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Neurokinin-1-Receptor Antagonists: A New Approach in Antiemetic Therapy
Oncology Research and Treatment, 2006Aprepitant (Emend), the first neurokinin-1-receptor antagonist (NK-1-RA), represents a new class of antiemetics. Aprepitant has been approved for the prevention and treatment of acute (0-24 h after chemotherapy) and delayed (1-5 days after chemotherapy) emesis resulting from cisplatin-based chemotherapy and moderately emetogenic chemotherapy.
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The Role of Neurokinin-1 Receptor Antagonists in CINV
2016Significant advances have been made in controlling chemotherapy-induced nausea and vomiting (CINV) in the past two decades. These advances are primarily due to a greater understanding of the physiological and molecular pathways underlying CINV, which resulted in major progress in the management of patients with CINV.
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Spiro-piperidine non-peptide neurokinin-1 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 1995Abstract The synthesis and activity of a novel spiro-piperidine non-peptide antagonist (2) of the neurokinin-1 (NK 1 ) receptor is described. Despite having essentially the same solution conformation as CP 99,994 (1) at physiological pH, (2) has reduced affinity for the NK 1 receptor.
D.R. Armour +12 more
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[Neurokinin 1 receptor antagonists--between hope and disappointment].
Medizinische Monatsschrift fur Pharmazeuten, 2006Substance P (SP)/Neurokinin 1 (NK1) receptor pathways have been repeatedly implicated in the pathophysiology of central, pulmonary, and gastric disorders. A large body of evidence that has been generated from animal experiments indicates that treatment with selective NK1 receptor antagonists might be effective in the treatment of certain forms of ...
Kristin, Rost +2 more
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Tradipitant: A Novel Neurokinin-1 Receptor Antagonist for Motion Sickness
American Journal of TherapeuticsBackground: Motion sickness affects millions of people with common symptoms, including nausea and vomiting. Medications used for management of motion sickness since 1870 predominately have anticholinergics and antihistamines properties. For the past 40 years, there have been no advances in medication options for
Timothy Nguyen +5 more
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In Silico Study of Neurokinin-1 Receptor Antagonists by QSAR Modeling
2017QSAR studies were performed on a series neurokinin-1 receptor. neurokinin-1 receptor have been analyzed in relation to their physicochemical and molecular properties. On the basis of QSAR studies presented here, the coefficients of Id, IOR, MR, MW, ST, MV, Pz are positive and therefore it may be suggested that denser, bulkier, more polar substituents ...
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Neurokinin(1) receptor antagonists as potential antidepressants.
Annual Review of Pharmacology and Toxicology, 2001S. C. Stout +2 more
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