Related Experiment Video
Updated: Feb 12, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Tachykinin Receptors and their Antagonists: Unraveling Their Role in Metabolic Disorders and Therapeutic Innovations
Waquar Ahsan1, Sadique A Javed1, Asim Najmi1
1Department of Pharmaceutical Chemistry and Pharmacognosy, College of Pharmacy, Jazan University, P.O. Box 114, Jazan, Saudi Arabia.
Introduction:
Metabolic disorders are major global health concerns with increasing prevalence worldwide. Experimental evidence suggests the role of tachykinins and their receptors in metabolic regulation, neuroendocrine control, and inflammatory responses. This review aims to explore the implications of tachykinin receptors and their antagonists in the management of metabolic disorders.
Methods:
A comprehensive literature search was performed across major scientific databases to identify and analyze preclinical and clinical studies on tachykinin receptors and their antagonists in the context of metabolic disorders. The key mechanisms of action of drugs, important therapeutic outcomes, and challenges associated with drug development were covered.
Results:
The reported experimental and clinical studies suggest that the antagonists of NK1R, NK2R, and NK3R could influence glucose metabolism, lipid homeostasis, and appetite regulation. While NK1R antagonists, such as aprepitant, demonstrated anti-inflammatory and neuroprotective effects, NK3R antagonists, including fezolinetant, showed promise in modulating energy balance and thermoregulation.
Discussion:
These studies emphasized the emerging potential of tachykinin receptors and their antagonists in the management of metabolic dysfunctions. However, the challenges associated with its clinical translation, including receptor redundancy, limited biomarker-based patient stratification, and variations in receptor expression across species, are still relevant and need to be addressed to improve therapeutic outcomes.
Conclusion:
Tachykinin receptor antagonists hold significant potential as therapeutic agents in the management of metabolic disorders. Further studies are warranted to overcome translational barriers, address safety issues, validate biomarkers, and refine receptor selectivity to achieve maximum therapeutic benefits.
More Related Videos
Related Concept Videos
Cholinergic Antagonists: Therapeutic Uses
Respiratory Tract: Ipratropium, aclidinium, and tiotropium treat asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD). They protect against bronchoconstriction caused by irritants like cigarette smoke, sulfur dioxide, and ozone. They also help reduce nasopharyngeal...
Drug-Receptor Interaction: Antagonist
Antagonists can be classified as competitive or noncompetitive based on their...
Antiasthma Drugs: Muscarinic Receptor Antagonists
Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...
Adrenergic Antagonists: ɑ and β-Receptor Blockers
Drugs Affecting GI Tract Motility: Dopamine Receptor Antagonists
Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally,...

