials and are potential therapeutic agents, but this potential is currently minimized. In humans, more studies on molecules acting as NK receptor antagonists and exerting a potential therapeutic action must be carried out. The antipruritic or antitumor action of NK-1R antagonists must be explored in greater depth: the highest safe dose and the time of administration (for a long period of time) of these antagonists must be well established.
Article highlights
The tachykinin/neurokinin receptor system is involved in the molecular bases of many human physiological and pathophysiological actions.
Patents using NK-1R antagonist to treat bacterial infection, cancer, cardiomyopathy, cough, emesis, pruritus, ocular pain, corneal neovascularization, and respiratory tract diseases; and those using NK-3R antagonist to treat conditioned fear, hot flushes, excess of body fat/weight, and NK-3R-mediated disorders have been reported.
Patents using dual NK-1R/NK-3R antagonists to treat sex-hormone dependent diseases or leptin/weight-related diseases were reported, as well as the action of NK-1R or NK-3R antagonists on melanogenesis, fish reproduction, and follicle development.
To date, only five NK-1R antagonists have been approved in humans but no NK-2R/NK-3R antagonist. The potential use of NK receptor antagonists is currently minimized. However, these antagonists are an excellent opportunity to potentially treat many human pathologies: the antitumor and antipruritic effects of NK-1R antagonists must be investigated and explored in greater depth.
To treat pruritus and cancer, the dose of the NK-1R antagonist (e.g. aprepitant) and the number of days administered (compared to standard clinical practice) might be increased: the highest therapeutic safe dose and the number of days of interrupted administration must be well established.
Acknowledgments
The authors wish to thank Mr. Vipin Patel (University of Birmingham, UK) for stylistic revision of the English text and Dr. Miguel E. Muñoz and Mr. Javier Muñoz (University of Seville, Spain) for technical assistance.
Reviewer disclosures
Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.
Declaration of interest
M Muñoz declares that he has a USPTO Application no. 20090012086 ‘Use of non-peptide NK-1 receptor antagonists for the production of apoptosis in tumor cells’. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.