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The Involvement of the Peptidergic Systems in Breast Cancer Development. [PDF]
Sánchez ML +5 more
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Beyond Medicalization: Menopause Care with Empathy: An Editorial Review. [PDF]
Sharma S, Mehra R.
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Safety of neurokinin-1 receptor antagonists
Expert Opinion on Drug Safety, 2013The substance P (SP)/neurokinin (NK)-1 receptor system is involved in many pathological processes. NK-1 receptor antagonists have many promising therapeutic indications. However, the only NK-1 receptor antagonist used in clinical practice is the drug aprepitant and its intravenously administered prodrug, fosaprepitant.
Miguel, Muñoz, Rafael, Coveñas
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A selective and extremely potent antagonist of the neurokinin-1 receptor
Brain Research, 1992Sendide [Tyr6,D-Phe7,D-His9]-substance P(6-11) has been examined by measurements of ligand binding to crude membrane fractions and by functional tests on the spinally mediated behavioral response. Sendide potently displaced [3H]-labeled substance P (SP) binding to mouse spinal cord membranes in a competitive manner.
T, Sakurada +6 more
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Neurokinin-1 receptor antagonists: a comprehensive patent survey
Expert Opinion on Therapeutic Patents, 2010Substance P is involved in mediating a number of biological effects such as emesis, pain, inflammation, bronchoconstriction, antitumor activity, and regulation of gastrointestinal and CNS function by binding to the neurokinin-1 (NK1) receptor. Antagonists of this receptor have the potential to be useful in the treatment of various disease conditions ...
Shih-Chung, Huang, Vijaya L, Korlipara
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Neurokinin-1 receptor antagonist SR140333
NeuroReport, 1997Substance P (SP) has been implicated in immune responses and could increase glutamate release, and inflammatory reactions are known to be able to potentiate ischemic damage. We have previously found that SP was over-expressed in cerebral ischemia and speculated that SP may play a role in exacerbating ischemic damage.
Z, Yu, G, Cheng, X, Huang, K, Li, X, Cao
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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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