Keywords: آگونیست معکوس; cannabinoid; CB2; chronic kidney disease; inverse agonist; renal fibrosis;
مقالات ISI آگونیست معکوس (ترجمه نشده)
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Keywords: آگونیست معکوس; Inverse agonist; Antagonist; Serotonin; 5-HT2A;
Keywords: آگونیست معکوس; 1,2,4-Triazole scaffold; Ghrelin receptor (GHS-R1a); Structural modulation; Chirality; Inverse agonist; Antagonist;
Keywords: آگونیست معکوس; CWNOJCWGIAESTH-LMDOGRNLSA-N; JCPWXJQJNJMDKE-XECWOPBBSA-N; PFHMOHCRGXRQJW-IBURTVSXSA-Nδ opioid receptor; Inverse agonist; NTI derivative; Fluoroalkyl substituent
Keywords: آگونیست معکوس; GhrelinR; Inverse agonist; Anti-obesity; Nicotinamide;
Keywords: آگونیست معکوس; GhrelinR; Inverse agonist; 2-Aminoalkyl nicotinamide; Obesity;
Blocking constitutive activity of GHSR1a in the lateral amygdala facilitates acquisition of conditioned taste aversion
Keywords: آگونیست معکوس; Ghrelin; GHSR1a; CTA; lateral amygdala; inverse agonist; constitutive activity;
The tamoxifen derivative ridaifen-B is a high affinity selective CB2 receptor inverse agonist exhibiting anti-inflammatory and anti-osteoclastogenic effects
Keywords: آگونیست معکوس; Cannabinoid receptors; G-protein coupled receptors; Inverse agonist; Antagonist; Drug action; AC; adenylyl cyclase; CB1R; cannabinoid receptor type 1; CB2R; cannabinoid receptor type 2; CHO; Chinese hamster ovary; CP-55,940; 5-(1,1-dimethylheptyl)-2-[5-hy
Discovery of orally efficacious RORγt inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives
Keywords: آگونیست معکوس; RORγt; retinoic acid receptor-related orphan receptor-gamma t; EAE; experimental autoimmune encephalomyelitis; BODIPY; boron-dipyrromethene; TR-FRET; time-resolved fluorescence resonance energy transfer; SAR; structure-activity relationship; IFN-γ; inte
Rimonabant, a potent CB1 cannabinoid receptor antagonist, is a Gαi/o protein inhibitor
Keywords: آگونیست معکوس; Bioluminescence resonance energy transfer (BRET); Cannabinoid receptor type 1 (CB1); CB1-receptor antagonist; Inverse agonist; G protein; G protein-coupled receptor (GPCR);
Identification and biological evaluation of thiazole-based inverse agonists of RORγt
Keywords: آگونیست معکوس; Retinoid-related orphan receptor gamma t; RORc; RORγt; Thiazole; Inverse agonist;
Identification of novel quinazolinedione derivatives as RORγt inverse agonist
Keywords: آگونیست معکوس; AUC; area under the plasma concentration-time curve; BA; bioavailability; EAE; experimental autoimmune encephalomyelitis; LBD; ligand-binding domain; RORγt; retinoic acid receptor-related orphan receptor-gamma t; SAR; structure-activity relationship; T
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds
Keywords: آگونیست معکوس; Retinoic acid receptor-related orphan receptor-gamma t (RORγt); Inverse agonist; Autoimmune disease; Th17; IL-17; Phenylglycinamide;
GABAergic over-inhibition, a promising hypothesis for cognitive deficits in Down syndrome
Keywords: آگونیست معکوس; Down syndrome; GABA; Inhibition; GABAalpha5; Inverse agonist;
Cannabinoid CB1 receptor inverse agonist MJ08 stimulates glucose production via hepatic sympathetic innervation in rats
Keywords: آگونیست معکوس; SR141716 (PubChem CID: 104850); WIN 55,212-2 (PubChem CID: 6604176); Propranolol (PubChem CID: 4946); Reserpine (PubChem CID: 5770); NF449 (PubChem CID: 4470); H89 (PubChem CID: 449241); Cannabinoid CB1 receptor; Inverse agonist; Hepatic glucose productio
In vivo pharmacological profile of S 38093, a novel histamine H3 receptor inverse agonist
Keywords: آگونیست معکوس; H3; Antagonist; Inverse agonist; Microdialysis; Memory tests; Arousal;
Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors
Keywords: آگونیست معکوس; H3; Antagonist; Inverse agonist; Functionality; Pharmacokinetics; Electrophysiology;
Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt
Keywords: آگونیست معکوس; RORγt; Retinoic acid-related orphan nuclear receptor gamma t; Agonist; Neutral antagonist; Inverse agonist; Th17; IL-17;
Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu5 negative allosteric modulation
Keywords: آگونیست معکوس; mGlu5; Isomers; Partial efficacy; NAM; Antagonist; Inverse agonist;
Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists
Keywords: آگونیست معکوس; Cannabinoid receptor; CB1 receptor; Inverse agonist; Peripheral selectivity; Peripherally restricted;
Tetrahydropyrazolo[4,3-c]pyridine derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists
Keywords: آگونیست معکوس; Cannabinoid receptor; CB1 receptor; Inverse agonist; Peripheral selectivity; Peripherally restricted;
Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties
Keywords: آگونیست معکوس; RORc; RORγ; Inverse agonist; IL-17; PBMCs; Oxa-sultam
AC-3933, a benzodiazepine partial inverse agonist, improves memory performance in MK-801-induced amnesia mouse model
Keywords: آگونیست معکوس; AC-3933; 5-(3-methoxyphenyl)-3-(5-methyl-1, 2, 4-oxadiazol-3-yl)-1, 6-naphthyridin-2(1H)-one; ACh; acetylcholine; AD; Alzheimer's disease; FG-7142; β-carboline-3-carboxylic acid methyl amide; i.p.; intraperitoneally; NMDA; N-methyl-d-aspartate; p.o.; per
Characterization of a selective inverse agonist for estrogen related receptor α as a potential agent for breast cancer
Keywords: آگونیست معکوس; Estrogen related receptor α; Inverse agonist; Breast cancer xenograft; Antitumor agent; Proliferation; Migration
Identification of N-phenyl-2-(N-phenylphenylsulfonamido)acetamides as new RORγ inverse agonists: Virtual screening, structure-based optimization, and biological evaluation
Keywords: آگونیست معکوس; Nuclear receptor; RORγ; Virtual screening; Molecular docking; Similarity-based screening; Inverse agonist; Autoimmune diseases; ZIOFMOWAXVRBME-UHFFFAOYSA-N; UHKZIAKQZPIMKJ-UHFFFAOYSA-N; HPUXMFXWXXZHQJ-UHFFFAOYSA-N; MIMLZOYRWZJUFW-UHFFFAOYSA-N; RAFBFRPGEX
Development of CINPA1 analogs as novel and potent inverse agonists of constitutive androstane receptor
Keywords: آگونیست معکوس; Constitutive androstane receptor; CINPA1; Inverse agonist; TR-FRETCAR, constitutive androstane receptor; PXR, pregnane X receptor; NR, nuclear receptor; CYP2Bs, cytochrome P450, family 2, subfamily B proteins; CYP2Cs, cytochrome P450, family 2, subfamily
Post-translational regulation of RORγt-A therapeutic target for the modulation of interleukin-17-mediated responses in autoimmune diseases
Keywords: آگونیست معکوس; Retinoic acid-related orphan receptor gamma; Nuclear receptor; Interleukin-17; Inverse agonist; Ubiquitinylation; Posttranslational regulation;
Nucleus accumbens shell excitability is decreased by methamphetamine self-administration and increased by 5-HT2C receptor inverse agonism and agonism
Keywords: آگونیست معکوس; Methamphetamine; Serotonin; Nucleus accumbens; Constitutive activity; Inverse agonist; 5-HT2C;
Synthesis and biological evaluation of (3â²,5â²-dichloro-2,6-dihydroxy-biphenyl-4-yl)-aryl/alkyl-methanone selective CB2 inverse agonist
Keywords: آگونیست معکوس; Cannabinoid; Inverse agonist; CB2 receptor; cAMP stimulation; ACTOne assay;
The identification of GPR3 inverse agonist AF64394; The first small molecule inhibitor of GPR3 receptor function
Keywords: آگونیست معکوس; GPR3; GPR6; GPR12; G protein coupled receptor; Orphan receptor; Inverse agonist; AF64394
CB2 cannabinoid receptor is a novel target for third-generation selective estrogen receptor modulators bazedoxifene and lasofoxifene
Keywords: آگونیست معکوس; SERM; selective estrogen receptor modulator; CB1; cannabinoid receptor 1; CB2; cannabinoid receptor 2; GPCR; G protein-coupled receptor; FDA; food and drug administration; HTRF; homogenous time resolved fluorescence; Cannabinoid receptor; Inverse agonist;
Procognitive effect of AC-3933 in aged mice, and synergistic effect of combination with donepezil in scopolamine-treated mice
Keywords: آگونیست معکوس; AC-3933; 5-(3-methoxyphenyl)-3-(5-methyl-1, 2, 4-oxadiazol-3-yl)-1, 6-naphthyridin-2(1H)-one; ACh; acetylcholine; AChE; acetylcholinesterase; β-CCM; β-carboline-3-carboxylate; GABA; γ-aminobutyric acid; i.p.; intraperitoneally; Tween® 80; polyoxyethyl
In vivo pharmacological characterization of AC-3933, a benzodiazepine receptor partial inverse agonist for the treatment of Alzheimer's disease
Keywords: آگونیست معکوس; AC-3933; 5-(3-methoxyphenyl)-3-(5-methyl-1,2,4-oxadiazol-3-yl)-1,6-naphthyridin-2(1H)-one; ACh; acetylcholine; AD; Alzheimer's disease; ANOVA; analysis of variance; β-CCM; beta-carboline-3-carboxylate; BzR; benzodiazepine receptor; EEG; electroencephal
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand
Keywords: آگونیست معکوس; ROR; Phenanthridinone; Inverse agonist; LXR;
Treating enhanced GABAergic inhibition in Down syndrome: Use of GABA α5-selective inverse agonists
Keywords: آگونیست معکوس; Down syndrome; γ-Aminobutyric acid; Inverse agonist; α5-Subunit containing GABAA receptor; Convulsion; Behavior;
Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor
Keywords: آگونیست معکوس; Ghrelin; Antagonist; Inverse agonist; Receptor; Receptor occupancy; Muscarinic;
CB1 and CB2 receptors are novel molecular targets for Tamoxifen and 4OH-Tamoxifen
Keywords: آگونیست معکوس; 4OH-Tam; 4OH-Tamoxifen; AC; adenylyl cyclase; CB1R; cannabinoid receptor type 1; CB2R; cannabinoid receptor type 2; CHO; Chinese hamster ovary; CP-55,940; 5-(1,1-dimethylheptyl)-2-[5-hydroxy-2-(3-hydroxypropyl)cyclohexyl]phenol; DMEM; Dulbecco's modific
Research reportPWZ-029, an inverse agonist selective for α5 GABAA receptors, improves object recognition, but not water-maze memory in normal and scopolamine-treated rats
Keywords: آگونیست معکوس; GABA; Inverse agonist; Memory; Object recognition; Water maze;
Selective GABAA α5 positive allosteric modulators improve cognitive function in aged rats with memory impairment
Keywords: آگونیست معکوس; GABA agonist; Inverse agonist; Neural hyperactivity; Water maze; Radial arm maze; Mild cognitive impairment;
Activation of MAPK by inverse agonists in six naturally occurring constitutively active mutant human melanocortin-4 receptors
Keywords: آگونیست معکوس; Melanocortin-4 receptor; Inverse agonist; Biased signaling; Constitutive activity;
Peripherally restricted CB1 receptor blockers
Keywords: آگونیست معکوس; Cannabinoid receptor blocker; Inverse agonist; Silent antagonist; Peripherally restricted; CB1-antagonist; Obesity; Diabetes; Metabolic disorders; Liver diseases; Rimonabant; AM6545; JD5037;
FG7142, yohimbine, and βCCE produce anxiogenic-like effects in the elevated plus-maze but do not affect brainstem activated hippocampal theta
Keywords: آگونیست معکوس; Hippocampus; Oscillation; Anxiety; Benzodiazepine receptor; α2 Adrenergic; Theta suppression model; Anxiogenesis; Inverse agonist; Elevated plus-maze
Identification of raloxifene as a novel CB2 inverse agonist
Keywords: آگونیست معکوس; CB1, cannabinoid receptor 1; CB2, cannabinoid receptor 2; GPCR, G protein-coupled receptor; FDA, food and drug administration; HTRF, homogenous time-resolved fluorescenceCannabinoid receptor; Inverse agonist; Drug repurposing; Raloxifene; Osteoporosis
Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists
Keywords: آگونیست معکوس; Phenoxypropyl-(R)-2-methylpyrrolidine; CEP-26401 irdabisant; Histamine H3 receptor; Inverse agonist; Sleep-wake
Research reportDMCM, a benzodiazepine site inverse agonist, improves active avoidance and motivation in the rat
Keywords: آگونیست معکوس; GABAA receptor; Inverse agonist; Depression; Memory; Forced swim test; Active avoidance;
Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists
Keywords: آگونیست معکوس; Histamine; H3 antagonist; Inverse agonist; Benzocinnolinone;
An efficient synthesis of 3-OBn-6β,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist
Keywords: آگونیست معکوس; Naltrexone; Naltrexol; Antagonist; Inverse Agonist; Opiate; 6β,14-Epoxymorphinan; Conformation; Rigid analog;
CommentaryCognitive enhancement by pharmacological and behavioral interventions: the murine Down syndrome model
Keywords: آگونیست معکوس; Alpha5 GABA-A receptor; Inverse agonist; RO4938581; Alpha5 IA; Ts65Dn mice;
Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor
Keywords: آگونیست معکوس; Ghrelin; GHS-R1a; Antagonist; Inverse agonist; Spirocyclic; Piperidine-azetidine;
Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selective α1B-adrenoceptor antagonist
Keywords: آگونیست معکوس; WB4101 analogues; 8-Substituted 1,4-benzodioxane; α1-Adrenoreceptor; 5-HT1A receptor; Binding affinity; Antagonist affinity; Inverse agonist