Search Results - "Narayanan, Sanju"
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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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2
Sigma receptors and cocaine abuse
Published in Current topics in medicinal chemistry (01-05-2011)“…Sigma receptors have been well documented as a protein target for cocaine and have been shown to be involved in the toxic and stimulant actions of cocaine…”
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3
Regiospecific Synthesis of 2,3-Disubstituted- l-Histidines and Histamines
Published in Bioorganic & medicinal chemistry letters (07-05-2001)“…Regiospecific synthesis of 2,3-disubstituted- l-histidines and 2,3-disubstituted histamines starting from l-histidine methyl ester and histamine is reported…”
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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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Identification of Potent Pyrazole‐Based Biased Small Molecule APJ Receptor Agonists
Published in The FASEB journal (01-04-2019)“…The apelinergic system comprises the APJ receptor and its cognate apelin and ELABELA peptides of various lengths. This system has become an increasingly…”
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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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8
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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Blockade of Cocaine or σ Receptor Agonist Self Administration by Subtype-Selective σ Receptor Antagonists
Published in The Journal of pharmacology and experimental therapeutics (01-07-2016)“…The identification of sigma receptor (σR) subtypes has been based on radioligand binding and, despite progress with σ1R cellular function, less is known about…”
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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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11
Sigma Receptor Agonists: Receptor Binding and Effects on Mesolimbic Dopamine Neurotransmission Assessed by Microdialysis
Published in Biological psychiatry (1969) (01-02-2011)“…Background Subtypes of sigma (σ) receptors, σ1 and σ2 , can be pharmacologically distinguished, and each may be involved in substance-abuse disorders…”
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The dopamine uptake inhibitor, WIN 35,428, has sigma2 receptor agonist effects that contribute to its self‐administration (848.10)
Published in The FASEB journal (01-04-2014)“…Sigma receptors (σRs) are intracellular chaperone proteins implicated in several diseases, as well as psychiatric disorders and drug abuse. Several in vivo…”
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13
Early development of sigma-receptor ligands
Published in Future medicinal chemistry (01-01-2011)“…Sigma receptors (σ-1 and σ-2) are non-opioid proteins implicated in the pathophysiology of various neurological disorders and cancer. The σ-1 subtype is a…”
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14
Sigma receptor ligands attenuate methamphetamine‐induced hyperthermia but do not modulate IL‐1B mRNA expression in select brain regions
Published in The FASEB journal (01-04-2012)“…Abstract only Methamphetamine is one of the most widely abused drugs worldwide, with hyperthermia being a primary cause of death. Methamphetamine‐induced…”
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15
Synthesis and Pharmacological Evaluation of 6-Acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79), a Cocaine Antagonist, in Rodents
Published in The AAPS journal (01-09-2011)“…Cocaine interacts with monoamine transporters and sigma (σ) receptors, providing logical targets for medication development. In the present study, in vitro and…”
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Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2
Published in Bioorganic & medicinal chemistry letters (15-01-2015)“…Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesic effects in relevant animal models. Using a pharmacophore model based on…”
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Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-le u cine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2
Published in Bioorganic & medicinal chemistry letters (05-01-2015)“…Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesic effects in relevant animal models. Using a pharmacophore model based on…”
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18
Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series
Published in Bioorganic & medicinal chemistry letters (01-08-2015)“…[Display omitted] The design and optimization of a novel trans-1,4-dioxycyclohexane GPR119 agonist series is described. A lead compound 21 was found to be a…”
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Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists
Published in Bioorganic & medicinal chemistry letters (01-09-2014)“…A series of 5-fluoro-4,6-dialkoxypyrimidine GPR119 modulators were discovered and optimized for in vitro agonist activity. A lead molecule was identified that…”
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Conversion of a Highly Selective Sigma-1 Receptor–Ligand to Sigma-2 Receptor Preferring Ligands with Anticocaine Activity
Published in Journal of medicinal chemistry (13-03-2008)“…Cocaine’s toxicity can be mitigated by blocking its interaction with sigma-1 receptors. The involvement of sigma-2 receptors remains unclear. To investigate…”
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