Search Results - "Aiyar, Nambi V"
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Differential vasoconstrictor activity of human urotensin‐II in vascular tissue isolated from the rat, mouse, dog, pig, marmoset and cynomolgus monkey
Published in British journal of pharmacology (01-12-2000)“…Urotensin‐II (U‐II) and its G‐protein‐coupled receptor, GPR14, are expressed within mammalian cardiac and peripheral vascular tissue and, as such, may regulate…”
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Interleukin-1 receptor and receptor antagonist gene expression after focal stroke in rats
Published in Stroke (1970) (01-01-1997)“…The expression of interleukin-1 beta (IL-1 beta) is upregulated after focal brain ischemia, and previous work has demonstrated its involvement in ischemic…”
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Characterization of neuromedin U effects in canine smooth muscle
Published in The Journal of pharmacology and experimental therapeutics (01-06-2002)“…Two endogenous receptors for the potent smooth muscle-stimulating peptide neuromedin U (NmU) have recently been identified and cloned. Pharmacological,…”
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Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14
Published in Nature (London) (16-09-1999)“…Urotensin-II (U-II) is a vasoactive 'somatostatin-like' cyclic peptide which was originally isolated from fish spinal cords, and which has recently been cloned…”
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Molecular and pharmacological characterization of genes encoding urotensin‐II peptides and their cognate G‐protein‐coupled receptors from the mouse and monkey
Published in British journal of pharmacology (01-05-2002)“…Urotensin‐II (U‐II) and its receptor (UT) represent novel therapeutic targets for management of a variety of cardiovascular diseases. To test such hypothesis,…”
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Tetrahydro-4-quinolinamines identified as novel P2Y1 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-12-2008)Get full text
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Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-12-2008)“…High-throughput screening of the GSK compound collection against the P2Y(1) receptor identified a novel series of tetrahydro-4-quinolinamine antagonists…”
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The peptidic urotensin‐II receptor ligand GSK248451 possesses less intrinsic activity than the low‐efficacy partial agonists SB‐710411 and urantide in native mammalian tissues and recombinant cell systems
Published in British journal of pharmacology (01-05-2006)“…1 Several peptidic urotensin‐II (UT) receptor antagonists exert ‘paradoxical’ agonist activity in recombinant cell‐ and tissue‐based bioassay systems, likely…”
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Identification and pharmacological characterization of native, functional human urotensin‐II receptors in rhabdomyosarcoma cell lines
Published in British journal of pharmacology (01-07-2004)“…In an effort to identify endogenous, native mammalian urotensin‐II (U‐II) receptors (UT), a diverse range of human, primate and rodent cell lines (49 in total)…”
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Identification and characterization of binding sites for human urotensin-II in Sprague–Dawley rat renal medulla using quantitative receptor autoradiography
Published in Peptides (New York, N.Y. : 1980) (01-06-2006)“…Urotensin-II (U-II), a ligand for the G-protein-coupled receptor UT, has been characterized as the most potent mammalian vasoconstrictor identified to date…”
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erratum: Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14
Published in Nature (London) (23-12-1999)Get full text
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Development of potent and selective small-molecule human Urotensin-II antagonists
Published in Bioorganic & medicinal chemistry (15-06-2008)“…This work describes the development of potent and selective human Urotensin-II antagonists starting from lead compound 1. Several problems relating to oral…”
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Differential agonistic and antagonistic effects of the urotensin-II ligand SB-710411 at rodent and primate UT receptors
Published in European journal of pharmacology (25-05-2004)“…SB-710411 (Cpa-c[d-Cys-Pal-d-Trp-Lys-Val-Cys]-Cpa-amide) inhibited [(125)I]urotensin-II rat and monkey UT receptor binding (pK(i)s 7.50+/-0.07 and…”
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Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles
Published in Bioorganic & medicinal chemistry letters (01-07-2008)“…Redesign of the potent human urotensin-II antagonist 1 with the 2-pyrrolidinylmethyl-3-phenyl-piperidine core to a new chemical series with a substituted…”
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Inhibitory effects of putative peptidic urotensin-II receptor antagonists on urotensin-II-induced contraction of cat isolated respiratory smooth muscle
Published in European journal of pharmacology (15-06-2005)“…Urotensin-II is purported to influence pulmonary function by modulating smooth muscle tone/growth. In the present study, Northern blot and reverse…”
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Human Urotensin-II is a Potent Vasoactive Peptide: Pharmacological Characterization in the Rat, Mouse, Dog and Primate
Published in Journal of cardiovascular pharmacology (2000)“…The observation that the novel G-protein-coupled receptor (GPCR) GPR14 and its cognate ligand, urotensin-II (U-II), are expressed within the mammalian…”
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Human Urotensin-II is a Potent Vasoactive Peptide: Pharmacological Characterization in the Rat, Mouse, Dog and Primate
Published in Journal of cardiovascular pharmacology (01-11-2000)“…The observation that the novel G-protein-coupled receptor (GPCR) GPR14 and its cognate ligand, urotensin-II (U-II), are expressed within the mammalian…”
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Nonpeptidic urotensin‐II receptor antagonists I: in vitro pharmacological characterization of SB‐706375
Published in British journal of pharmacology (01-07-2005)“…1 SB‐706375 potently inhibited [125I]hU‐II binding to both mammalian recombinant and ‘native’ UT receptors (Ki 4.7±1.5 to 20.7±3.6 nM at rodent, feline and…”
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Tetrahydro-4-quinolinamines identified as novel P2Y sub(1) receptor antagonists
Published in Bioorganic & medicinal chemistry (01-12-2008)“…High-throughput screening of the GSK compound collection against the P2Y sub(1) receptor identified a novel series of tetrahydro-4-quinolinamine antagonists…”
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20
Discovery of Adrenomedullin in Rat Ischemic Cortex and Evidence for its Role in Exacerbating Focal Brain Ischemic Damage
Published in Proceedings of the National Academy of Sciences - PNAS (05-12-1995)“…Focal brain ischemia is the most common event leading to stroke in humans. To understand the molecular mechanisms associated with brain ischemia, we applied…”
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