NK1 receptor antagonist
Neurokinin 1 (NK1) antagonist possess antidepressant, anxiolytic, and antiemetic properties.
NK-1 antagonists boost the efficacy of 5-HT3 antagonists to prevent nausea and vomiting.
Tachykinin NK1 receptor, often referred to as NK1 receptor, is a member of family of G protein-coupled receptors and binds to the Gαq protein.
NK1 receptor consists of 407 amino acid residues, and it has a molecular weight of 58.000.
An example of a drug in this class is aprepitant.
The acute phase of chemotherapy induced emesis responds to 5-HT3 antagonists while the delayed phase remains difficult to control.
NK1 receptor antagonists have antiemetic effects in both acute and especially in delayed phases of emesis.
Casopitant, netupitant and rolapitant are additions in this group.
NK1 antagonists, also known as substance P antagonists, are a class of drugs that block the activity of the neurokinin-1 (NK1) receptor.
The NK1 receptor is a type of receptor found in the central nervous system and peripheral tissues, particularly in areas associated with pain and inflammation.
Substance P is a neuropeptide that binds to the NK1 receptor and is involved in various physiological processes, including pain transmission, neurogenic inflammation, and stress responses.
By blocking the NK1 receptor, NK1 antagonists inhibit the actions of substance P, leading to a reduction in pain and inflammation.
NK1 antagonists have been studied and used in the management of several conditions, including:
Chemotherapy-induced nausea and vomiting: NK1 antagonists, such as aprepitant and fosaprepitant, are often used in combination with other antiemetic drugs to prevent nausea and vomiting caused by chemotherapy.
Mental health disorders: Substance P has been implicated in the regulation of mood and anxiety, and NK1 antagonists have shown potential in the treatment of anxiety disorders and depression.
Inflammatory conditions: NK1 antagonists have demonstrated anti-inflammatory effects and may have potential in the treatment of conditions like asthma, allergic rhinitis, and inflammatory bowel disease.
Substance P is involved in transmitting pain signals, and NK1 antagonists have been explored as potential analgesics.
As with any medication, NK1 antagonists can have side effects, such as fatigue, dizziness, and gastrointestinal disturbances.
Chemotherapy-induced emesis appears to consist of acute and delayed phases.
Acute phase emesis responds to 5-HT3 antagonists while the delayed phase remains difficult to control.
NK1 receptor antagonists have elicited antiemetic effect in both acute and especially in delayed phases of emesis.
Casopitant, netupitant and rolapitant are newer additions in this group.
Rolapitant has a significantly longer half-life of 160 hours.
Tachykinin NK1 receptor, often referred to as NK1 receptor, is a member of family 1 of G protein-coupled receptors and binds to the Gαq protein.