Results 151 to 160 of about 160,899 (200)
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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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Mini-Reviews in Medical Chemistry, 2019
Breast cancer (BC) is the most frequently diagnosed cancer and the leading cause of cancer death among females. BC cells not showing HER-2/Neu amplification and not expressing estrogen/progesterone receptors are named triple-negative BC (TNBC) cells ...
M. Muñoz, M. Rosso, R. Coveñas
semanticscholar +1 more source
Breast cancer (BC) is the most frequently diagnosed cancer and the leading cause of cancer death among females. BC cells not showing HER-2/Neu amplification and not expressing estrogen/progesterone receptors are named triple-negative BC (TNBC) cells ...
M. Muñoz, M. Rosso, R. Coveñas
semanticscholar +1 more source
Neurokinin-1 Receptor Antagonists in Lung Cancer Therapy
Letters in Drug Design and Discovery, 2017Rafael Coveñas, MIGUEL Munoz
exaly +2 more sources
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 ...
C. Apfel, A. Malhotra, J. Leslie
semanticscholar +3 more sources
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 ...
C. Apfel, A. Malhotra, J. Leslie
semanticscholar +3 more sources
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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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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Neurokinin 1 receptor antagonists--current prospects.
Current opinion in drug discovery & development, 2007The isolation of substance P (SP) in 1931, and the later discovery of its preferred neurokinin (NK)1 receptor, led to an intense research effort aimed at elucidating the biological role of SP, particularly within the central nervous system. There is now a large body of evidence to support the hypothesis that SP is one of the most important ...
Giuseppe, Alvaro, Romano, Di Fabio
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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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Journal of Pharmacology and Experimental Therapeutics, 2001
CP-122721 and CP-141938 are potent and selective neurokinin-1 (NK(1)) receptor antagonists with very different brain disposition and potency in models of centrally mediated activity. These investigations sought to determine whether differences in potency
Bill Smith +5 more
semanticscholar +1 more source
CP-122721 and CP-141938 are potent and selective neurokinin-1 (NK(1)) receptor antagonists with very different brain disposition and potency in models of centrally mediated activity. These investigations sought to determine whether differences in potency
Bill Smith +5 more
semanticscholar +1 more source