NESS06SM reduces body weight with an improved profile relative to SR141716A
Tài liệu tham khảo
Tchernof, 2013, Pathophysiology of human visceral obesity: an update, Physiological Reviews, 93, 359, 10.1152/physrev.00033.2011
Maccarrone, 2010, The endocannabinoid system and its relevance for nutrition, Annual Review of Nutrition, 30, 423, 10.1146/annurev.nutr.012809.104701
Silvestri, 2011, Peripheral effects of the endocannabinoid system in energy homeostasis: adipose tissue, liver and skeletal muscle, Reviews in Endocrine and Metabolic Disorders, 12, 153, 10.1007/s11154-011-9167-3
Miller, 2011, The highs and lows of cannabinoid receptor expression in disease: mechanisms and their therapeutic implications, Pharmacological Reviews, 63, 461, 10.1124/pr.110.003491
Solinas, 2008, The endocannabinoid system in brain reward processes, British Journal of Pharmacology, 154, 369, 10.1038/bjp.2008.130
Tseng, 2008, Journal of Medicinal Chemistry, 51, 5397, 10.1021/jm800066v
Lin, 2010, Biphasic suppression of appetite by cannabinoid CB1 receptor antagonists with distinct functional activities, Pharmacological Research, 62, 337, 10.1016/j.phrs.2010.06.001
Lee, 2008, Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity, Journal of Medicinal Chemistry, 51, 7216, 10.1021/jm800843r
Meye, 2012, Neutral antagonism at the cannabinoid 1 receptor: a safer treatment for obesity, Molecular Psychiatry, 10.1038/mp.2012.145
Mastinu, 2012, NESS038C6, a novel selective CB1 antagonist agent with anti-obesity activity and improved molecular profile, Behavioural Brain Research, 234, 192, 10.1016/j.bbr.2012.06.033
Christopoulou, 2011, An overview of the metabolic effects of rimonabant in randomized controlled trials: potential for other cannabinoid 1 receptor blockers in obesity, Clinical Pharmacology & Therapeutics, 36, 10
Zhang, 2012, Effects of chronic oral rimonabant administration on energy budgets of diet-induced obese C57BL/6 mice, Obesity, 20, 954, 10.1038/oby.2011.357
Després, 2005, Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia, The New England Journal of Medicine, 353, 2121, 10.1056/NEJMoa044537
Pi-Sunyer, 2006, Effect of rimonabant, a cannabinoid-1 receptor blocker, on weight and cardiometabolic risk factors in overweight or obese patients: RIO-North America: a randomized controlled trial, Journal of the American Medical Association, 295, 761, 10.1001/jama.295.7.761
Van Gaal, 2008, Long-term effect of CB1 blockade with rimonabant on cardiometabolic risk factors: two year results from the RIO-Europe Study, European Heart Journal, 29, 1761, 10.1093/eurheartj/ehn076
Christensen, 2007, Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials, Lancet, 370, 1706, 10.1016/S0140-6736(07)61721-8
Beyer, 2010, Depression-like phenotype following chronic CB1 receptor antagonism, Neurobiology of Disease, 39, 148, 10.1016/j.nbd.2010.03.020
Hill, 2009, The endocannabinoid system and the treatment of mood and anxiety disorders, CNS & Neurological Disorders – Drug Targets, 8, 451, 10.2174/187152709789824624
Esteban, 2012, Effects induced by cannabinoids on monoaminergic systems in the brain and their implications for psychiatric disorders, Progress in Neuro-Psychopharmacology & Biological Psychiatry, 38, 78, 10.1016/j.pnpbp.2011.11.007
Kirilly, 2012, CB1 receptor antagonists: new discoveries leading to new perspectives, Acta Physiologica, 205, 41, 10.1111/j.1748-1716.2011.02402.x
Bermudez-Silva, 2010, The endocannabinoid system, eating behavior and energy homeostasis: the end or a new beginning, Pharmacology Biochemistry and Behavior, 95, 375, 10.1016/j.pbb.2010.03.012
Wu, 2011, A new perspective of cannabinoid 1 receptor antagonists: approaches toward peripheral CB1R blockers without crossing the blood–brain barrier, Current Topics in Medicinal Chemistry, 11, 1421, 10.2174/156802611795860997
Ward, 2011, Rimonabant redux and strategies to improve the future outlook of CB1 receptor neutral-antagonist/inverse-agonist therapies, Obesity, 19, 1325, 10.1038/oby.2011.69
McLaughlin, 2012, Reports of the death of CB1 antagonists have been greatly exaggerated: recent preclinical findings predict improved safety in the treatment of obesity, Behavioural Pharmacology, 23, 537, 10.1097/FBP.0b013e3283566a8c
Silvestri, 2012, Second generation CB1 receptor blockers and other inhibitors of peripheral endocannabinoid overactivity and the rationale of their use against metabolic disorders, Expert Opinion on Investigational Drugs, 21, 1309, 10.1517/13543784.2012.704019
Tam, 2010, Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity, Journal of Clinical Investigation, 120, 2953, 10.1172/JCI42551
Receveur, 2010, Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood–brain-barrier, Bioorganic & Medicinal Chemistry Letters, 20, 453, 10.1016/j.bmcl.2009.12.003
Pavón, 2008, Central versus peripheral antagonism of cannabinoid CB1 receptor in obesity: effects of LH-21, a peripherally acting neutral cannabinoid receptor antagonist, in Zucker rats, Journal of Neuroendocrinology, 20, 116, 10.1111/j.1365-2826.2008.01693.x
Fulp, 2012, Design and synthesis of cannabinoid receptor 1 antagonists for peripheral selectivity, Journal of Medicinal Chemistry, 55, 2820, 10.1021/jm201731z
Stoit, 2002, Design, synthesis and biological activity of rigid cannabinoid CB1 receptor antagonists, Chemical and Pharmaceutical Bulletin, 50, 1109, 10.1248/cpb.50.1109
Zhang, 2008, Conformationally constrained analogues of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716): design, synthesis, computational analysis, and biological evaluations, Journal of Medicinal Chemistry, 51, 3526, 10.1021/jm8000778
Lazzari, 2012, Synthesis and pharmacological evaluation of novel 4-alkyl-5-thien-2′-yl pyrazole carboxamides, Central Nervous System Agents in Medicinal Chemistry, 12, 254, 10.2174/187152412803760636
Manca, 2013, Novel pyrazole derivatives as neutral CB1 antagonists with significant activity towards food intake, European Journal of Medicinal Chemistry, 62, 256, 10.1016/j.ejmech.2012.12.056
Murineddu, 2005, Tricyclic pyrazoles. 3. Synthesis, biological evaluation, and molecular modeling of analogues of the cannabinoid antagonist 8-chloro-1-(2′,4′-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7] cyclohepta[1,2-c]pyrazole-3-carboxamide, Journal of Medicinal Chemistry, 48, 7351, 10.1021/jm050317f
Murineddu, 2005, Tricyclic pyrazoles. Part 2: Synthesis and biological evaluation of novel 4,5-dihydro-1H-benzo[g]indazole-based ligands for cannabinoid receptors, Bioorganic & Medicinal Chemistry, 13, 3309, 10.1016/j.bmc.2005.02.032
Lazzari P, Ruiu S, Pinna GA, Murineddu G. Pharmaceutical compounds. Patent No: US 7,659,407, 2005.
Lazzari P, Loriga G, Manca I, Pinna GA, Pani L. Pharmaceutical compounds, US Patent Application No: 2010/0215741, 2010.
Lazzari P, Loriga G, Manca I, Pinna GA. Pharmaceutical compound, US Patent Application No: 2010/0,215,759, 2010.
Lazzari P, Ruiu S, Pinna GA, Murineddu G, Tricyclic pyrazole derivatives as cannabinoid receptor antagonists. European Patent No: EP 1,602,658, 2011.
Pertwee, 2005, Inverse agonism and neutral antagonism at cannabinoid CB1 receptors, Life Sciences, 76, 1307, 10.1016/j.lfs.2004.10.025
Pertwee, 2006, The pharmacology of cannabinoid receptors and their ligands: an overview, International Journal of Obesity, 30, S13, 10.1038/sj.ijo.0803272
Greig IR, Ross RA, Pertwee RG. US Patent Application No.: 20,100,022,611, 2010.
Clark, 2003, In silico prediction of blood–brain barrier permeation, Drug Discovery Today, 8, 927, 10.1016/S1359-6446(03)02827-7
Clark, 1999, Rapid calculation of polar molecular surface area and its application to the prediction of transport phenomena. 2. Prediction of blood–brain barrier penetration, Journal of Pharmaceutical Sciences, 88, 815, 10.1021/js980402t
Clark, 2000, Computational methods for the prediction of ‘drug-likeness’, Drug Discovery Today, 5, 49, 10.1016/S1359-6446(99)01451-8
Viswanadhan, 1989, Journal of Chemical Information and Modeling, 3, 163, 10.1021/ci00063a006
Ferrara, 2002, Evaluation of a fast implicit solvent model for molecular dynamics simulations, Proteins, 46, 24, 10.1002/prot.10001
Kloska, 2012, Synthetic genistein derivatives as modulators of glycosaminoglycan storage, Journal of Translational Medicine, 10, 153, 10.1186/1479-5876-10-153
Hung, 2010, Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophe n-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist, ChemMedChem, 5, 1439, 10.1002/cmdc.201000246
Lazzari, 2011, Weight loss induced by rimonabant is associated with an altered leptin expression and hypothalamic leptin signaling in diet-induced obese mice, Behavioural Brain Research, 217, 432, 10.1016/j.bbr.2010.11.022
Lazzari, 2012, Myrtanil substituent in 3 position of pyrazole ring determines CB1 agonism of novel 4,5-dihydrobenzo-oxa-cycloheptapyrazole cannabinoids, 3
Rosini, 2012, Diet-induced obesity: rodent model for the study of obesity-related disorders, Revista da Associação Médica Brasileira, 58, 383, 10.1016/S0104-4230(12)70211-7
Buettner, 2007, High-fat diets: modeling the metabolic disorders of human obesity in rodents, Obesity, 15, 798, 10.1038/oby.2007.608
Di Marzo, 2005, Endocannabinoid control of food intake and energy balance, Nature Neuroscience, 8, 585, 10.1038/nn1457
Wiley, 2005, CB1 cannabinoid receptor-mediated modulation of food intake in mice, British Journal of Pharmacology, 145, 293, 10.1038/sj.bjp.0706157
Bellocchio, 2010, Bimodal control of stimulated food intake by the endocannabinoid system, Nature Neuroscience, 13, 281, 10.1038/nn.2494
McDonald, 2011, Adverse metabolic effects of a hypercaloric, high-fat diet in rodents precede observable changes in body weight, Nutrition Research, 31, 707, 10.1016/j.nutres.2011.08.009
Van Proeyen, 2010, Training in the fasted state improves glucose tolerance during fat-rich diet, Journal of Physiology, 588, 4289, 10.1113/jphysiol.2010.196493
Rodríguez-Hernández, 2011, Decrease of aminotransferase levels in obese women is related to body weight reduction, irrespective of type of diet, Annals of Hepatology, 10, 486, 10.1016/S1665-2681(19)31517-0
Bellocchio, 2006, Cannabinoid receptors as therapeutic targets for obesity and metabolic diseases, Current Opinion in Pharmacology, 6, 586, 10.1016/j.coph.2006.09.001
Jourdan, 2012, Antagonism of peripheral hepatic cannabinoid receptor-1 improves liver lipid metabolism in mice: evidence from cultured explants, Hepatology, 55, 790, 10.1002/hep.24733
Nam, 2012, Blockade of cannabinoid receptor 1 improves insulin resistance, lipid metabolism, and diabetic nephropathy in db/db mice, Endocrinology, 153, 1387, 10.1210/en.2011-1423
Valentino, 2010, Central and peripheral molecular targets for antiobesity pharmacotherapy, Clinical Pharmacology & Therapeutics, 87, 652, 10.1038/clpt.2010.57
Rodgers, 2012, Anti-obesity drugs: past, present and future, Disease Models & Mechanisms, 5, 621, 10.1242/dmm.009621
Kim, 2011, Regulation of appetite to treat obesity, Expert Review of Clinical Pharmacology, 4, 243, 10.1586/ecp.11.3
Engeli, 2008, Dysregulation of the endocannabinoid system in obesity, Journal of Neuroendocrinology, 54, 2838
Engeli, 2012, Central and peripheral cannabinoid receptors as therapeutic targets in the control of food intake and body weight, Handbook of Experimental Pharmacology, 209, 357, 10.1007/978-3-642-24716-3_17
Jourdan, 2010, CB1 antagonism exerts specific molecular effects on visceral and subcutaneous fat and reverses liver steatosis in diet-induced obese mice, Diabetes, 59, 926, 10.2337/db09-1482
Vettor, 2009, The role of the endocannabinoid system in lipogenesis and fatty acid metabolism, Best Practice & Research: Clinical Endocrinology & Metabolism, 23, 51, 10.1016/j.beem.2008.10.002
Priego, 2008, Sex-differential expression of metabolism-related genes in response to a high-fat diet, Obesity, 16, 819, 10.1038/oby.2007.117
Boizard, 1998, Obesity-related overexpression of fatty-acid synthase gene in adipose tissue involves sterol regulatory element-binding protein transcription factors, Journal of Biological Chemistry, 273, 29164, 10.1074/jbc.273.44.29164
Zhao, 2010, Genome-wide expression profiling revealed peripheral effects of cannabinoid receptor 1 inverse agonists in improving insulin sensitivity and metabolic parameters, Molecular Pharmacology, 78, 350, 10.1124/mol.110.064980
Berger, 2002, The mechanisms of action of PPARs, Annual Review of Medicine, 26, 244
Berger, 2005, PPARs: therapeutic targets for metabolic disease, Trends in Pharmacological Sciences, 26, 244, 10.1016/j.tips.2005.03.003
Batra, 2012, The role of visceral fat, Digital Distribution, 30, 70
Klempel, 2011, Reliability of leptin, but not adiponectin, as a biomarker for diet-induced weight loss in humans, Nutrition Reviews, 69, 145, 10.1111/j.1753-4887.2011.00373.x
Mantzoros, 2011, Leptin in human physiology and pathophysiology, American Journal of Physiology – Endocrinology and Metabolism, 301, E567, 10.1152/ajpendo.00315.2011
Thundyil, 2012, Adiponectin receptor signalling in the brain, British Journal of Pharmacology, 165, 313, 10.1111/j.1476-5381.2011.01560.x
Kishida, 2011, Relationships between circulating adiponectin levels and fat distribution in obese subjects, Journal of Atherosclerosis and Thrombosis, 18, 592, 10.5551/jat.7625
Goldstein, 2004, Adiponectin A novel adipokine linking adipocytes and vascular function, Journal of Clinical Endocrinology & Metabolism, 89, 2563, 10.1210/jc.2004-0518
Scherer, 2011, Yin and Yang of hypothalamic insulin and leptin signaling in regulating white adipose tissue metabolism, Reviews in Endocrine and Metabolic Disorders, 12, 235, 10.1007/s11154-011-9190-4
Hochberg, 2010, Expanding the definition of hypothalamic obesity, Obesity Reviews, 11, 709, 10.1111/j.1467-789X.2010.00727.x
Cardinal, 2012, Hypothalamic CB1 cannabinoid receptors regulate energy balance in mice, Endocrinology, 153, 4136, 10.1210/en.2012-1405
Van Gaal, 2008, Efficacy and safety of rimonabant for improvement of multiple cardiometabolic risk factors in overweight/obese patients: pooled 1-year data from the Rimonabant in Obesity (RIO) program, Diabetes Care, 31, S229, 10.2337/dc08-s258
Nathan, 2011, Neuropsychiatric adverse effects of centrally acting antiobesity drugs, CNS Neuroscience & Therapeutics, 17, 490, 10.1111/j.1755-5949.2010.00172.x
Takahashi, 2008, Additive subthreshold dose effects of cannabinoid CB(1) receptor antagonist and selective serotonin reuptake inhibitor in antidepressant behavioral tests, European Journal of Pharmacology, 589, 149, 10.1016/j.ejphar.2008.05.020
Spiga, 2010, Altered architecture and functional consequences of the mesolimbic dopamine system in cannabis dependence, Addiction Biology, 15, 266, 10.1111/j.1369-1600.2010.00218.x
Spiga, 2011, Altered mesolimbic dopamine system in THC dependence, Current Neuropharmacology, 9, 200, 10.2174/157015911795017083
Umathe, 2011, Involvement of endocannabinoids in antidepressant and anti-compulsive effect of fluoxetine in mice, Behavioural Brain Research, 223, 125, 10.1016/j.bbr.2011.04.031
McLaughlin, 2013, Upregulation of CB(1) receptor binding in the ventromedial prefrontal cortex promotes proactive stress-coping strategies following chronic stress exposure, Behavioural Brain Research, 237, 333, 10.1016/j.bbr.2012.09.053
Dubreucq, 2012, Cannabinoid type 1 receptors located on single-minded 1-expressing neurons control emotional behaviors, Neuroscience, 204, 230, 10.1016/j.neuroscience.2011.08.049
Ganon-Elazar, 2012, Cannabinoids prevent the development of behavioral and endocrine alterations in a rat model of intense stress, Neuropsychopharmacology, 37, 456, 10.1038/npp.2011.204
Kristensen, 2011, SLC6 neurotransmitter transporters: structure, function, and regulation, Pharmacological Reviews, 63, 585, 10.1124/pr.108.000869
Zhao, 2009, Association of changes in norepinephrine and serotonin transporter expression with the long-term behavioral effects of antidepressant drugs, Neuropsychopharmacology, 34, 1467, 10.1038/npp.2008.183
Lee, 2010, The roles of BDNF in the pathophysiology of major depression and in antidepressant treatment, Psychiatry Investigation, 7, 231, 10.4306/pi.2010.7.4.231
Chourbaji, 2011, Altering BDNF expression by genetics and/or environment: impact for emotional and depression-like behaviour in laboratory mice, Neuroscience & Biobehavioral Reviews, 35, 599, 10.1016/j.neubiorev.2010.07.003
Willemen, 2012, Reasons for and time to discontinuation of rimonabant therapy: a modified prescription-event monitoring study, Drug Safety, 35, 1147, 10.1007/BF03262000
