A brain-first framework for perimenopause management: the case for non-invasive neuromodulation. [PDF]
Radytė E, Karvelyte I.
europepmc +1 more source
Safety and tolerability of elinzanetant: a pooled analysis from four randomized clinical trials. [PDF]
Pinkerton JV +7 more
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Detection of an Antagonist Bound to the Neurokinin a Receptor in Styrene-Maleic Acid Lipid Particles by <sup>19</sup>F Ultrafast Magic-Angle Spinning Nuclear Magnetic Resonance Spectroscopy. [PDF]
Seidl S +6 more
europepmc +1 more source
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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 Antagonists as Anticancer Drugs
Letters in Drug Design & Discovery, 2019Background::Human tumor cells lines and tumor samples overexpress the neurokinin-1 receptor (NK-1R). Substance P (SP), after binding to NK-1Rs, induces tumor cell proliferation, an antiapoptotic effect and promotes angiogenesis and the migration of cancer cells for invasion and metastasis.Methods: :In contrast, NK-1R antagonists block the previous ...
Muñoz Sáez, Miguel, Coveñas, Rafael
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Glioma and Neurokinin-1 Receptor Antagonists: A New Therapeutic Approach
Anti-Cancer Agents in Medicinal Chemistry, 2019Background:In adults, the most lethal and frequent primary brain tumor is glioblastoma. Despite multimodal aggressive therapies, the median survival time after diagnosis is around 15 months. In part, this is due to the blood-brain barrier that restricts common treatments (e.g., chemotherapy). Unfortunately, glioma recurs in 90% of patients.
Miguel, Muñoz, Rafael, Coveñas
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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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