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Advances in the research and application of neurokinin-1 receptor antagonists
Journal of Zhejiang University-SCIENCE BRecently, 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 ...
Xiangyu Hong +4 more
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Potential therapeutic targets for neurokinin-1 receptor antagonists
Expert Opinion on Emerging Drugs, 2004The peptide substance P and its tachykinin receptor, neurokinin-1 (NK1), have been the focus of considerable research for their role in a variety of both central and peripheral diseases. Recent preclinical data, as well as relevant clinical findings, support the potential therapeutic value of NK1 receptor antagonists in centrally mediated disease ...
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Peptides, 2012
The last decades have seen no significant progress in extending the survival of lung cancer patients and there is an urgent need to improve current therapies. The substance P (SP)/neurokinin-1 receptor (NK-1R) system plays an important role in the development of cancer: SP and NK-1R antagonists respectively induce cell proliferation and inhibition in ...
Miguel, Muñoz +6 more
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The last decades have seen no significant progress in extending the survival of lung cancer patients and there is an urgent need to improve current therapies. The substance P (SP)/neurokinin-1 receptor (NK-1R) system plays an important role in the development of cancer: SP and NK-1R antagonists respectively induce cell proliferation and inhibition in ...
Miguel, Muñoz +6 more
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Multivalently binding antagonists for the neurokinin-1 receptor
2020The goal of this thesis was to investigate the neurokinin-1 receptor (NK1R) as a potential target site for multivalent receptor blockade. Since the NK1R is peripherally expressed on various cell types of the human body and its expression increases when an immune response occurs, this receptor seems to offer great potential for selective and specific ...
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Antagonists that demonstrate species differences in neurokinin-1 receptors.
Molecular Pharmacology, 1992125I-Bolton-Hunter-substance P (125I-BH-SP) binding properties of three novel classes of neurokinin-1 (NK-1) receptor antagonists were investigated in tissues derived from humans, guinea pigs, and rats. 125I-BH-SP was shown to bind to a single class of binding sites, with similar dissociation constants, Kd, in human astrocytoma cells (U-373 MG), human ...
K C, Appell +4 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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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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Current Opinion in Anaesthesiology, 2008
To review the characteristics of neurokinin-1 receptor antagonists and their potential role in the management of postoperative nausea and vomiting.Neurokinin-1 antagonists compete with substance P, an endogenous ligand with a high density of receptors in the area postrema and the nucleus tractus solitarii, believed to be involved in terminal emetic ...
Christian C, Apfel +2 more
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To review the characteristics of neurokinin-1 receptor antagonists and their potential role in the management of postoperative nausea and vomiting.Neurokinin-1 antagonists compete with substance P, an endogenous ligand with a high density of receptors in the area postrema and the nucleus tractus solitarii, believed to be involved in terminal emetic ...
Christian C, Apfel +2 more
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Neurokinin-1 receptor antagonists modulate brain noradrenaline and serotonin interactions
European Journal of Pharmacology, 2008Substance P (neurokinin-1; NK1) receptor antagonists represent a putative new class of antidepressant/anxiolytic drugs. Using in vivo electrophysiological paradigms in rats, this study examined the effects of acute, sub-acute and long-term administration of these drugs on the firing of rat noradrenaline and serotonin (5-HT) neurons.
Nasser, Haddjeri, Pierre, Blier
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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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