receptor antagonist
Production of interleukin-1 receptor antagonist by human articular chondrocytes.
... Abstract Interleukin-1 receptor antagonist (IL-1Ra) is a natural IL-1 inhibitor possessing anti-inflammatory properties. IL-1Ra is produced as different isoforms, one secreted (sIL-1Ra) and three ...
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Randomized Dose-Response Study of the New Dual Endothelin Receptor Antagonist Aprocitentan in Hypertension
... Summary Aprocitentan, a dual endothelin receptor antagonist, was evalu- ated in a dose-response study examining its effects on BP in 490 patients with mild-to-moderate hypertension. Changes in BP were ...
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Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain.
... We thank A.M. Lhiaubet for labeling [ 125 I]neurotensin. C.B. is supported by a post-doctoral fellowship from INSERM (Institut National de la Santé et de la Recherche Médicale), France. References Betancur, C., Canton, ...
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Rosiglitazone induces interleukin-1 receptor antagonist in interleukin-1beta-stimulated rat synovial fibroblasts via a peroxisome proliferator-activated receptor beta/delta-dependent mechanism
... natural receptor antagonist (IL-1Ra). The IL-1 receptor family is composed of 2 receptors that have different physiologic roles: the type 1 receptor (IL-1RI), which transduces a signal upon ...
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Beneficial Effect of a Selective Adenosine A2A Receptor Antagonist in the APPswe/PS1dE9 Mouse Model of Alzheimer’s Disease
... Department of Neurodegenerative Diseases and Geropsychiatry/Neurology, University of Bonn Medical Center, Bonn, Germany Edited by: Detlev Boison, Legacy Health, United States Reviewed by: Annakaisa Haapasalo, A.I. ...
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Ciproxifan, a Histamine H 3 -Receptor Antagonist/Inverse Agonist, Potentiates Neurochemical and Behavioral Effects of Haloperidol in the Rat
... - receptor ligands on the regulation of enkephalin mRNA expression in the ...-receptor antagonist/inverse agonist, did not modify the expression of the neuropeptide by itself but strongly increased ...
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Thromboxane–prostaglandin receptor antagonist, terutroban, prevents neurovascular events after subarachnoid haemorrhage: a nanoSPECT study in rats
... Terutroban (TBN), a specific TP receptor antagonist [ 21 ], was first studied as an antiplatelet and vasoprotec- tive agent. Lesault et al. [ 22 ] revealed that TBN im- proved endothelial function and ...
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A dual thromboxane inhibitor and thromboxane receptor antagonist prevents pig myocardial infarction induced by coronary thrombosis
... A2 receptor antagonist and thromboxane synthase inhibitor, on myocardial infarction induced by topical ferric chloride (FeCl3) application to the left anterior descending (LAD) coronary artery in ...
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The triple neurokinin-receptor antagonist CS-003 inhibits neurokinin A-induced bronchoconstriction in patients with asthma
... 2 receptor antagonism results in prevention of NKA-induced ...tachykinin receptor antagonist CS-003 on NKA- induced bronchoconstriction in ...
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Neurotensin receptor antagonist administered during cocaine withdrawal decreases locomotor sensitization and conditioned place preference.
... suggested to participate in these phenomena. We and others have reported that SR 48692, a neurotensin receptor antagonist, given in pre-or co-treatments with cocaine or amphetamine, alters some behavioral ...
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The Interleukin-1 receptor antagonist is a direct target gene of PPARalpha in liver.: PPARalpha controls the expression of the sIL-1ra in liver
... IL-1 receptor antagonist While many genes involved in inflammation were down-regulated by Wy14643, hepatic expression of Interleukin 1 receptor antagonist (IL-1ra) was highly increased by PPAR ...
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BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.
... mGlu receptor subtypes was examined. The same index of receptor activation as for group-I mGluRs ...mGlu8 receptor, equal to ...mGlu1 receptor 50 ± μ 50 (data not ...an antagonist, ...
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Role of Insulin-Like Growth Factor Binding Proteins in Limitation of Igf-I Degradation into the N-Methyl-D-Aspartate Receptor Antagonist Gpe: Evidence from Gonadotrophin-Releasing Hormone Secretion in Vitro at Two Developmental Stages
... 8. J.P. Bourguignon, M.L. Alvarez Gonzalez, A. Gérard, P. Franchimont, Gonadotrophin-releasing hormone inhibitory autofeedback by subproducts antagonist at N -methyl- D -aspartate receptors: a model of autocrine ...
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Long-term effectiveness and safety of interleukin-1 receptor antagonist (anakinra) in Schnitzler's syndrome: A French multicenter study.
... Schnitzler's syndrome (SchS) is a rare disease that manifests with a urticarial skin rash, monoclonal gammopathy (mostly IgM kappa), and a variable combination of recurrent[r] ...
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Effect of prenatal androgen receptor antagonist or aromatase inhibitor on the differentiation of neuronal Fos responses to estrous female pheromones in the rat accessory olfactory system
... In the present study, we asked whether prenatal blockade of androgen receptor (AR) activation in either male or female rats using Flutamide would attenuate later neuronal Fos responses in the AOS to estrous odors. ...
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Molecular and cellular bases for the protective effects of dopamine D1 receptor antagonist, SCH23390, against methamphetamine-induced neurotoxicity in the rat brain
... 1.9 Molecular mechanisms of METH neurotoxicity 1.9.1 METH-induced regulation of immediate early genes expression Neuronal responses to psychostimulants involve a regulatory mechanism of gene expression in different brain ...
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Differential effects of histamine H 3 receptor inverse agonist thioperamide, given alone or in combination with the N-methyl-d-aspartate receptor antagonist dizocilpine, on reconsolidation and consolidation of a contextual fear memory in mice
... 3 receptor inverse agonists (which augment hista- mine release), we investigated to what extent the most rep- resentative of them, thioperamide, is able to facilitate recon- solidation of a ...
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mGlu5 receptor antagonist blocks bromocriptine-induced conditioned place preference in bilateral mesolimbic-lesioned rat
... mGlu5 receptor in the reinforcement, using the CPP paradigm, in bilateral pVTA-lesioned rats that have been previously sensitized with bromocriptine [39] ...mGlu5 receptor negative allosteric modulator ...
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The beta adrenergic receptor antagonist propranolol alters mitogenic and apoptotic signaling in late stage breast cancer
... Conclusion: Collectively, these data provide support for the incorporation of b-AR antago- nists into the clinical management of breast cancer, and elucidate a partial molecular mechanism explaining the efficacy of b-AR ...
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Shuttle-Cargo fusion molecules of transport peptides and the hD 2/3 receptor antagonist fallypride : a feasible approach to preserve ligand-receptor binding?
... transferrin receptor binding peptides (transported via the TfR), 10 neurotensin (transported via neurotensin receptors NTS1, NTS2, and NTS3), 11,12 chol- ecystokinin (transported via cholecystokinin receptors ...
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