Related Experiment Video
Updated: Jul 4, 2025

Ex Vivo Release of Calcitonin Gene-Related Peptide from the Trigeminovascular System in Rodents
Published on: May 16, 2022
Advances in the research and application of neurokinin-1 receptor antagonists
Xiangyu Hong1, Junjie Ma1, Shanshan Zheng1
1College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China.
Abstract:
Recently, the substance P (SP)/neurokinin-1 receptor (NK-1R) system has been found to be involved in various human pathophysiological disorders including the symptoms of coronavirus disease 2019 (COVID-19). Besides, studies in the oncological field have demonstrated an intricate correlation between the upregulation of NK-1R and the activation of SP/NK-1R system with the progression of multiple carcinoma types and poor clinical prognosis. These findings indicate that the modulation of SP/NK-1R system with NK-1R antagonists can be a potential broad-spectrum antitumor strategy. This review updates the latest potential and applications of NK-1R antagonists in the treatment of human diseases and cancers, as well as the underlying mechanisms. Furthermore, the strategies to improve the bioavailability and efficacy of NK-1R antagonist drugs are summarized, such as solid dispersion systems, nanonization, and nanoencapsulation. As a radiopharmaceutical therapeutic, the NK-1R antagonist aprepitant was originally developed as radioligand receptor to target NK-1R-overexpressing tumors. However, combining NK-1R antagonists with other drugs can produce a synergistic effect, thereby enhancing the therapeutic effect, alleviating the symptoms, and improving patients quality of life in several diseases and cancers.
Insights
The substance P (SP)/neurokinin-1 receptor (NK-1R) system is implicated in diseases like COVID-19 and cancer. NK-1R antagonists show promise as broad-spectrum antitumor agents, with strategies to enhance their efficacy.
Area of Science:
- Pharmacology
- Oncology
- Neuroscience
Background:
- The substance P (SP)/neurokinin-1 receptor (NK-1R) system is increasingly recognized for its role in various pathophysiological conditions, including COVID-19 symptoms and cancer progression.
- Upregulation of NK-1R and SP/NK-1R system activation correlate with multiple carcinoma types and poorer clinical outcomes.
Conclusions:
- Modulation of the SP/NK-1R system via antagonists offers a promising therapeutic avenue for various diseases and cancers.
- Enhancing drug delivery and combining therapies can improve the efficacy of NK-1R antagonists.
- NK-1R antagonists hold potential for alleviating symptoms and improving patient quality of life.
More Related Videos
Related Concept Videos
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
Drug-Receptor Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous...
Drug-Receptor Interaction: Antagonist
Antagonists can be classified as competitive or noncompetitive based on their...
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists
Adrenergic Agonists: Therapeutic Uses
Emergency and Intensive Care Unit (ICU) applications: Pressor agents increase blood pressure, heart rate, and contractility in shock and organ failure situations. Dopamine can induce vasodilation and stimulate adrenoceptors. Endogenous catecholamines are effective in treating cardiogenic shock. α2-agonists like clonidine can reverse anesthesia-induced hypertension.
Allergies and...

