Search Results - "Mcleod, Robbie L"
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Treatment of acute lung injury by targeting MG53-mediated cell membrane repair
Published in Nature communications (18-07-2014)“…Injury to lung epithelial cells has a role in multiple lung diseases. We previously identified mitsugumin 53 (MG53) as a component of the cell membrane repair…”
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2
Mineralocorticoid receptor antagonists attenuate pulmonary inflammation and bleomycin-evoked fibrosis in rodent models
Published in European journal of pharmacology (15-10-2013)“…Accumulating evidence indicates protective actions of mineralocorticoid antagonists (MR antagonists) on cardiovascular pathology, which includes blunting…”
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3
Preclinical Experimental and Mathematical Approaches for Assessing Effective Doses of Inhaled Drugs, Using Mometasone to Support Human Dose Predictions
Published in Journal of aerosol medicine and pulmonary drug delivery (01-08-2016)“…Understanding the relationship between dose, lung exposure, and drug efficacy continues to be a challenging aspect of inhaled drug development. An experimental…”
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4
Efficacy of a NOP1 Agonist (SCH486757) in Subacute Cough
Published in Lung (01-01-2010)“…Currently, opiates are widely used as antitussives but have substantial side effects. Recently, it has been proposed that NOP1 receptor agonists may be useful…”
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Pharmacological evaluation of selective α2c-adrenergic agonists in experimental animal models of nasal congestion
Published in The Journal of pharmacology and experimental therapeutics (01-04-2014)“…Nasal congestion is one of the most troublesome symptoms of many upper airways diseases. We characterized the effect of selective α2c-adrenergic agonists in…”
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6
Discovery of Orally Active 3-Pyridinyl-tropane As a Potent Nociceptin Receptor Agonist for the Management of Cough
Published in Journal of medicinal chemistry (10-09-2009)“…A series of 3-pyridinyl-tropane analogues based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high…”
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7
Anandamide induces cough in conscious guinea‐pigs through VR1 receptors
Published in British journal of pharmacology (01-11-2002)“…Endogenous neuronal lipid mediator anandamide, which can be synthesized in the lung, is a ligand of both cannabinoid (CB) and vanilloid receptors (VR). The…”
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8
The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety
Published in Bioorganic & medicinal chemistry letters (01-05-2009)“…The discovery of 1 as a high-affinity ligand for the nociceptin receptor has led to the synthesis of a series of tropane (8-methyl-8-azabicyclo[3.2.1]octane)…”
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9
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators
Published in Journal of medicinal chemistry (22-04-2021)“…The approvals of idelalisib and duvelisib have validated PI3Kδ inhibitors for the treatment for hematological malignancies driven by the PI3K/AKT pathway. Our…”
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Effect of combined histamine H1 and H3 receptor blockade on cutaneous microvascular permeability elicited by compound 48/80
Published in Life sciences (1973) (04-03-2005)“…The pharmacological consequences of combining a histamine H1 receptor antagonist with a H3 antagonist on cutaneous microvascular permeability due to…”
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Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability
Published in Journal of medicinal chemistry (09-05-2019)“…PI3Kδ catalytic activity is required for immune cell activation, and has been implicated in inflammatory diseases as well as hematological malignancies in…”
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Characterizing Pharmacokinetic-Pharmacodynamic Relationships and Efficacy of PI3K δ Inhibitors in Respiratory Models of TH2 and TH1 Inflammation
Published in The Journal of pharmacology and experimental therapeutics (01-05-2019)“…We leveraged a clinical pharmacokinetic (PK)/pharmacodynamics (PD)/efficacy relationship established with an oral phosphatidylinositol 3-kinase (PI3K)…”
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13
Alpha-2c-adrenergic receptors contribute to basal nasal patency in the anesthetized cat
Published in Pharmacology (01-01-2010)“…Nasal congestion is the most troublesome symptom associated with a variety of upper airway diseases, including allergic rhinitis and the common cold. A better…”
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14
Characterization of murine CEACAM1 in vivo reveals low expression on CD8 + T cells and no tumor growth modulating activity by anti-CEACAM1 mAb CC1
Published in Oncotarget (02-10-2018)“…Carcinoembryonic antigen-related cell adhesion molecule 1 (CEACAM1) has been reported to mediate both tumorigenic and anti-tumor effects . Blockade of the…”
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Anti-inflammatory actions of Chemoattractant Receptor-homologous molecule expressed on Th2 by the antagonist MK-7246 in a novel rat model of Alternaria alternata elicited pulmonary inflammation
Published in European journal of pharmacology (15-11-2014)“…Alternaria alternata is a fungal allergen linked to the development of severe asthma in humans. In view of the clinical relationship between A. alternata and…”
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Etanercept ameliorates inflammation and pain in a novel mono-arthritic multi-flare model of streptococcal cell wall induced arthritis
Published in BMC musculoskeletal disorders (04-12-2014)“…The impact of anti-TNF, corticosteroid and analgesic therapy on inflammation and pain was evaluated in a novel mono-arthritic multi-flare rat Streptococcal…”
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TRPV1 Antagonists as Potential Antitussive Agents
Published in Lung (01-01-2008)“…Cough is an important defensive pulmonary reflex that removes irritants, fluids, or foreign materials from the airways. However, when cough is exceptionally…”
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Pharmacological profile of the NOP agonist and cough suppressing agent SCH 486757 (8-[Bis(2-Chlorophenyl)Methyl]-3-(2-Pyrimidinyl)-8-Azabicyclo[3.2.1]Octan-3-Ol) in preclinical models
Published in European journal of pharmacology (25-03-2010)“…We describe the pharmacological and pharmacokinetic profiles of SCH 486757, a nociceptin/orphanin FQ peptide (NOP) receptor agonist that has recently entered…”
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Where are the new cough treatments: a debriefing of recent clinical proof-of-concept trials with the NOP agonist SCH 486757
Published in Pharmacology (01-01-2011)“…Cough continues to be one of the top reasons why patients seek medical attention from health care providers. The prescription antitussive market is dominated…”
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In vivo metabolism-based discovery of a potent cholesterol absorption inhibitor, SCH58235, in the rat and rhesus monkey through the identification of the active metabolites of SCH48461
Published in The Journal of pharmacology and experimental therapeutics (01-10-1997)“…SCH48461 is a selective and highly potent inhibitor of cholesterol absorption. In rats, SCH48461 is rapidly and completely metabolized in the first pass…”
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