Search Results - "Runyon, Scott P."
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Regulation of the Apelinergic System and Its Potential in Cardiovascular Disease: Peptides and Small Molecules as Tools for Discovery
Published in Journal of medicinal chemistry (22-10-2015)“…Apelin peptides and the apelin receptor represent a relatively new therapeutic axis for the potential treatment of cardiovascular disease. Several reports…”
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The importance of the 6- and 7-positions of tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor
Published in Bioorganic & medicinal chemistry (01-09-2015)“…[Display omitted] Selective antagonism of the orexin 1 (OX1) receptor has been proposed as a potential mechanism for treatment of drug addiction. We have…”
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Effect of 1‑Substitution on Tetrahydroisoquinolines as Selective Antagonists for the Orexin‑1 Receptor
Published in ACS chemical neuroscience (15-04-2015)“…Selective blockade of the orexin-1 receptor (OX1) has been suggested as a potential approach to drug addiction therapy because of its role in modulating the…”
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Identification of potent pyrazole based APELIN receptor (APJ) agonists
Published in Bioorganic & medicinal chemistry (15-02-2020)“…[Display omitted] The apelinergic system comprises the apelin receptor and its cognate apelin and elabela peptide ligands of various lengths. This system has…”
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Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin receptor
Published in Bioorganic & medicinal chemistry (15-07-2022)“…[Display omitted] The apelin receptor (APJ) is a target for cardiovascular indications. Previously, we had identified a novel pyrazole-based agonist 1…”
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Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in Mice
Published in Journal of medicinal chemistry (25-03-2021)“…Apelin receptor agonism improves symptoms of metabolic syndrome. However, endogenous apelin peptides have short half-lives, making their utility as potential…”
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RTI-263, a biased neuropeptide S receptor agonist that retains an anxiolytic effect, attenuates cocaine-seeking behavior in rats
Published in Neuropharmacology (15-12-2023)“…Neuropeptide S (NPS) is a neuromodulatory peptide that acts via a G protein-coupled receptor. Centrally administered NPS suppresses anxiety-like behaviors in…”
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Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor
Published in Journal of medicinal chemistry (24-05-2018)“…Type 1 cannabinoid receptor (CB1) antagonists have demonstrated promise for the treatment of obesity, liver disease, metabolic syndrome, and dyslipidemias…”
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Identifying structural determinants of potency for analogs of apelin-13: Integration of C-terminal truncation with structure–activity
Published in Bioorganic & medicinal chemistry (01-06-2014)“…Apelin peptides function as endogenous ligands of the APJ receptor and have been implicated in a number of important biological processes. While several…”
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Preclinical Efficacy and Selectivity of Vaccines Targeting Fentanyl, Alfentanil, Sufentanil, and Acetylfentanyl in Rats
Published in ACS omega (17-05-2022)“…The ongoing public health emergency of opioid use disorders (OUD) and overdose in the United States is largely driven by fentanyl and its related analogues and…”
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Discovery of a novel small molecule agonist scaffold for the APJ receptor
Published in Bioorganic & medicinal chemistry (15-08-2016)“…[Display omitted] The apelinergic system includes a series of endogenous peptides apelin, ELABELA/TODDLER and their 7-transmembrane G-protein coupled apelin…”
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Identification of the first biased NPS receptor agonist that retains anxiolytic and memory promoting effects with reduced levels of locomotor stimulation
Published in Neuropharmacology (15-05-2017)“…The neuropeptide S system has been implicated in a number of centrally mediated behaviors including memory consolidation, anxiolysis, and increased locomotor…”
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Anti-Müllerian hormone as a biomarker for acute testicular degeneration caused by toxic insults to stallion testes
Published in Theriogenology (01-08-2018)“…Recently, anti-Müllerian hormone (AMH) was validated as a reliable marker of testicular damage caused by various chemotherapy drugs in humans and in mice. In…”
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Regulation of the Apelinergic System and Its Potential in Cardiovascular Disease: Peptides and Small Molecules as Tools for Discovery: Miniperspective
Published in Journal of medicinal chemistry (22-10-2015)“…Apelin peptides and the apelin receptor represent a relatively new therapeutic axis for the potential treatment of cardiovascular disease. Several reports…”
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Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3R)‑7-Hydroxy‑N‑[(1S)‑2-methyl-1-(piperidin-1-ylmethyl)propyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (PDTic)
Published in Journal of medicinal chemistry (13-09-2018)“…Past studies have shown that it has been difficult to discover and develop potent and selective κ opioid receptor antagonists, particularly compounds having…”
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Synthesis and pharmacological characterization of functionalized 6-piperazin-1-yl-purines as cannabinoid receptor 1 (CB1) inverse agonists
Published in Bioorganic & medicinal chemistry (15-08-2018)“…[Display omitted] Antagonists of peripheral type 1 cannabinoid receptors (CB1) may have utility in the treatment of obesity, liver disease, metabolic syndrome…”
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Antagonism of the neuropeptide S receptor with RTI-118 decreases cocaine self-administration and cocaine-seeking behavior in rats
Published in Pharmacology, biochemistry and behavior (01-12-2012)“…Neuropeptide S (NPS) is a neuromodulatory peptide, acting via a G-protein-coupled receptor to regulate sleep, anxiety and behavioral arousal. Recent research…”
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Effects of inhibitory GABA-active neurosteroids on cocaine seeking and cocaine taking in rats
Published in Psychopharmacology (01-09-2014)“…Rationale Several compounds that potentiate GABA-induced inhibitory currents also decrease stress, anxiety and addiction-related behaviors. Because of the…”
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A therapeutic combination of metyrapone and oxazepam increases brain levels of GABA-active neurosteroids and decreases cocaine self-administration in male rats
Published in Behavioural brain research (15-09-2015)“…•Combination of metyrapone and oxazepam (MET/OX) decreases drug self-administration.•MET/OX treatment increases neurosteroid levels in rat brain…”
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Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3R)‑N‑[1R)‑1-(Cyclohexylmethyl)-2-methylpropyl]-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (CDTic
Published in Journal of medicinal chemistry (13-09-2018)“…Animal pharmacological studies suggest that potent and selective κ opioid receptor antagonists have potential as pharmacotherapies targeting depression,…”
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