am 251 has been researched along with Obesity in 23 studies
AM 251: an analog of SR141716A; structure given in first source
AM-251 : A carbohydrazide obtained by formal condensation of the carboxy group of 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid with the amino group of 1-aminopiperidine. An antagonist at the CB1 cannabinoid receptor.
Obesity: A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).
| Excerpt | Relevance | Reference |
|---|---|---|
| "Our results indicate that the cannabinoid CB1 inverse agonist AM 251 represents a promising therapeutic strategy for the treatment of obesity and metabolic syndrome." | 7.79 | Novel effects of the cannabinoid inverse agonist AM 251 on parameters related to metabolic syndrome in obese Zucker rats. ( Aranda, P; Errami, M; Galisteo, M; Llopis, J; López-Chaves, C; López-Jurado, M; Martínez, R; Merroun, I; Porres, JM; Sánchez-González, C; Zarzuelo, A, 2013) |
| "Our results indicate that the cannabinoid CB1 inverse agonist AM 251 represents a promising therapeutic strategy for the treatment of obesity and metabolic syndrome." | 3.79 | Novel effects of the cannabinoid inverse agonist AM 251 on parameters related to metabolic syndrome in obese Zucker rats. ( Aranda, P; Errami, M; Galisteo, M; Llopis, J; López-Chaves, C; López-Jurado, M; Martínez, R; Merroun, I; Porres, JM; Sánchez-González, C; Zarzuelo, A, 2013) |
| "Obesity is characterized by chronic low-grade inflammation that contributes to development of cardiometabolic disorders." | 1.51 | Cannabinoid Receptor 1 Blockade Attenuates Obesity and Adipose Tissue Type 1 Inflammation Through miR-30e-5p Regulation of Delta-Like-4 in Macrophages and Consequently Downregulation of Th1 Cells. ( Mehrpouya-Bahrami, P; Miranda, K; Nagarkatti, M; Nagarkatti, PS, 2019) |
| "Obesity is a global public health problem." | 1.48 | Orexin-A and endocannabinoid signaling regulate glucose-responsive arcuate nucleus neurons and feeding behavior in obese rats. ( Guo, F; Sun, X; Wang, M; Xu, L; Yang, D; Zhang, D, 2018) |
| "Weight loss was greater with AM251 than could be accounted for by food restriction (∼25%), an effect likely mediated by the EE response to CB1R inhibition." | 1.38 | Cannabinoid-1 receptor inhibition prevents the reduction of 24-hour energy expenditure with weight loss. ( Achanfuo-Yeboah, J; Cunningham, PK; Faidley, T; Fong, TM; Heymsfield, SB; Hickey, G; Hora, D; Johnson-Levonas, AO; Nicolich, S; Strack, AM; Thompson, D, 2012) |
| "05); the dose-response curve was shifted to the left in the obese." | 1.34 | Effects of cannabinoid receptors on skeletal muscle oxidative pathways. ( Cameron-Smith, D; Cavuoto, P; Hatzinikolas, G; McAinch, AJ; Wittert, GA, 2007) |
| "We determined the effect of a cannabinoid CB1 receptor antagonist (AM-251; N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide) on food intake, body weight and adipose tissue mass in Western diet-induced obese (DIO) mice using a chronic, interrupted, oral dosing paradigm." | 1.32 | Antiobesity effects of chronic cannabinoid CB1 receptor antagonist treatment in diet-induced obese mice. ( Black, SC; Hildebrandt, AL; Kelly-Sullivan, DM, 2003) |
| " However, combined oral dosing of nalmefene and subthreshold doses of AM251, a cannabinoid CB1 receptor inverse agonist, led to a significant reduction in food intake in both lean and diet-induced obese (DIO) mice." | 1.32 | Synergistic effects of cannabinoid inverse agonist AM251 and opioid antagonist nalmefene on food intake in mice. ( Chen, RZ; Fong, TM; Huang, RR; MacNeil, DJ; Shen, CP, 2004) |
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 9 (39.13) | 29.6817 |
| 2010's | 14 (60.87) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| Authors | Studies |
|---|---|
| Kapur, A | 1 |
| Zhao, P | 1 |
| Sharir, H | 1 |
| Bai, Y | 1 |
| Caron, MG | 1 |
| Barak, LS | 1 |
| Abood, ME | 1 |
| Yang, D | 1 |
| Xu, L | 1 |
| Guo, F | 1 |
| Sun, X | 1 |
| Zhang, D | 1 |
| Wang, M | 1 |
| Miranda, K | 1 |
| Mehrpouya-Bahrami, P | 1 |
| Nagarkatti, PS | 1 |
| Nagarkatti, M | 1 |
| Merroun, I | 1 |
| Sánchez-González, C | 1 |
| Martínez, R | 1 |
| López-Chaves, C | 1 |
| Porres, JM | 1 |
| Aranda, P | 1 |
| Llopis, J | 1 |
| Galisteo, M | 1 |
| Zarzuelo, A | 1 |
| Errami, M | 1 |
| López-Jurado, M | 1 |
| Ravussin, Y | 1 |
| Xiao, C | 1 |
| Gavrilova, O | 1 |
| Reitman, ML | 1 |
| Vida, M | 2 |
| Rivera, P | 4 |
| Gavito, AL | 1 |
| Suárez, J | 4 |
| Pavón, FJ | 4 |
| Arrabal, S | 2 |
| Romero-Cuevas, M | 1 |
| Bautista, D | 1 |
| Martínez, A | 1 |
| de Fonseca, FR | 3 |
| Serrano, A | 4 |
| Baixeras, E | 2 |
| Jenkin, KA | 1 |
| O'Keefe, L | 1 |
| Simcocks, AC | 1 |
| Grinfeld, E | 1 |
| Mathai, ML | 1 |
| McAinch, AJ | 2 |
| Hryciw, DH | 1 |
| Lucena, MA | 1 |
| Canduela, MJ | 1 |
| Ramos-Uriarte, A | 1 |
| Decara, J | 1 |
| Vargas, A | 1 |
| Martín-Rufián, M | 1 |
| Márquez, J | 1 |
| Fernández-Llébrez, P | 2 |
| De Roos, B | 1 |
| Grandes, P | 1 |
| Rodríguez de Fonseca, F | 1 |
| González-Mariscal, I | 1 |
| Krzysik-Walker, SM | 1 |
| Kim, W | 1 |
| Rouse, M | 1 |
| Egan, JM | 1 |
| Chen, CC | 1 |
| Lee, TY | 1 |
| Kwok, CF | 1 |
| Hsu, YP | 1 |
| Shih, KC | 1 |
| Lin, YJ | 1 |
| Ho, LT | 1 |
| Mathes, CM | 1 |
| Ferrara, M | 1 |
| Rowland, NE | 1 |
| Judge, MK | 1 |
| Zhang, Y | 1 |
| Scarpace, PJ | 1 |
| Droste, SM | 1 |
| Saland, SK | 1 |
| Schlitter, EK | 1 |
| Rodefer, JS | 1 |
| Romero-Zerbo, Y | 1 |
| López-Ávalos, MD | 1 |
| Cifuentes, M | 2 |
| Grondona, JM | 2 |
| Bermúdez-Silva, FJ | 2 |
| Pérez-Martín, M | 1 |
| Cota, D | 1 |
| Marsicano, G | 1 |
| Strack, AM | 1 |
| Nicolich, S | 1 |
| Faidley, T | 1 |
| Achanfuo-Yeboah, J | 1 |
| Cunningham, PK | 1 |
| Hora, D | 1 |
| Thompson, D | 1 |
| Hickey, G | 1 |
| Johnson-Levonas, AO | 1 |
| Fong, TM | 2 |
| Heymsfield, SB | 1 |
| Luque-Rojas, MJ | 1 |
| Pastor, A | 1 |
| Blanco, E | 1 |
| Crespillo, A | 1 |
| de la Torre, R | 1 |
| Hildebrandt, AL | 1 |
| Kelly-Sullivan, DM | 1 |
| Black, SC | 1 |
| Chen, RZ | 1 |
| Huang, RR | 1 |
| Shen, CP | 1 |
| MacNeil, DJ | 1 |
| Chambers, AP | 1 |
| Sharkey, KA | 1 |
| Koopmans, HS | 1 |
| Cavuoto, P | 1 |
| Hatzinikolas, G | 1 |
| Cameron-Smith, D | 1 |
| Wittert, GA | 1 |
| Irwin, N | 1 |
| Hunter, K | 1 |
| Flatt, PR | 1 |
| Santoro, A | 1 |
| Gazzerro, P | 1 |
| Malfitano, AM | 1 |
| Pisanti, S | 1 |
| Laezza, C | 1 |
| Bifulco, M | 1 |
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| The Effects of Topical Cannabidiol Cream on Post-exercise Recovery[NCT05044936] | Early Phase 1 | 0 participants (Actual) | Interventional | 2023-05-15 | Withdrawn (stopped due to The researchers were not able to acquire funding to initiate the study. Also, the study was not approved by the local IRB which requested a FDA new drug application.) | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
23 other studies available for am 251 and Obesity
| Article | Year |
|---|---|
Atypical responsiveness of the orphan receptor GPR55 to cannabinoid ligands.
Topics: Analgesics; Arrestins; beta-Arrestins; Cannabinoid Receptor Agonists; Cannabinoids; Cell Line; Cyclo | 2009 |
Orexin-A and endocannabinoid signaling regulate glucose-responsive arcuate nucleus neurons and feeding behavior in obese rats.
Topics: Animals; Arcuate Nucleus of Hypothalamus; Disease Models, Animal; Endocannabinoids; Feeding Behavior | 2018 |
Cannabinoid Receptor 1 Blockade Attenuates Obesity and Adipose Tissue Type 1 Inflammation Through miR-30e-5p Regulation of Delta-Like-4 in Macrophages and Consequently Downregulation of Th1 Cells.
Topics: Adaptor Proteins, Signal Transducing; Adipose Tissue; Animals; Calcium-Binding Proteins; Diet, High- | 2019 |
Novel effects of the cannabinoid inverse agonist AM 251 on parameters related to metabolic syndrome in obese Zucker rats.
Topics: Animals; Biomarkers; Cannabinoid Receptor Antagonists; Eating; Energy Metabolism; Fatty Liver; Insul | 2013 |
Effect of intermittent cold exposure on brown fat activation, obesity, and energy homeostasis in mice.
Topics: Adipose Tissue, Brown; Animals; Biomarkers; Body Composition; Body Weight; Cold Temperature; Deoxygl | 2014 |
CB1 blockade potentiates down-regulation of lipogenic gene expression in perirenal adipose tissue in high carbohydrate diet-induced obesity.
Topics: Adipose Tissue, White; Animals; Body Weight; Diet, High-Fat; Dietary Carbohydrates; Down-Regulation; | 2014 |
Chronic administration of AM251 improves albuminuria and renal tubular structure in obese rats.
Topics: Albuminuria; Animals; Collagen; Diet, High-Fat; Humans; Kidney Tubules; Male; Obesity; Piperidines; | 2015 |
Pharmacological Blockade of Cannabinoid CB1 Receptors in Diet-Induced Obesity Regulates Mitochondrial Dihydrolipoamide Dehydrogenase in Muscle.
Topics: Animals; Body Weight; Cell Line; Diet; Dietary Carbohydrates; Dihydrolipoamide Dehydrogenase; Electr | 2015 |
Blockade of cannabinoid 1 receptor improves GLP-1R mediated insulin secretion in mice.
Topics: Animals; Arachidonic Acids; Cannabinoid Receptor Agonists; Cannabinoid Receptor Antagonists; Cell Li | 2016 |
Cannabinoid receptor type 1 mediates high-fat diet-induced insulin resistance by increasing forkhead box O1 activity in a mouse model of obesity.
Topics: Animals; Cannabinoid Receptor Agonists; Citrate (si)-Synthase; Diet, High-Fat; DNA-Binding Proteins; | 2016 |
Selection of a palatable dietary option is not preferentially reduced by cannabinoid CB1 receptor antagonist AM251 in female C57Bl/6J mice.
Topics: Analysis of Variance; Animals; Behavior, Animal; Body Weight; Choice Behavior; Diet; Dietary Fats; D | 2009 |
Responses to the cannabinoid receptor-1 antagonist, AM251, are more robust with age and with high-fat feeding.
Topics: Age Factors; Animals; Appetite Depressants; Body Composition; Dietary Fats; Energy Intake; Hyperphag | 2009 |
AM 251 differentially effects food-maintained responding depending on food palatability.
Topics: Animal Feed; Animals; Appetite Regulation; Appetitive Behavior; Behavior, Animal; Cacao; Cannabinoid | 2010 |
Obesity-dependent cannabinoid modulation of proliferation in adult neurogenic regions.
Topics: Adiponectin; Animals; Blood Glucose; Body Weight; Cannabinoid Receptor Modulators; Cell Proliferatio | 2011 |
New fat and new neurons: endocannabinoids control neurogenesis in obesity (Commentary on Rivera et al.).
Topics: Adipose Tissue; Body Weight; Cannabinoid Receptor Modulators; Dietary Fats; Eating; Endocannabinoids | 2011 |
Cannabinoid-1 receptor inhibition prevents the reduction of 24-hour energy expenditure with weight loss.
Topics: Absorptiometry, Photon; Animals; Disease Models, Animal; Dogs; Eating; Energy Metabolism; Female; Gl | 2012 |
Diet-dependent modulation of hippocampal expression of endocannabinoid signaling-related proteins in cannabinoid antagonist-treated obese rats.
Topics: Amidohydrolases; Animals; Arachidonic Acids; Cannabinoid Receptor Agonists; Cannabinoid Receptor Ant | 2013 |
Antiobesity effects of chronic cannabinoid CB1 receptor antagonist treatment in diet-induced obese mice.
Topics: Animals; Blood Glucose; Body Weight; Cholesterol; Dietary Fats; Dose-Response Relationship, Drug; Ea | 2003 |
Synergistic effects of cannabinoid inverse agonist AM251 and opioid antagonist nalmefene on food intake in mice.
Topics: Animals; Appetite Regulation; Body Weight; Brain; Cannabinoid Receptor Modulators; Cannabinoids; Dos | 2004 |
Cannabinoid (CB)1 receptor antagonist, AM 251, causes a sustained reduction of daily food intake in the rat.
Topics: Analysis of Variance; Animals; Arachidonic Acids; Dose-Response Relationship, Drug; Eating; Male; Ob | 2004 |
Effects of cannabinoid receptors on skeletal muscle oxidative pathways.
Topics: Adult; AMP-Activated Protein Kinases; Arachidonic Acids; Cells, Cultured; Dose-Response Relationship | 2007 |
Comparison of independent and combined chronic metabolic effects of GIP and CB1 receptor blockade in high-fat fed mice.
Topics: Animals; Appetite; Area Under Curve; Blood Glucose; Body Weight; Dietary Fats; Drug Evaluation, Prec | 2008 |
Reply to the letter to the editor "Long-term cannabinoid receptor (CB1) blockade in obesity: implications for the development of colorectal cancer".
Topics: Animals; Anti-Inflammatory Agents; Anti-Obesity Agents; Antineoplastic Agents; Carcinoma; Cell Survi | 2008 |