Search Results - "Humphrys, Laura J."
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Clonidine stimulates force of contraction via histamine H2 receptors in the human atrium
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-01-2024)“…Clonidine has various clinical effects mediated by agonism of α 1 - or α 2 -adrenoceptors and the blocking of hyperpolarization-activated-nucleotide-gated…”
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A G protein-coupled receptor dimer imaging assay reveals selectively modified pharmacology of neuropeptide Y Y1/Y5 receptor heterodimers
Published in Molecular pharmacology (01-04-2015)“…The ability of G protein-coupled receptors (GPCRs) to form dimers, and particularly heterodimers, offers potential for targeted therapeutics with improved…”
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[3H]UR-JG102–A Radiolabeled Cyclic Peptide with High Affinity and Excellent Selectivity for the Neuropeptide Y Y4 Receptor
Published in Journal of medicinal chemistry (12-10-2023)“…The family of human neuropeptide Y receptors (YRs) comprises four subtypes (Y1R, Y2R, Y4R, and Y5R) that are involved in the regulation of numerous…”
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4
Lysergic acid diethylamide stimulates cardiac human H2 histamine and cardiac human 5-HT4-serotonin receptors
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-01-2024)“…Lysergic acid diethylamide (LSD) is an artificial hallucinogenic drug. Thus, we hypothesized that LSD might act 5-HT 4 serotonin receptors and/or H 2 histamine…”
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5
Ergometrine stimulates histamine H2 receptors in the isolated human atrium
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-12-2023)“…Ergometrine (6a R ,9 R )- N -(( S )-1-hydroxypropan-2-yl)-7-methyl-4,6,6a,7,8,9-hexa-hydro-indolo-[4,3- fg ]chinolin-9-carboxamide or lysergide acid…”
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6
Stereochemistry-Driven Interactions of α,γ-Peptide Ligands with the Neuropeptide Y Y 4 -Receptor
Published in Journal of medicinal chemistry (27-07-2023)“…The G-protein-coupled Y -receptor (Y R) and its endogenous ligand, pancreatic polypeptide (PP), suppress appetite in response to food intake and, thus, are…”
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Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify receptor-transducer coupling and mediate intracellular pathway bias
Published in The Journal of biological chemistry (01-09-2022)“…Within the intestine, the human G protein–coupled receptor (GPCR) GPR35 is involved in oncogenic signaling, bacterial infections, and inflammatory bowel…”
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The dark sides of the GPCR tree - research progress on understudied GPCRs
Published in British journal of pharmacology (10-02-2024)“…A large portion of the human GPCRome is still in the dark and understudied, consisting even of entire subfamilies of GPCRs such as odorant receptors, class A…”
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Stereochemistry-Driven Interactions of α,γ-Peptide Ligands with the Neuropeptide Y Y4‑Receptor
Published in Journal of medicinal chemistry (27-07-2023)“…The G-protein-coupled Y4-receptor (Y4R) and its endogenous ligand, pancreatic polypeptide (PP), suppress appetite in response to food intake and, thus, are…”
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10
Dual Piperidine-Based Histamine H3 and Sigma‑1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain
Published in Journal of medicinal chemistry (27-07-2023)“…In search of new dual-acting histamine H3/sigma-1 receptor ligands, we designed a series of compounds structurally based on highly active in vivo ligands…”
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Dual Piperidine-Based Histamine H 3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain
Published in Journal of medicinal chemistry (27-07-2023)“…In search of new dual-acting histamine H /sigma-1 receptor ligands, we designed a series of compounds structurally based on highly active ligands previously…”
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A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H3 Receptor
Published in Journal of medicinal chemistry (12-08-2021)“…The histamine H3 receptor (H3R) is considered an attractive drug target for various neurological diseases. We here report the synthesis of UR-NR266, a novel…”
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Activation of Multiple G Protein Pathways to Characterize the Five Dopamine Receptor Subtypes Using Bioluminescence Technology
Published in ACS pharmacology & translational science (08-03-2024)“…G protein-coupled receptors show preference for G protein subtypes but can recruit multiple G proteins with various downstream signaling cascades. This…”
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Illuminating Neuropeptide Y Y 4 Receptor Binding: Fluorescent Cyclic Peptides with Subnanomolar Binding Affinity as Novel Molecular Tools
Published in ACS pharmacology & translational science (12-04-2024)“…The neuropeptide Y (NPY) Y receptor (Y R), a member of the family of NPY receptors, is physiologically activated by the linear 36-amino acid peptide pancreatic…”
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Illuminating Neuropeptide Y Y4 Receptor Binding: Fluorescent Cyclic Peptides with Subnanomolar Binding Affinity as Novel Molecular Tools
Published in ACS pharmacology & translational science (12-04-2024)“…The neuropeptide Y (NPY) Y4 receptor (Y4R), a member of the family of NPY receptors, is physiologically activated by the linear 36-amino acid peptide…”
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[ 3 H]UR-JG102–A Radiolabeled Cyclic Peptide with High Affinity and Excellent Selectivity for the Neuropeptide Y Y 4 Receptor
Published in Journal of medicinal chemistry (12-10-2023)Get full text
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Lysergic acid diethylamide stimulates cardiac human H 2 histamine and cardiac human 5-HT 4 -serotonin receptors
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-01-2024)“…Lysergic acid diethylamide (LSD) is an artificial hallucinogenic drug. Thus, we hypothesized that LSD might act 5-HT serotonin receptors and/or H histamine…”
Get full text
Journal Article -
19
Clonidine stimulates force of contraction via histamine H 2 receptors in the human atrium
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-01-2024)“…Clonidine has various clinical effects mediated by agonism of α - or α -adrenoceptors and the blocking of hyperpolarization-activated-nucleotide-gated…”
Get full text
Journal Article -
20
Ergometrine stimulates histamine H 2 receptors in the isolated human atrium
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-12-2023)“…Ergometrine (6aR,9R)-N-((S)-1-hydroxypropan-2-yl)-7-methyl-4,6,6a,7,8,9-hexa-hydro-indolo-[4,3-fg]chinolin-9-carboxamide or lysergide acid β-ethanolamide or…”
Get full text
Journal Article