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Published in 2018 at "Archives of Toxicology"
DOI: 10.1007/s00204-018-2270-4
Abstract: Upon liver intoxication with malnutrition or high-fat diet feeding, fibrinogen is synthesized by hepatocytes and secreted into the blood in human and mouse. Its primary function is to occlude blood vessels upon damage and thereby…
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Keywords:
fat diet;
inverse agonist;
fibrinogen;
high fat ... See more keywords
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1
Published in 2017 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2017.09.001
Abstract: GPR12 is a constitutively active, Gs protein-coupled receptor that currently has no confirmed endogenous ligands. GPR12 may be involved in physiological processes such as maintenance of oocyte meiotic arrest and brain development, as well as…
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Keywords:
inverse agonist;
cbd;
agonist gpr12;
cancer ... See more keywords
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Published in 2017 at "European Journal of Pharmacology"
DOI: 10.1016/j.ejphar.2017.03.013
Abstract: Abstract Histaminergic H3 inverse agonists, by stimulating central histamine release, represent attractive drug candidates to treat cognitive disorders. The present studies aimed to describe the mechanistic profile of S 38093 a novel H3 receptors inverse…
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Keywords:
inverse agonist;
human receptors;
novel inverse;
agonist ... See more keywords
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Published in 2018 at "iScience"
DOI: 10.1016/j.isci.2018.06.012
Abstract: Summary Peroxisome proliferator activated receptor γ (PPARγ) is a nuclear receptor and target for antidiabetics that increase insulin sensitivity. Owing to the side effects of PPARγ full agonists, research has recently focused on non-activating ligands…
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Keywords:
ppar;
inverse agonist;
activation helix;
helix ... See more keywords
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Published in 2018 at "Toxicology and Applied Pharmacology"
DOI: 10.1016/j.taap.2018.06.009
Abstract: &NA; Selective estrogen receptor modulators (SERMs) target estrogen receptors (ERs) to treat breast cancer and osteoporosis. Several SERMs exhibit anti‐cancer activity not related to ERs. To discover novel anti‐cancer drugs acting via ER‐independent mechanisms, derivatives…
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Keywords:
anti inflammatory;
inverse agonist;
high affinity;
affinity ... See more keywords
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Published in 2018 at "Biomacromolecules"
DOI: 10.1021/acs.biomac.8b00158
Abstract: Osteoarthritis (OA) results from degenerative and abnormal function of joints, with localized biochemistry playing a critical role in its onset and progression. As high levels of all- trans retinoic acid (ATRA) in synovial fluid have…
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Keywords:
protein;
inverse agonist;
delivery;
osteoarthritis ... See more keywords
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Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00392
Abstract: The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to…
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Keywords:
acid receptor;
inverse agonist;
receptor related;
retinoic acid ... See more keywords
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Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c06060
Abstract: A-9758 is an inverse agonist of retinoic acid-related orphan receptor γt with well-characterized in vitro and in vivo anti-inflammatory activity. A chromatography-free decagram-scale synthesis of this compound was developed to support pre-clinical research activities. This…
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Keywords:
acid related;
agonist retinoic;
acid;
9758 inverse ... See more keywords
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Published in 2021 at "Translational Psychiatry"
DOI: 10.1038/s41398-021-01430-7
Abstract: The status of serotonin 5HT 2A receptors (5HT 2A Rs) in schizophrenia has been controversial. In vivo positron emission tomography neuroimaging and in vitro post-mortem binding studies have reported conflicting results about 5HT 2A R…
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Keywords:
inverse agonist;
pharmacological profile;
subjects schizophrenia;
density ... See more keywords
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Published in 2020 at "Sleep"
DOI: 10.1093/sleep/zsaa056.070
Abstract: Narcolepsy is a chronic sleep disorder characterized by overwhelming daytime drowsiness, sudden attacks of sleep and sometimes accompanied by cataplexy. Although the orexin deficiency is considered to be the primary cause of this disorder, lot…
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Keywords:
suvn g3031;
inverse agonist;
histamine;
g3031 ... See more keywords
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Published in 2023 at "SLEEP"
DOI: 10.1093/sleep/zsad077.0051
Abstract: Samelisant (SUVN-G3031) is a potent and selective histamine 3 receptor (H3R) inverse agonist with hH3 Ki of 8.7 nM. Samelisant exhibited desired pharmacokinetic properties and favorable brain penetration in rodents. Preclinical studies demonstrated samelisant produced…
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Keywords:
samelisant;
daytime sleepiness;
excessive daytime;
treatment ... See more keywords