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British Journal of Pharmacology, ISSN 0007-1188, 02/1999, Volume 126, Issue 3, pp. 665 - 672
We have tested our prediction that AM630 is a CB2 cannabinoid receptor ligand and also investigated whether L759633 and L759656, are CB2 receptor agonists.... 
AM630 | CB2‐selective ligands | L759656 | CB2‐selective inverse agonist | [35S]‐GTPγS | CB2‐selective agonist | cyclic AMP | Cannabinoid CB1 and CB2 receptors | L759633 | Cannabinoid CB | selective agonist | receptors | Cyclic AMP | selective ligands | and CB | selective inverse agonist | S]-GTPγS | ANTAGONIST | cannabinoid CB1 and CB2 receptors | [S-35]-GTP gamma S | CB2-selective agonist | CB2-selective ligands | CB2-selective inverse agonist | PHARMACOLOGY | PHARMACOLOGY & PHARMACY | BINDING | BRAIN | Guanosine 5'-O-(3-Thiotriphosphate) - pharmacology | Cannabinoids - antagonists & inhibitors | Humans | Bornanes - pharmacology | Tritium | Benzoxazines | Receptors, Drug - agonists | Cyclohexanols - metabolism | Chromans - pharmacology | Indoles - pharmacology | Cyclohexanols - pharmacology | Radioligand Assay | Naphthalenes - metabolism | Cannabinoids - metabolism | Cyclic AMP - metabolism | CHO Cells | Pyrazoles - pharmacology | Cricetinae | Colforsin - pharmacology | Morpholines - pharmacology | Morpholines - metabolism | Pyrazoles - metabolism | Receptors, Drug - metabolism | Naphthalenes - pharmacology | Binding, Competitive - drug effects | Guanosine 5'-O-(3-Thiotriphosphate) - metabolism | Animals | Bornanes - metabolism | Receptors, Cannabinoid | Receptors, Drug - antagonists & inhibitors | Papers | [35S]-GTPγS
Journal Article
ACS MEDICINAL CHEMISTRY LETTERS, ISSN 1948-5875, 02/2018, Volume 9, Issue 2, pp. 120 - 124
Biaryl amides as new ROR gamma t modulators were discovered. The crystal structure of biaryl amide agonist 6 in complex with ROR gamma t ligand binding domain... 
CHEMISTRY, MEDICINAL | inverse agonist | NUCLEAR RECEPTORS | ROR gamma t | TARGETING TH17 CELLS | agonist | cocrystal structure | DISCOVERY | AUTOIMMUNE | POTENT | DISEASES | Th17 cell differentiation | MULTIPLE-SCLEROSIS | INTERLEUKIN-17 | DIFFERENTIATION | ANTAGONISTS | biaryl amides
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 06/2019, Volume 29, Issue 12, pp. 1463 - 1470
We have previously reported the syntheses of a series of 3,6-disubstituted quinolines as modulators of the retinoic acid receptor-related orphan receptor gamma... 
Retinoic acid-related orphan nuclear receptor gamma t | Th17 | Inverse agonist | IL-17 | RORγt | gamma t | CHEMISTRY, MEDICINAL | LIGANDS | PATHWAY | ROR gamma t | CHEMISTRY, ORGANIC | Retinoic acid-related orphan nuclear receptor
Journal Article
Journal Article
by Sun, NN and Yuan, CM and Ma, XJ and Wang, YH and Gu, XF and Fu, W
MOLECULES, ISSN 1420-3049, 12/2018, Volume 23, Issue 12
As an attractive drug-target, retinoic acid receptor-related orphan receptor-gamma-t (RORt) has been employed widely to develop clinically relevant small... 
CELLS | inverse agonist | MODULATORS | BIOCHEMISTRY & MOLECULAR BIOLOGY | GAMMA-T | agonist | CHEMISTRY, MULTIDISCIPLINARY | DISCOVERY | NUCLEAR RECEPTOR | POTENT | RORt | molecular mechanism of action (MOA) | DERIVATIVES
Journal Article
Neuropharmacology, ISSN 0028-3908, 10/2012, Volume 63, Issue 5, pp. 905 - 915
Mu-opioid and CB1-cannabinoid agonists produce analgesia; however, adverse effects limit use of drugs in both classes. Additive or synergistic effects... 
Analgesia | Morphine | Marijuana | G-protein | Adenylyl cyclase | CB1 receptors | AGONIST MORPHINE | ACTIVATION | PROTEIN-KINASE | CB1 CANNABINOID RECEPTOR | SYNERGISTIC INTERACTIONS | NEUROSCIENCES | INHIBITION | KAPPA | FULL AGONIST | ADENYLYL-CYCLASE | PHARMACOLOGY & PHARMACY | RAT-BRAIN | Pyrazoles - therapeutic use | Receptor, Cannabinoid, CB2 - agonists | Humans | Analgesics, Opioid - pharmacology | Receptors, Opioid, mu - agonists | Piperidines - pharmacology | Cannabinoid Receptor Agonists - therapeutic use | Recombinant Proteins - antagonists & inhibitors | Piperidines - metabolism | Receptors, Opioid, mu - metabolism | Morpholines - metabolism | Analgesics, Non-Narcotic - metabolism | Drug Inverse Agonism | Mice | Analgesics, Opioid - metabolism | Kinetics | Receptor, Cannabinoid, CB1 - antagonists & inhibitors | Analgesics, Opioid - antagonists & inhibitors | Cannabinoid Receptor Agonists - metabolism | Cricetulus | Analgesics, Non-Narcotic - pharmacology | Cannabinoid Receptor Agonists - pharmacology | Receptor, Cannabinoid, CB2 - genetics | Analgesics, Opioid - adverse effects | Narcotic Antagonists - metabolism | Receptor, Cannabinoid, CB1 - agonists | Analgesics, Non-Narcotic - adverse effects | Cannabinoid Receptor Agonists - adverse effects | Morpholines - adverse effects | CHO Cells | Pyrazoles - adverse effects | Pyrazoles - pharmacology | Binding, Competitive | Recombinant Proteins - metabolism | Cricetinae | Morpholines - pharmacology | Narcotic Antagonists - adverse effects | Recombinant Proteins - agonists | Analgesics, Non-Narcotic - therapeutic use | Pyrazoles - metabolism | Mice, Inbred Strains | Receptors, Opioid, mu - antagonists & inhibitors | Receptor, Cannabinoid, CB1 - metabolism | Receptor, Cannabinoid, CB2 - metabolism | Animals | Narcotic Antagonists - therapeutic use | Piperidines - therapeutic use | Narcotic Antagonists - pharmacology | Piperidines - adverse effects | Receptors, Opioid, mu - genetics | Index Medicus | Drugs | Pain perception | Opioid receptors | Cyclic AMP | Opioid receptors (type mu) | Antagonists | Cannabinoid CB1 receptors | Guanine nucleotide-binding protein | Antagonism | Cell activation | Side effects | Inverse agonists | CB1 Receptors | Adenylyl Cyclase
Journal Article
European Neuropsychopharmacology, ISSN 0924-977X, 2016, Volume 27, Issue 1, pp. 87 - 90
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 05/2019, Volume 176, Issue 10, pp. 1481 - 1491
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 08/2019, Volume 27, Issue 16, pp. 3632 - 3649
Antagonists of type 1 cannabinoid receptors (CB1) may be useful in treating diabetes, hepatic disorders, and fibrosis. Otenabant ( ) is a potent and selective... 
CB2 | CB1 | Peripheral | Endocannabinoid | Inverse agonist | Purine | Antagonist | Cannabinoid | Otenabant | Blood brain barrier | INTERFERENCE COMPOUNDS PAINS | DESIGN | CHEMISTRY, MEDICINAL | PERMEABILITY | EFFICACY | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | ENDOCANNABINOID SYSTEM | CHEMISTRY, ORGANIC | DISCOVERY | BLOCKERS | ANTAGONISTS | BINDING | Purines | Alkaloids | Inositol | Amines | Sulfonamides | Depression, Mental | Organic compounds
Journal Article
Biochemistry, ISSN 0006-2960, 06/2010, Volume 49, Issue 22, pp. 4583 - 4600
The melanocortin-4 receptor (MC4R) is a G-protein-coupled receptor (GPCR) that is expressed in the central nervous system and has a role in regulating feeding... 
GENE-MUTATIONS | ALPHA-MELANOTROPIN | BIOCHEMISTRY & MOLECULAR BIOLOGY | CELL-SURFACE EXPRESSION | INVERSE AGONIST | MC4R MUTATIONS | MOLECULAR-CLONING | FUNCTIONAL-CHARACTERIZATION | TETRAPEPTIDE AC-HIS-DPHE-ARG-TRP-NH2 | STIMULATING HORMONE | CHILDHOOD OBESITY | Protein Binding - genetics | alpha-MSH - pharmacology | gamma-MSH - pharmacology | Humans | Molecular Sequence Data | Male | Receptor, Melanocortin, Type 4 - biosynthesis | Obesity - genetics | Pro-Opiomelanocortin - physiology | alpha-MSH - metabolism | beta-MSH - pharmacology | beta-MSH - metabolism | Protein Binding - drug effects | Agouti-Related Protein - antagonists & inhibitors | Amino Acid Sequence | Cell Line | Receptor, Melanocortin, Type 4 - antagonists & inhibitors | gamma-MSH - metabolism | Mutagenesis, Site-Directed | Receptor, Melanocortin, Type 4 - agonists | Receptor, Melanocortin, Type 4 - genetics | Pro-Opiomelanocortin - antagonists & inhibitors | Agouti-Related Protein - metabolism | Obesity - metabolism | Polymorphism, Genetic | Binding, Competitive - drug effects | Gene Expression Regulation - drug effects | Agouti-Related Protein - biosynthesis | Agouti-Related Protein - physiology | Pro-Opiomelanocortin - agonists | Pro-Opiomelanocortin - biosynthesis | alpha-MSH - physiology | Binding, Competitive - genetics | Ligands | alpha-MSH - analogs & derivatives | Antagonists (Biochemistry) | Proteins | Gene mutations | Analysis | Chemical properties | Single nucleotide polymorphisms | Structure
Journal Article
PHARMACOLOGY & THERAPEUTICS, ISSN 0163-7258, 08/2019, Volume 200, pp. 69 - 84
Since the discovery of the histamine H-3 receptor in 1983, tremendous advances in the pharmacological aspects of H-3 receptor antagonists/inverse agonists have... 
ALZHEIMERS-DISEASE | Clinical trials | H3 INVERSE AGONIST | COGNITIVE IMPAIRMENT | ANTAGONIST/INVERSE AGONIST | Pitolisant | H-3-RECEPTOR ANTAGONIST | INTERNATIONAL-LEAGUE | S 38093 | THERAPEUTIC DRUG TARGET | H-3 antagonists | H-3 inverse agonists | DOUBLE-BLIND | PHARMACOLOGY & PHARMACY | Histamine H-3 receptor | Neurological disorders | PROCOGNITIVE PROPERTIES
Journal Article
Nature, ISSN 0028-0836, 02/2012, Volume 482, Issue 7384, pp. 237 - 240
Journal Article