Temat: "Drug Inverse Agonism" - OpacWWW

Skocz do pozycji: 1.

Tytuł:: Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.
Autorzy:: Kong J; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Chuddy J; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Stock IA; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Loria PM; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Straub SV; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Vage C; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Cameron KO; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Bhattacharya SK; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Lapham K; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
McClure KF; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Zhang Y; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.
Jackson VM; Cardiovascular and Metabolic Diseases Research Unit, Pfizer Worldwide Research and Development, Cambridge, MA, 01239, USA.; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2016 May; Vol. 173 (9), pp. 1452-64. Date of Electronic Publication: 2016 Mar 17.
Typ publikacji:: Journal Article
MeSH Terms:: Drug Inverse Agonism*
Azetidines/*pharmacology
Glucose/*metabolism
Insulin/*metabolism
Receptors, Ghrelin/*antagonists & inhibitors
Spiro Compounds/*pharmacology
Vagus Nerve/*drug effects
Animals ; Azetidines/chemistry ; Calcium/metabolism ; Dose-Response Relationship, Drug ; HEK293 Cells ; Humans ; Insulin Secretion ; Male ; Rats ; Rats, Sprague-Dawley ; Spiro Compounds/chemistry ; Structure-Activity Relationship ; Vagus Nerve/metabolism ; Vagus Nerve/physiology

Czasopismo naukowe

na półce

Pełny tekst Pełny tekst Szczegóły

Skocz do pozycji: 2.

Tytuł:: Evidence for both inverse agonism at the cannabinoid CB1 receptor and the lack of an endogenous cannabinoid tone in the rat and guinea-pig isolated ileum myenteric plexus-longitudinal muscle preparation.
Autorzy:: Makwana R; The Sackler Institute of Pulmonary Pharmacology, King's College London, Waterloo Campus, London, UK. />Molleman A
Parsons ME; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2010 Jun; Vol. 160 (3), pp. 615-26.
Typ publikacji:: Journal Article
MeSH Terms:: Drug Inverse Agonism*
Amidohydrolases/*antagonists & inhibitors
Ileum/*drug effects
Muscle Contraction/*physiology
Myenteric Plexus/*physiology
Piperidines/*antagonists & inhibitors
Pyrazoles/*antagonists & inhibitors
Animals ; Arachidonic Acids/pharmacology ; Cannabinoid Receptor Modulators/metabolism ; Cannabinoid Receptor Modulators/pharmacology ; Cannabinoid Receptor Modulators/physiology ; Cannabinoids/antagonists & inhibitors ; Cannabinoids/pharmacology ; Dronabinol/analogs & derivatives ; Dronabinol/pharmacology ; Guinea Pigs ; Muscle Contraction/drug effects ; Myenteric Plexus/drug effects ; Piperidines/pharmacology ; Pyrans/pharmacology ; Pyrazoles/pharmacology ; Rats ; Receptor, Cannabinoid, CB1/agonists ; Receptor, Cannabinoid, CB1/antagonists & inhibitors ; Receptor, Cannabinoid, CB1/physiology ; Rimonabant

Czasopismo naukowe

na półce

Pełny tekst Szczegóły

Skocz do pozycji: 3.

Tytuł:: SB265610 is an allosteric, inverse agonist at the human CXCR2 receptor.
Autorzy:: Bradley ME; Novartis Institutes for Biomedical Research, Horsham, West Sussex, UK.
Bond ME
Manini J
Brown Z
Charlton SJ; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2009 Sep; Vol. 158 (1), pp. 328-38. Date of Electronic Publication: 2009 Apr 24.
Typ publikacji:: Comparative Study; Journal Article
MeSH Terms:: Drug Inverse Agonism*
Phenylurea Compounds/*pharmacology
Receptors, Interleukin-8B/*agonists
Receptors, Interleukin-8B/*antagonists & inhibitors
Triazoles/*pharmacology
Allosteric Regulation/physiology ; Animals ; CHO Cells ; Chemokines/chemistry ; Chemokines/metabolism ; Cricetinae ; Cricetulus ; Humans ; Protein Binding/physiology ; Receptors, Interleukin-8B/metabolism

Czasopismo naukowe

na półce

Pełny tekst Szczegóły

Skocz do pozycji: 4.

Tytuł:: Antidote to cannabinoid intoxication: the CB 1 receptor inverse agonist, AM251, reverses hypothermic effects of the CB 1 receptor agonist, CB-13, in mice.
Autorzy:: Pryce G; Blizard Institute, Barts and the London School of Medicine and Dentistry, Queen Mary University of London, London, UK.
Baker D; Blizard Institute, Barts and the London School of Medicine and Dentistry, Queen Mary University of London, London, UK.; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2017 Nov; Vol. 174 (21), pp. 3790-3794. Date of Electronic Publication: 2017 Sep 20.
Typ publikacji:: Journal Article
MeSH Terms:: Antidotes/*pharmacology
Cannabinoid Receptor Agonists/*poisoning
Naphthalenes/*poisoning
Piperidines/*pharmacology
Pyrazoles/*pharmacology
Animals ; Drug Inverse Agonism ; Female ; Hypothermia/chemically induced ; Hypothermia/prevention & control ; Mice ; Mice, Biozzi ; Receptor, Cannabinoid, CB1/drug effects ; Receptor, Cannabinoid, CB1/metabolism

Czasopismo naukowe

na półce

Pełny tekst Pełny tekst Szczegóły

Skocz do pozycji: 5.

Tytuł:: The atypical antipsychotics clozapine and olanzapine promote down-regulation and display functional selectivity at human 5-HT7 receptors.
Autorzy:: Andressen KW; Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway.; K.G. Jebsen Cardiac Research Centre and Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Oslo, Norway.
Manfra O; Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway.; K.G. Jebsen Cardiac Research Centre and Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Oslo, Norway.
Brevik CH; Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway.
Ulsund AH; Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway.; K.G. Jebsen Cardiac Research Centre and Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Oslo, Norway.
Vanhoenacker P; Laboratory of Eukaryotic Gene Expression and Signal Transduction, Ghent University, Ghent, Belgium.; Intrexon ActoBiotics N.V., Technologiepark 4, Zwijnaarde, Belgium.
Levy FO; Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway.; K.G. Jebsen Cardiac Research Centre and Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Oslo, Norway.
Krobert KA; Department of Pharmacology, Institute of Clinical Medicine, University of Oslo and Oslo University Hospital, Oslo, Norway.; K.G. Jebsen Cardiac Research Centre and Center for Heart Failure Research, Faculty of Medicine, University of Oslo, Oslo, Norway.; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2015 Aug; Vol. 172 (15), pp. 3846-60. Date of Electronic Publication: 2015 Jun 12.
Typ publikacji:: Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms:: Antipsychotic Agents/*pharmacology
Benzodiazepines/*pharmacology
Clozapine/*pharmacology
Down-Regulation/*drug effects
Receptors, Serotonin/*metabolism
Arrestins/metabolism ; Cells, Cultured ; Chloroquine/pharmacology ; Drug Inverse Agonism ; Ergolines/pharmacology ; HEK293 Cells ; Humans ; Ligands ; Lysosomes/drug effects ; Lysosomes/metabolism ; Olanzapine ; Phenols/pharmacology ; Radioligand Assay ; Receptors, Serotonin/genetics ; Serotonin/pharmacology ; Serotonin Antagonists/pharmacology ; Serotonin Receptor Agonists/pharmacology ; Signal Transduction/drug effects ; Sulfonamides/pharmacology ; beta-Arrestins

Czasopismo naukowe

na półce

Pełny tekst Pełny tekst Szczegóły

Skocz do pozycji: 6.

Tytuł:: Brain RVD-haemopressin, a haemoglobin-derived peptide, inhibits bombesin-induced central activation of adrenomedullary outflow in the rat.
Autorzy:: Tanaka K; Department of Pharmacology, Kochi University School of Medicine, Nankoku, Japan.
Shimizu T
Yanagita T
Nemoto T
Nakamura K
Taniuchi K
Dimitriadis F
Yokotani K
Saito M; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2014 Jan; Vol. 171 (1), pp. 202-13.
Typ publikacji:: Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms:: Adrenal Medulla/*drug effects
Adrenal Medulla/*innervation
Bombesin/*pharmacology
Cannabinoid Receptor Agonists/*pharmacology
Epinephrine/*blood
Hemoglobins/*pharmacology
Norepinephrine/*blood
Paraventricular Hypothalamic Nucleus/*drug effects
Peptide Fragments/*pharmacology
Spinal Nerves/*drug effects
Adrenal Medulla/metabolism ; Animals ; Bombesin/administration & dosage ; Cannabinoid Receptor Agonists/administration & dosage ; Cattle ; Cells, Cultured ; Chromaffin Cells/drug effects ; Chromaffin Cells/metabolism ; Dose-Response Relationship, Drug ; Drug Inverse Agonism ; Epinephrine/metabolism ; Hemoglobins/administration & dosage ; Injections, Intraventricular ; Male ; Norepinephrine/metabolism ; Paraventricular Hypothalamic Nucleus/metabolism ; Peptide Fragments/administration & dosage ; Rats ; Rats, Wistar ; Receptor, Cannabinoid, CB1/agonists ; Receptor, Cannabinoid, CB1/metabolism ; Spinal Nerves/metabolism ; Time Factors

Czasopismo naukowe

na półce

Pełny tekst Pełny tekst Szczegóły

Skocz do pozycji: 7.

Tytuł:: Signalling profile differences: paliperidone versus risperidone.
Autorzy:: Clarke WP; Department of Pharmacology, University of Texas Health Science Center, San Antonio, TX, USA.
Chavera TA
Silva M
Sullivan LC
Berg KA; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2013 Oct; Vol. 170 (3), pp. 532-45.
Typ publikacji:: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms:: Antipsychotic Agents/*pharmacology
Isoxazoles/*pharmacology
Pyrimidines/*pharmacology
Risperidone/*pharmacology
Signal Transduction/*drug effects
Adenylyl Cyclases/metabolism ; Animals ; Antipsychotic Agents/chemistry ; Arrestins/metabolism ; CHO Cells ; Cricetinae ; Cricetulus ; Dopamine Agonists/pharmacology ; Dose-Response Relationship, Drug ; Drug Inverse Agonism ; Extracellular Signal-Regulated MAP Kinases/metabolism ; Histamine Agonists/pharmacology ; Humans ; Isoxazoles/chemistry ; Molecular Structure ; Paliperidone Palmitate ; Pyrimidines/chemistry ; Receptor, Serotonin, 5-HT2A/drug effects ; Receptor, Serotonin, 5-HT2A/genetics ; Receptor, Serotonin, 5-HT2A/metabolism ; Receptor, Serotonin, 5-HT2C/drug effects ; Receptor, Serotonin, 5-HT2C/genetics ; Receptor, Serotonin, 5-HT2C/metabolism ; Receptors, Dopamine D2/drug effects ; Receptors, Dopamine D2/genetics ; Receptors, Dopamine D2/metabolism ; Receptors, Histamine H1/drug effects ; Receptors, Histamine H1/genetics ; Receptors, Histamine H1/metabolism ; Risperidone/chemistry ; Serotonin Receptor Agonists/pharmacology ; Structure-Activity Relationship ; Transfection ; beta-Arrestins

Czasopismo naukowe

na półce

Pełny tekst Pełny tekst Szczegóły

Skocz do pozycji: 8.

Tytuł:: Pharmacological modulation of the endocannabinoid signalling alters binge-type eating behaviour in female rats.
Autorzy:: Scherma M; Department of Biomedical Science, Section of Neuroscience and Clinical Pharmacology, University of Cagliari, Monserrato (Cagliari), Italy.
Fattore L
Satta V
Businco F
Pigliacampo B
Goldberg SR
Dessi C
Fratta W
Fadda P; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2013 Jun; Vol. 169 (4), pp. 820-33.
Typ publikacji:: Comparative Study; Journal Article; Research Support, N.I.H., Intramural; Research Support, Non-U.S. Gov't
MeSH Terms:: Disease Models, Animal*
Binge-Eating Disorder/*drug therapy
Cannabinoid Receptor Antagonists/*therapeutic use
Endocannabinoids/*antagonists & inhibitors
Piperidines/*therapeutic use
Pyrazoles/*therapeutic use
Receptor, Cannabinoid, CB1/*antagonists & inhibitors
Signal Transduction/*drug effects
Animals ; Behavior, Animal/drug effects ; Binge-Eating Disorder/chemically induced ; Binge-Eating Disorder/metabolism ; Cannabinoid Receptor Agonists/administration & dosage ; Cannabinoid Receptor Agonists/toxicity ; Cannabinoid Receptor Antagonists/administration & dosage ; Dose-Response Relationship, Drug ; Dronabinol/administration & dosage ; Dronabinol/toxicity ; Drug Inverse Agonism ; Drug Tolerance ; Endocannabinoids/agonists ; Endocannabinoids/metabolism ; Energy Intake/drug effects ; Feeding Behavior/drug effects ; Female ; Margarine/adverse effects ; Piperidines/administration & dosage ; Pyrazoles/administration & dosage ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Receptor, Cannabinoid, CB1/agonists ; Receptor, Cannabinoid, CB1/metabolism ; Rimonabant ; Weight Loss/drug effects

Czasopismo naukowe

na półce

Pełny tekst Pełny tekst Szczegóły

Skocz do pozycji: 9.

Tytuł:: Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors.
Autorzy:: Marini P; School of Medical Sciences, Institute of Medical Sciences, University of Aberdeen, Aberdeen, UK. />Cascio MG
King A
Pertwee RG
Ross RA; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2013 Jun; Vol. 169 (4), pp. 887-99.
Typ publikacji:: Comparative Study; Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
MeSH Terms:: Analgesics/*metabolism
Cannabinoid Receptor Agonists/*metabolism
Receptor, Cannabinoid, CB2/*metabolism
Spleen/*metabolism
Analgesics/pharmacology ; Animals ; CHO Cells ; Cannabinoid Receptor Agonists/pharmacology ; Cell Membrane/metabolism ; Cricetulus ; Cyclic AMP/metabolism ; Drug Inverse Agonism ; Guanosine 5'-O-(3-Thiotriphosphate)/metabolism ; Humans ; Ligands ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Rats ; Rats, Wistar ; Receptor, Cannabinoid, CB2/agonists ; Receptor, Cannabinoid, CB2/genetics ; Recombinant Proteins/chemistry ; Recombinant Proteins/metabolism ; Reproducibility of Results ; Spleen/drug effects

Czasopismo naukowe

na półce

Pełny tekst Pełny tekst Szczegóły

Skocz do pozycji: 10.

Tytuł:: Use of the GTPγS ([35S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and efficacy at G protein-coupled receptors.
Autorzy:: Strange PG; School of Pharmacy, University of Reading, Whiteknights, Reading, UK.; Pokaż więcej
Źródło:: British journal of pharmacology [Br J Pharmacol] 2010 Nov; Vol. 161 (6), pp. 1238-49.
Typ publikacji:: Journal Article; Research Support, Non-U.S. Gov't; Review
MeSH Terms:: Guanosine 5'-O-(3-Thiotriphosphate)/*metabolism
Radioligand Assay/*statistics & numerical data
Receptors, G-Protein-Coupled/*metabolism
Animals ; Drug Inverse Agonism ; Humans ; Ligands ; Radioligand Assay/methods ; Sulfur Radioisotopes/metabolism