PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 19862666-6 2010 Furthermore, anandamide inhibited basal release and stimulated release of adrenocortical steroids (corticosterone and aldosterone); this effect was reversed by CB1 antagonist (SR141716A). Rimonabant 176-185 cannabinoid receptor 1 Homo sapiens 160-163 20146701-3 2010 AIM: To study the influence of rimonabant, the endocannabinoid 1 (CB1) receptor antagonist, on gastric sensorimotor function in healthy controls. Rimonabant 31-41 cannabinoid receptor 1 Homo sapiens 66-69 19938110-10 2010 The blockage of the CB1-R by using its selective antagonist SR141716 (rimonabant) induced an opposite action on sperm survival supporting a role for this receptor in the biology of the male gamete. Rimonabant 60-68 cannabinoid receptor 1 Homo sapiens 20-25 20045337-1 2010 Numerous research groups have been engaged in searching for novel CB1 receptor antagonists, since SR141716A (rimonabant), a CB1 receptor antagonist, proved to be efficacious in human for the treatment of obesity. Rimonabant 98-107 cannabinoid receptor 1 Homo sapiens 66-69 20045337-1 2010 Numerous research groups have been engaged in searching for novel CB1 receptor antagonists, since SR141716A (rimonabant), a CB1 receptor antagonist, proved to be efficacious in human for the treatment of obesity. Rimonabant 98-107 cannabinoid receptor 1 Homo sapiens 124-127 24973151-2 2009 Rimonabant, a cannabinoid receptor (CB1) antagonist, is an anti-obesity agent and decreases risk for metabolic syndrome. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 36-39 21050934-1 2010 Rimonabant (acomplia) is a 1,5-diarylpyrazole derivative that acts as a type 1 cannabinoid receptor (CB1) inverse agonist. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 101-104 19956878-0 2010 Synergistic inhibition of human colon cancer cell growth by the cannabinoid CB1 receptor antagonist rimonabant and oxaliplatin. Rimonabant 100-110 cannabinoid receptor 1 Homo sapiens 76-79 19236442-8 2009 Rimonabant, the first endocannabinoid CB1 antagonist, is associated with weight reduction and it improves diabetic parameters; nevertheless, it is associated with psychiatric disorders; indeed, a recently conducted safety review led to the temporal suspension of its commercialization. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 38-41 19690173-5 2009 Interestingly, only the effect of AEA on BiP was reversed by the CB1R antagonist SR141716, in SH-SY5Y cells as well as in human neuroblastoma LAN-5 cells (that express a functional CB1R) but not in SK-NBE cells (which do not express CB1R). Rimonabant 81-89 cannabinoid receptor 1 Homo sapiens 65-69 19575185-1 2009 RATIONALE: The cannabinoid CB1 selective antagonist SR141716A (Rimonabant) has been shown to decrease body weight in laboratory animals and humans. Rimonabant 52-61 cannabinoid receptor 1 Homo sapiens 27-30 19492411-5 2009 The blockage of CB1-R by the specific antagonist SR141716 increased both capacitation and sperm motility suggesting an involvement of the CB1-R in the acquisition of sperm fertilizing activity. Rimonabant 49-57 cannabinoid receptor 1 Homo sapiens 16-21 19492411-5 2009 The blockage of CB1-R by the specific antagonist SR141716 increased both capacitation and sperm motility suggesting an involvement of the CB1-R in the acquisition of sperm fertilizing activity. Rimonabant 49-57 cannabinoid receptor 1 Homo sapiens 138-143 19479993-1 2009 The selective CB1 receptor antagonist rimonabant (SR141716) was shown to perform a number of biological effects in several pathological conditions. Rimonabant 38-48 cannabinoid receptor 1 Homo sapiens 14-17 19479993-1 2009 The selective CB1 receptor antagonist rimonabant (SR141716) was shown to perform a number of biological effects in several pathological conditions. Rimonabant 50-58 cannabinoid receptor 1 Homo sapiens 14-17 19337726-0 2009 Acute administration of the cannabinoid CB1 antagonist rimonabant impairs positive affective memory in healthy volunteers. Rimonabant 55-65 cannabinoid receptor 1 Homo sapiens 40-43 19609004-5 2009 The effects were attenuated using SR141716A, which has high affinity to cannabinoid receptor 1 (CB1). Rimonabant 34-43 cannabinoid receptor 1 Homo sapiens 72-94 19609004-5 2009 The effects were attenuated using SR141716A, which has high affinity to cannabinoid receptor 1 (CB1). Rimonabant 34-43 cannabinoid receptor 1 Homo sapiens 96-99 20641388-12 2004 (-)-3-(4-chlorophenyl)-N"-[(4-[(11)C]cyanophenyl)sulfonyl]-4-phenyl- 4,5-dihydro-1H-pyrazole-1-carboxamidine ([(11)C]CB1-(-)-12a) is a potent and selective CB1 antagonist with nanomolar affinity and lower lipophilicity than SR141716A (9). Rimonabant 224-233 cannabinoid receptor 1 Homo sapiens 117-120 19328001-1 2009 A myriad of research groups have been engaged in searching for novel CB1 receptor antagonists, since SR141716A (rimonabant), a CB1 receptor antagonist, was discovered for an obesity treatment. Rimonabant 101-110 cannabinoid receptor 1 Homo sapiens 69-72 19328001-1 2009 A myriad of research groups have been engaged in searching for novel CB1 receptor antagonists, since SR141716A (rimonabant), a CB1 receptor antagonist, was discovered for an obesity treatment. Rimonabant 101-110 cannabinoid receptor 1 Homo sapiens 127-130 19249987-6 2009 One CB1 receptor antagonist/inverse agonist, rimonabant, has emerged as the first-in-class drug approved outside the United States for weight control. Rimonabant 45-55 cannabinoid receptor 1 Homo sapiens 4-7 19285260-6 2009 All these effects are blocked by the CB1 antagonist rimonabant, suggesting that the weight-reducing effect of CB1 blockade is due not only to the transient suppression of food intake and reduction of lipogenesis but also to an increased mitochondrial biogenesis and oxidative metabolism which counteracts the inhibitory effects of ECs, levels of which are increased in fat tissues of obese rodents and humans. Rimonabant 52-62 cannabinoid receptor 1 Homo sapiens 37-40 19285260-6 2009 All these effects are blocked by the CB1 antagonist rimonabant, suggesting that the weight-reducing effect of CB1 blockade is due not only to the transient suppression of food intake and reduction of lipogenesis but also to an increased mitochondrial biogenesis and oxidative metabolism which counteracts the inhibitory effects of ECs, levels of which are increased in fat tissues of obese rodents and humans. Rimonabant 52-62 cannabinoid receptor 1 Homo sapiens 110-113 18511157-1 2009 Cyano analogs of Rimonabant with high binding affinity for the cerebral cannabinoid receptor (CB1) and with optimized lipophilicity have been synthesized as potential positron emission tomography (PET) ligands. Rimonabant 17-27 cannabinoid receptor 1 Homo sapiens 94-97 19578688-2 2009 Thus, the objective of the present review is to discuss the potential psychiatric side-effects of CB1 receptor antagonists, such as rimonabant, which has been recently marketed in several countries for the treatment of smoking cessation, obesity and associated metabolic disorders. Rimonabant 132-142 cannabinoid receptor 1 Homo sapiens 98-101 20641388-12 2004 (-)-3-(4-chlorophenyl)-N"-[(4-[(11)C]cyanophenyl)sulfonyl]-4-phenyl- 4,5-dihydro-1H-pyrazole-1-carboxamidine ([(11)C]CB1-(-)-12a) is a potent and selective CB1 antagonist with nanomolar affinity and lower lipophilicity than SR141716A (9). Rimonabant 224-233 cannabinoid receptor 1 Homo sapiens 156-159 19022666-1 2009 Since the CB1 receptor antagonist SR141716 (rimonabant) was reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target in the treatment of obesity. Rimonabant 34-42 cannabinoid receptor 1 Homo sapiens 10-13 19022666-1 2009 Since the CB1 receptor antagonist SR141716 (rimonabant) was reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target in the treatment of obesity. Rimonabant 34-42 cannabinoid receptor 1 Homo sapiens 94-97 18580872-7 2009 Systemic administration of a CB1 antagonist, rimonabant (SR141716), also potently inhibited extinction learning. Rimonabant 45-55 cannabinoid receptor 1 Homo sapiens 29-32 19689362-6 2009 In this review, we summarize advances that have been made and the status of studies of a diverse array of CB(1)R antagonists that have been identified mainly based on modifications of the first-in-class CB(1)R antagonist, rimonabant. Rimonabant 222-232 cannabinoid receptor 1 Homo sapiens 106-112 19333392-3 2009 This paper tested the hypothesis that bias affects review articles regarding rimonabant, an anti-obesity drug that blocks the central cannabinoid receptor. Rimonabant 77-87 cannabinoid receptor 1 Homo sapiens 126-154 18580872-7 2009 Systemic administration of a CB1 antagonist, rimonabant (SR141716), also potently inhibited extinction learning. Rimonabant 57-65 cannabinoid receptor 1 Homo sapiens 29-32 18954042-1 2008 Since the CB1 cannabinoid receptor antagonist 1 (SR141716, rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. Rimonabant 49-57 cannabinoid receptor 1 Homo sapiens 10-13 18954042-1 2008 Since the CB1 cannabinoid receptor antagonist 1 (SR141716, rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. Rimonabant 49-57 cannabinoid receptor 1 Homo sapiens 120-123 18796007-10 2008 The CB1R antagonist SR 141716A reverses ethanol-induced depression of mEPSC frequency. Rimonabant 20-30 cannabinoid receptor 1 Homo sapiens 4-8 18377702-6 2008 AM-404 (10 mg/kg) attenuated this action of cocaine, an effect which was reversed by pretreatment with the selective CB1R antagonist SR141716A. Rimonabant 133-142 cannabinoid receptor 1 Homo sapiens 117-121 18991793-7 2008 In July 2006, European regulatory authorities approved the use of rimonabant, SR141716, a selective CB1 receptor antagonist, in obese patients (BMI > or =30kg/m(2), or >27kg/m(2) with complications). Rimonabant 78-86 cannabinoid receptor 1 Homo sapiens 100-103 18654765-1 2008 Rimonabant is an inverse agonist specific for cannabinoid receptors and selective for their cannabinoid-1 (CB(1)) subtype. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 92-112 18957525-3 2008 Here, we report that the CB 1 receptor antagonist rimonabant disrupts extinction learning in an aversive, but not in an appetitive, Barnes maze conditioning task. Rimonabant 50-60 cannabinoid receptor 1 Homo sapiens 25-29 18539938-6 2008 The AEA-induced enhancement of outflow facility was blocked by SR141716A, a CB1 antagonist, and was partially blocked by SR144528, a CB2 antagonist. Rimonabant 63-72 cannabinoid receptor 1 Homo sapiens 76-79 18607180-2 2008 Rimonabant, an inverse agonist of the CB1 receptor is being used therapeutically. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 38-41 18397936-7 2008 We anticipate that, in addition to the approval in several countries of the CB(1) antagonist, rimonabant, for the treatment of obesity and associated metabolic dysfunctions, other cannabinoid modulators are likely to have an impact on human disease in the future, including hepatic fibrosis and neoplasia. Rimonabant 94-104 cannabinoid receptor 1 Homo sapiens 76-81 18597752-8 2008 The 2-AG-induced enhancement of outflow was blocked by SR141716A, a CB1 antagonist, and SR144528, a CB2 antagonist. Rimonabant 55-64 cannabinoid receptor 1 Homo sapiens 68-71 18480689-0 2008 Cannabinoid receptor 1 blocker rimonabant (SR 141716) for treatment of alcohol dependence: results from a placebo-controlled, double-blind trial. Rimonabant 31-41 cannabinoid receptor 1 Homo sapiens 0-22 18454166-1 2008 The synthetic cannabinoid CB1 receptor antagonist rimonabant (sold in the United Kingdom under the brand name Acomplia) was reported to improve the profile of cardiovascular risk factors in obese patients with the metabolic syndrome, a cluster of metabolic disorders that often precedes the onset of type II diabetes. Rimonabant 50-60 cannabinoid receptor 1 Homo sapiens 26-29 18551116-3 2008 We examined effects of the natural CB1 agonist, 2-Arachidonoylglycerol (2-AG), and the synthetic CB1 antagonist, SR141716, on insulin action in cultured adipocytes. Rimonabant 113-121 cannabinoid receptor 1 Homo sapiens 97-100 18480689-3 2008 This was a 12-week double-blind, placebo-controlled, proof-of-concept study to assess the possible efficacy of the cannabinoid receptor 1 antagonist rimonabant 20 mg/d (2 x 10 mg) in the prevention of relapse to alcohol in recently detoxified alcohol-dependent patients. Rimonabant 149-159 cannabinoid receptor 1 Homo sapiens 115-137 18076956-1 2008 The CB1 inverse agonist/antagonist SR141716A recently has been introduced for the management of obesity (rimonabant; Acomplia) and appears to have beneficial effects. Rimonabant 35-44 cannabinoid receptor 1 Homo sapiens 4-7 18669206-9 2008 Rimonabant, a CB1 antagonist, has been recently launched for the treatment of obese or overweight patients at high cardiometabolic risk. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 14-17 18319252-2 2008 Occupancy by the agonist DAMGO (Tyr-d-Ala-Gly-N-methyl-Phe-Gly-ol) resulted in phosphorylation of the ERK1/2 MAP kinases, which was blocked by the opioid antagonist naloxone but not the cannabinoid CB1 receptor inverse agonist SR141716A. Rimonabant 227-236 cannabinoid receptor 1 Homo sapiens 198-201 18243711-1 2008 After the CB1 receptor antagonist SR141716 (rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. Rimonabant 34-42 cannabinoid receptor 1 Homo sapiens 10-13 18076956-4 2008 Thus far, data comparing SR141716A and AM4113 across several species indicate that both drugs produce dose-related direct effects on operant behavior within the same range of doses that serve to antagonize the behavioral and hypothermic effects of a CB1 agonist. Rimonabant 25-34 cannabinoid receptor 1 Homo sapiens 250-253 18155257-9 2008 Emerging preclinical data suggest that CB1 receptor neutral antagonists may represent breakthrough medications superior to antagonists/inverse agonists such as rimonabant for therapeutic attenuation of CB1 receptor transmission. Rimonabant 160-170 cannabinoid receptor 1 Homo sapiens 202-205 18157162-1 2008 BACKGROUND AND PURPOSE: Rimonabant (SR141716) is the first selective cannabinoid receptor CB(1) antagonist described. Rimonabant 36-44 cannabinoid receptor 1 Homo sapiens 90-95 23687711-6 2008 Rimonabant, a selective cannabinoid-1 receptor (CB1) blocker, has been shown to reduce smoking, body weight and improve and improves the profile of several metabolic risk factors in high-risk patients. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 24-46 21221184-3 2008 AIMS: To review the evidence on rimonabant, a novel CB1 receptor antagonist, for the treatment of obese and overweight patients. Rimonabant 32-42 cannabinoid receptor 1 Homo sapiens 52-55 18042663-8 2008 The enhanced PGE(2) production caused by CP55,940 was abrogated by cotreatment with either SR141716A or NS398, illustrating that the cannabinoid action on prostaglandin production in fetal membranes is mediated by CB1 agonism and COX-2. Rimonabant 91-100 cannabinoid receptor 1 Homo sapiens 214-217 23687711-6 2008 Rimonabant, a selective cannabinoid-1 receptor (CB1) blocker, has been shown to reduce smoking, body weight and improve and improves the profile of several metabolic risk factors in high-risk patients. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 48-51 18563799-1 2008 The observed antiobesity effect of rimonabant (1) in a pharmacological rodent model 10 years ago has led to a surge in the search for novel cannabinoid CB1 antagonists as a new therapeutic target for the treatment of obesity. Rimonabant 35-45 cannabinoid receptor 1 Homo sapiens 152-155 18416822-13 2008 Cannabinoid receptor stimulation of fibroblast-like cells from OA and RA patients produced a time-dependent phosphorylation of extracellular signal-regulated kinase (ERK)-1 and ERK-2 which was significantly blocked by the CB1 antagonist SR141716A. Rimonabant 237-246 cannabinoid receptor 1 Homo sapiens 222-225 17686497-6 2008 The THC-mediated increase in DARPP-32 phosphorylation is reduced by administration of the CB1 receptor antagonist, SR141716A (3mg/kg). Rimonabant 115-124 cannabinoid receptor 1 Homo sapiens 90-93 19300605-3 2007 Preclinical and clinical studies suggest that the endocannabinoid system can be manipulated by the CB1 receptor antagonist SR141716A, that might constitute a new generation of compounds for treating addiction across different classes of abused drugs. Rimonabant 123-132 cannabinoid receptor 1 Homo sapiens 99-102 18303686-1 2008 Rimonabant (Acomplia): first CB1 receptor antagonist of the endocannabinoid system]. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 29-32 17666847-3 2007 These analogs bearing a piperidinyl carboxamide at the C(3) of the pyrazole ring exhibited affinities comparable to those of the CB1 reference antagonist SR141716, which warrants further investigation using the radiolabeled form for biological imaging studies. Rimonabant 154-162 cannabinoid receptor 1 Homo sapiens 129-132 17971763-5 2007 Rimonabant is an endocannabinoid CB1 receptor antagonist which induces a 4-5 kg mean weight loss and improves glycemic and lipid profiles, but it induces anxiety and depressive disorders. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 33-36 17720358-3 2007 Rimonabant, a cannabinoid-1 (CB1) receptor blocker, has been shown to induce weight loss and improve cardiometabolic parameters, implying that the endocannabinoid system is a promising target for obesity-related health improvement. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 29-32 17409233-9 2007 Local infusion of the CB1 antagonist SR 141716A into the NAc significantly reduced ethanol, but not cocaine, self-administration. Rimonabant 37-47 cannabinoid receptor 1 Homo sapiens 22-25 29788669-8 2007 Rimonabant, a selective CB1 blocker, reduces food intake and body weight in animals and humans. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 24-27 17667865-9 2007 In addition, results from the RIO-Lipids study, which was conducted in high-risk obese, dyslipidemic patients, have provided evidence that CB1 receptor blockade with rimonabant can induce significant weight loss, and, more importantly, improve the cardiometabolic risk profile beyond what could be explained by the weight loss effects of the drug. Rimonabant 166-176 cannabinoid receptor 1 Homo sapiens 139-142 17327463-2 2007 The advent of the highly selective cannabinoid receptor (CB1) antagonist, rimonabant (SR141716; Acomplia) can revolutionize the ability of the clinicians to manage obesity. Rimonabant 74-84 cannabinoid receptor 1 Homo sapiens 57-60 17327463-2 2007 The advent of the highly selective cannabinoid receptor (CB1) antagonist, rimonabant (SR141716; Acomplia) can revolutionize the ability of the clinicians to manage obesity. Rimonabant 86-94 cannabinoid receptor 1 Homo sapiens 57-60 17961655-1 2007 The endocannabinoid system associates the cannabinoid receptors (CB1 and CB2), largely expressed in the central nervous system as well as in the peripheric one, the endocannabinoids (the two main ones being anandamine and the 2 arachidonoyl glycerol), the endocannabinoid-degrading enzymes, and the synthetic antagonists of the CB1 receptor, such as SR141716 (rimonabant). Rimonabant 350-358 cannabinoid receptor 1 Homo sapiens 65-68 17784530-6 2007 Rimonabant is the first cannabinoid receptor 1 antagonist to be marketed in Europe and the first to file an New Drug Application in the United States. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 24-46 17110038-6 2007 Application of the CB1 receptor antagonists SR141716A (1 microM) or AM251 (1 microM) to "epileptic" neurons caused the development of continuous epileptiform activity, resembling electrographic status epilepticus. Rimonabant 44-53 cannabinoid receptor 1 Homo sapiens 19-22 17322160-13 2007 CONCLUSION: Rimonabant, a selective CB(1) antagonist, is a novel treatment option for obese and overweight individuals. Rimonabant 12-22 cannabinoid receptor 1 Homo sapiens 36-41 17948363-10 2007 Clinical trials with rimonabant, a CB1 receptor antagonist, have demonstrated significant weight loss as well as increased HDL-C levels and reduced triglyceride levels. Rimonabant 21-31 cannabinoid receptor 1 Homo sapiens 35-38 21977272-3 2007 Recent studies with the CB1 receptor antagonist rimonabant have demonstrated favorable effects such as a reduction in body weight and waist circumference and an improvement in metabolic factors (cholesterol, triglycerides, glycemia etc). Rimonabant 48-58 cannabinoid receptor 1 Homo sapiens 24-27 17580728-3 2007 Rimonabant is the first cannabinoid receptor (CB-1) antagonist being studied and utilized to treat obesity (it is approved in Europe but is currently under review in the United States). Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 46-50 17109677-1 2006 Rimonabant is the first drug to target the endocannabinoid (CB) pathway by inhibiting the actions of anandamide and 2-archidonyl-glycerol on CB1 receptors. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 141-144 16697306-1 2006 Rimonabant is a first selective blocker of the cannabinoid receptor type 1 (CB1) being developed for the treatment of multiple cardiometabolic risk factors, including abdominal obesity and smoking. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 76-79 16822929-0 2006 The cannabinoid CB1 receptor antagonist rimonabant (SR141716) inhibits human breast cancer cell proliferation through a lipid raft-mediated mechanism. Rimonabant 52-60 cannabinoid receptor 1 Homo sapiens 16-19 16822929-2 2006 In this study, we show that cannabinoid receptor type 1 (CB1) antagonist Rimonabant (SR141716) inhibited human breast cancer cell proliferation, being more effective in highly invasive metastatic MDA-MB-231 cells than in less-invasive T47D and MCF-7 cells. Rimonabant 73-83 cannabinoid receptor 1 Homo sapiens 28-60 16822929-2 2006 In this study, we show that cannabinoid receptor type 1 (CB1) antagonist Rimonabant (SR141716) inhibited human breast cancer cell proliferation, being more effective in highly invasive metastatic MDA-MB-231 cells than in less-invasive T47D and MCF-7 cells. Rimonabant 85-93 cannabinoid receptor 1 Homo sapiens 28-60 16822929-7 2006 Indeed, we found that CB1 receptor (CB1R) is completely displaced from lipid rafts in SR141716-treated MDA-MB-231 cells, and cholesterol depletion by methyl-beta-cyclodextrin strongly prevented SR141716-mediated antiproliferative effect. Rimonabant 86-94 cannabinoid receptor 1 Homo sapiens 22-34 16822929-7 2006 Indeed, we found that CB1 receptor (CB1R) is completely displaced from lipid rafts in SR141716-treated MDA-MB-231 cells, and cholesterol depletion by methyl-beta-cyclodextrin strongly prevented SR141716-mediated antiproliferative effect. Rimonabant 86-94 cannabinoid receptor 1 Homo sapiens 36-40 16822929-7 2006 Indeed, we found that CB1 receptor (CB1R) is completely displaced from lipid rafts in SR141716-treated MDA-MB-231 cells, and cholesterol depletion by methyl-beta-cyclodextrin strongly prevented SR141716-mediated antiproliferative effect. Rimonabant 194-202 cannabinoid receptor 1 Homo sapiens 22-34 16822929-7 2006 Indeed, we found that CB1 receptor (CB1R) is completely displaced from lipid rafts in SR141716-treated MDA-MB-231 cells, and cholesterol depletion by methyl-beta-cyclodextrin strongly prevented SR141716-mediated antiproliferative effect. Rimonabant 194-202 cannabinoid receptor 1 Homo sapiens 36-40 16822929-8 2006 Taken together, our results suggest that SR141716 inhibits human breast cancer cell growth via a CB1R lipid raft/caveolae-mediated mechanism. Rimonabant 41-49 cannabinoid receptor 1 Homo sapiens 97-101 16533866-9 2006 These data suggest that cannabinoid CB1 antagonists such as SR141716A may have limited antipsychotic potential in man as to positive symptoms. Rimonabant 60-69 cannabinoid receptor 1 Homo sapiens 36-39 16715087-7 2006 Treatment with the CB1 receptor antagonist SR141716A decreased the wound-healing response to acute liver injury and inhibited progression of fibrosis in three models of chronic liver injury. Rimonabant 43-52 cannabinoid receptor 1 Homo sapiens 19-22 17233530-0 2006 Conformational characteristics of the interaction of SR141716A with the CB1 cannabinoid receptor as determined through the use of conformationally constrained analogs. Rimonabant 53-62 cannabinoid receptor 1 Homo sapiens 72-75 16423891-7 2006 SR141716, a selective antagonist of the cannabinoid CB1 receptor, had no intrinsic activity in control preparations but potentiated the neural twitch in diseased tissues by up to 196% in a concentration dependent manner. Rimonabant 0-8 cannabinoid receptor 1 Homo sapiens 52-55 16609959-6 2006 These effects were completely reverted when cells were exposed to the synthetic cannabinoid in the presence of the specific CB1-receptor antagonist, SR141716A (1 microM). Rimonabant 149-158 cannabinoid receptor 1 Homo sapiens 124-127 16639008-7 2006 The effect of 30 nM of noladin ether was completely blocked by SR141716A, a selective CB1 antagonist. Rimonabant 63-72 cannabinoid receptor 1 Homo sapiens 86-89 16767305-7 2006 Rimonabant is a specific antagonist to the main endocannabinoid receptor (CB1). Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 74-77 16378681-10 2006 Microinjection of the CB1 antagonist/inverse agonist rimonabant (SR141716A) into the BLA, a limbic forebrain region with high densities of CB1 receptors, suppressed SIA relative to control conditions. Rimonabant 53-63 cannabinoid receptor 1 Homo sapiens 22-25 16378681-10 2006 Microinjection of the CB1 antagonist/inverse agonist rimonabant (SR141716A) into the BLA, a limbic forebrain region with high densities of CB1 receptors, suppressed SIA relative to control conditions. Rimonabant 53-63 cannabinoid receptor 1 Homo sapiens 139-142 16378681-10 2006 Microinjection of the CB1 antagonist/inverse agonist rimonabant (SR141716A) into the BLA, a limbic forebrain region with high densities of CB1 receptors, suppressed SIA relative to control conditions. Rimonabant 65-74 cannabinoid receptor 1 Homo sapiens 22-25 16378681-10 2006 Microinjection of the CB1 antagonist/inverse agonist rimonabant (SR141716A) into the BLA, a limbic forebrain region with high densities of CB1 receptors, suppressed SIA relative to control conditions. Rimonabant 65-74 cannabinoid receptor 1 Homo sapiens 139-142 16617296-8 2006 CB1 antagonist SR141716A antagonized noladin ether-induced inhibition of migration of TM cells. Rimonabant 15-24 cannabinoid receptor 1 Homo sapiens 0-3 17208664-6 2006 Although many questions remain unanswered at present, the emerging concept of endocannabinoids as metabolic regulators helps to explain the success of rimonabant (SR141716), an antagonist of (CB(1)) receptors, currently in Phase III studies. Rimonabant 151-161 cannabinoid receptor 1 Homo sapiens 192-197 16570099-8 2006 Antagonists include the CB1-selective SR141716A, AM251, AM281 and LY320135, and the CB2-selective SR144528 and AM630. Rimonabant 38-47 cannabinoid receptor 1 Homo sapiens 24-27 17208664-6 2006 Although many questions remain unanswered at present, the emerging concept of endocannabinoids as metabolic regulators helps to explain the success of rimonabant (SR141716), an antagonist of (CB(1)) receptors, currently in Phase III studies. Rimonabant 163-171 cannabinoid receptor 1 Homo sapiens 192-197 16503875-4 2005 Recent studies with rimonabant, a cannabinoid type 1 receptor (CB(1)) antagonist, demonstrate clinically significant weight loss as well as reduction in metabolic syndromme burden in obese patients. Rimonabant 20-30 cannabinoid receptor 1 Homo sapiens 34-68 16337199-3 2005 Interestingly, equipotent doses of the CB1 antagonist SR141716A and the CB1/CB2 agonist anandamide inflicted additive negative effects on viability. Rimonabant 54-63 cannabinoid receptor 1 Homo sapiens 39-42 17017918-1 2006 Rimonabant (SR141716, Acomplia) has been described as an antagonist/inverse agonist at the cannabinoid receptor type 1 (CB1). Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 91-124 17017918-1 2006 Rimonabant (SR141716, Acomplia) has been described as an antagonist/inverse agonist at the cannabinoid receptor type 1 (CB1). Rimonabant 12-20 cannabinoid receptor 1 Homo sapiens 91-124 17017918-7 2006 Recently, it has been shown that rimonabant prevents indomethacin-induced intestinal injury by decreasing the levels of pro-inflammatory cytokine tumour necrosis factor alpha (TNFalpha), thus indicating that CB1 receptor antagonists might exhibit potential anti-inflammatory activity in acute and chronic diseases. Rimonabant 33-43 cannabinoid receptor 1 Homo sapiens 208-211 17112304-1 2006 Rimonabant is the first of a new class of selective cannabinoid receptor-1 blockers. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 52-74 16291982-1 2005 BACKGROUND: Rimonabant, a selective cannabinoid-1 receptor (CB1) blocker, has been shown to reduce body weight and improve cardiovascular risk factors in obese patients. Rimonabant 12-22 cannabinoid receptor 1 Homo sapiens 36-58 16291982-1 2005 BACKGROUND: Rimonabant, a selective cannabinoid-1 receptor (CB1) blocker, has been shown to reduce body weight and improve cardiovascular risk factors in obese patients. Rimonabant 12-22 cannabinoid receptor 1 Homo sapiens 60-63 16269998-11 2005 One of the new drugs under evaluation is rimonabant, the first representatives of a new class of drugs, selective CB1 endocannabinoid receptor antagonists. Rimonabant 41-51 cannabinoid receptor 1 Homo sapiens 114-117 15904723-1 2005 The present study shows that the selective cannabinoid CB1 receptor antagonist SR141716A attenuated responding for both nicotine- and sucrose-associated stimuli in a long-term extinction-reinstatement model. Rimonabant 79-88 cannabinoid receptor 1 Homo sapiens 55-58 16148442-2 2005 In laboratory animals, cannabinoid CB1 receptor antagonism decreases motivation for palatable foods, and most recently, the CB1 receptor antagonist SR141716A, or rimonabant (Acomplia), was reported to produce weight loss in obese human subjects. Rimonabant 148-157 cannabinoid receptor 1 Homo sapiens 124-127 15894565-4 2005 In MPTP-lesioned marmosets previously treated with levodopa to establish LID, attenuation of CB1 signaling by systemic administration of rimonabant (1 and 3 mg/kg) had anti-parkinsonian actions, equivalent to a 71% increase in motor activity at 3 mg/kg. Rimonabant 137-147 cannabinoid receptor 1 Homo sapiens 93-96 15390091-9 2005 The CB1 and CB2 receptor-specific antagonists SR141716A and SR144528, respectively, partially blocked this suppressive effect. Rimonabant 46-55 cannabinoid receptor 1 Homo sapiens 4-7 15910885-5 2005 Both effects were blocked by the CB1 receptor antagonist SR141716A. Rimonabant 57-66 cannabinoid receptor 1 Homo sapiens 33-36 15836887-2 2005 We assessed the effect of rimonabant, a selective CB1 blocker, on bodyweight and cardiovascular risk factors in overweight or obese patients. Rimonabant 26-36 cannabinoid receptor 1 Homo sapiens 50-53 15836887-10 2005 INTERPRETATION: CB1 blockade with rimonabant 20 mg, combined with a hypocaloric diet over 1 year, promoted significant decrease of bodyweight and waist circumference, and improvement in cardiovascular risk factors. Rimonabant 34-44 cannabinoid receptor 1 Homo sapiens 16-19 15755787-0 2005 Rimonabant--a selective CB1 antagonist. Rimonabant 0-11 cannabinoid receptor 1 Homo sapiens 24-27 15562018-7 2005 The specificity of anandamide effects in human sperm were confirmed by the effects of the CB(1)-R antagonist SR141716. Rimonabant 109-117 cannabinoid receptor 1 Homo sapiens 90-97 15381634-0 2004 The cannabinoid CB1 receptor antagonist SR141716 blocks the orexigenic effects of intrahypothalamic ghrelin. Rimonabant 40-48 cannabinoid receptor 1 Homo sapiens 16-19 15807291-6 2005 Rimonabant is a selective blocker of cannabinoid-1 (CB1) receptors and participates in the regulation of impaired endocannabinoid system. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 37-50 15807291-6 2005 Rimonabant is a selective blocker of cannabinoid-1 (CB1) receptors and participates in the regulation of impaired endocannabinoid system. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 52-55 16596770-7 2005 Cannabinoid receptor antagonists include the CB1-selective SR141716A, AM251, AM281 and LY320135, and the CB2-selective SR144528 and AM630. Rimonabant 59-68 cannabinoid receptor 1 Homo sapiens 45-48 15548432-6 2004 The selective TRPV1 receptor antagonist (capsazepine), CB1 receptor antagonist (SR141716A) and CB2 receptor antagonist (SR144528) inhibited these responses. Rimonabant 80-89 cannabinoid receptor 1 Homo sapiens 55-58 15613777-3 2004 Examinations using [3H]CP-55940 or [3H]SR141716A revealed that the density of CB1 receptors, a central type of cannabinoid receptor, is increased in subregions of the prefrontal cortex in schizophrenia. Rimonabant 39-48 cannabinoid receptor 1 Homo sapiens 78-81 15525787-8 2004 Limited food-related reductions in the activity of NCM neurons were reversed by the cannabinoid antagonist SR141716A (N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide), implicating CB1 cannabinoid receptor involvement. Rimonabant 107-116 cannabinoid receptor 1 Homo sapiens 218-221 14980654-0 2004 Potent imidazole and triazole CB1 receptor antagonists related to SR141716. Rimonabant 66-74 cannabinoid receptor 1 Homo sapiens 30-33 15134279-8 2004 The CB1 receptor antagonist, rimonabant (SR-141716), discovered by Sanofi-Synthelabo, is in phase III clinical trials for the treatment of obesity and has been found to decrease appetite and body weight in humans. Rimonabant 29-39 cannabinoid receptor 1 Homo sapiens 4-7 15134279-8 2004 The CB1 receptor antagonist, rimonabant (SR-141716), discovered by Sanofi-Synthelabo, is in phase III clinical trials for the treatment of obesity and has been found to decrease appetite and body weight in humans. Rimonabant 41-50 cannabinoid receptor 1 Homo sapiens 4-7 15338959-2 2004 Novel chemical entities having CB1 antagonistic properties have recently been disclosed by several pharmaceutical companies and some academic research groups, some of which are close structural analogs of the leading compound rimonabant (SR-141716A; Sanofi-Synthelabo). Rimonabant 226-236 cannabinoid receptor 1 Homo sapiens 31-34 14707029-14 2004 ODA (10 microm)-stimulated [(35)S]GTPgammaS binding was reversed by the selective CB(1) antagonist SR141716A (IC(50)=2.11 nm (0.32-13.77 nm), R(2)=1.00, n=6). Rimonabant 99-108 cannabinoid receptor 1 Homo sapiens 82-87 14617682-5 2004 By contrast, the CB1 cannabinoid receptor antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboximide hydrochloride (SR141716; SR1), capsazepine (vanilloid receptor antagonist), the inhibitors of ceramide generation, or pertussis toxin did not counteract CBD effects. Rimonabant 164-172 cannabinoid receptor 1 Homo sapiens 17-20 14978245-4 2004 Agonist-mediated Ca2+ current inhibition was blocked by a selective CB1R antagonist [SR141716A, N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboximide hydrochloride] and pertussis toxin (PTX) pretreatment. Rimonabant 85-94 cannabinoid receptor 1 Homo sapiens 68-72 14751433-0 2004 Selective antagonist [3H]SR141716A binding to cannabinoid CB1 receptors is increased in the anterior cingulate cortex in schizophrenia. Rimonabant 25-34 cannabinoid receptor 1 Homo sapiens 58-61 14751433-5 2004 Radioligand binding of [3H]SR141716A, an antagonist that specifically targets CB1 receptors of the endogenous cannabinoid system, was examined on ACC sections using quantitative autoradiography. Rimonabant 27-36 cannabinoid receptor 1 Homo sapiens 78-81 15005177-3 2004 Relatively selective agonists and antagonists for these receptors have been developed, although one agent (SR141716A) widely used as an antagonist at CB1 receptors has non-cannabinoid receptor-mediated effects at concentrations which are often used to define the presence of the CB1 receptor. Rimonabant 107-116 cannabinoid receptor 1 Homo sapiens 150-153 15005177-3 2004 Relatively selective agonists and antagonists for these receptors have been developed, although one agent (SR141716A) widely used as an antagonist at CB1 receptors has non-cannabinoid receptor-mediated effects at concentrations which are often used to define the presence of the CB1 receptor. Rimonabant 107-116 cannabinoid receptor 1 Homo sapiens 279-282 14746372-15 2003 The induction in sleep and the rise in adenosine were blocked by the CB1-receptor antagonist, SR141716A. Rimonabant 94-103 cannabinoid receptor 1 Homo sapiens 69-72 12690115-0 2003 Hypersensitization of the Orexin 1 receptor by the CB1 receptor: evidence for cross-talk blocked by the specific CB1 antagonist, SR141716. Rimonabant 129-137 cannabinoid receptor 1 Homo sapiens 51-54 14613317-3 2003 Modeling studies reported here suggest that in the inactive state of CB(1), the binding site of the CB(1) inverse agonist/antagonist SR141716A is within the TMH3-4-5-6 aromatic microdomain and involves direct aromatic stacking interactions with F3.36, Y5.39, and W5.43, as well as hydrogen bonding with K3.28. Rimonabant 133-142 cannabinoid receptor 1 Homo sapiens 69-74 14613317-3 2003 Modeling studies reported here suggest that in the inactive state of CB(1), the binding site of the CB(1) inverse agonist/antagonist SR141716A is within the TMH3-4-5-6 aromatic microdomain and involves direct aromatic stacking interactions with F3.36, Y5.39, and W5.43, as well as hydrogen bonding with K3.28. Rimonabant 133-142 cannabinoid receptor 1 Homo sapiens 100-105 14561865-5 2003 Thus, intrahippocampal infusion of the CB1R antagonist SR141716A or pertussis toxin blocked the inhibition of hippocampal ACh release induced by the high dose of WIN55,212-2, but was without effect on the stimulatory action of the low dose. Rimonabant 55-64 cannabinoid receptor 1 Homo sapiens 39-43 12690115-3 2003 This effect required a functional CB1 receptor as evidenced by the blockade of the orexin response by the specific CB1 antagonist, N-(piperidino-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-pyrazole-3-carboxamide (SR141716), but also by pertussis toxin, suggesting that this potentiation is Gi-mediated. Rimonabant 226-234 cannabinoid receptor 1 Homo sapiens 34-37 12690115-3 2003 This effect required a functional CB1 receptor as evidenced by the blockade of the orexin response by the specific CB1 antagonist, N-(piperidino-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-pyrazole-3-carboxamide (SR141716), but also by pertussis toxin, suggesting that this potentiation is Gi-mediated. Rimonabant 226-234 cannabinoid receptor 1 Homo sapiens 115-118 12690115-7 2003 Considering the antiobesity effect of SR141716, these results open new avenues to understand the mechanism by which the molecule may prevent weight gain through functional interaction between CB1 and other receptors involved in the control of appetite. Rimonabant 38-46 cannabinoid receptor 1 Homo sapiens 192-195 12690115-0 2003 Hypersensitization of the Orexin 1 receptor by the CB1 receptor: evidence for cross-talk blocked by the specific CB1 antagonist, SR141716. Rimonabant 129-137 cannabinoid receptor 1 Homo sapiens 113-116 12737320-4 2003 This effect was blocked by the CB1 receptor antagonist SR141716A (0.5 microM), and by phosphoinositide-3-kinase and phospholipase C inhibitors. Rimonabant 55-64 cannabinoid receptor 1 Homo sapiens 31-34 12759440-5 2003 In a previous study, we have shown that macrophages activated by SR141716A, a ligand of the cannabinoid receptor CB1, acquired the capacity to control Brucella and observed that the CB1 receptor-triggering engages the microbicidal activity of phagocytes. Rimonabant 65-74 cannabinoid receptor 1 Homo sapiens 113-116 12759440-5 2003 In a previous study, we have shown that macrophages activated by SR141716A, a ligand of the cannabinoid receptor CB1, acquired the capacity to control Brucella and observed that the CB1 receptor-triggering engages the microbicidal activity of phagocytes. Rimonabant 65-74 cannabinoid receptor 1 Homo sapiens 182-185 12737320-5 2003 The endogenous agonist of CB1 and VR1 receptors, anandamide, was more efficacious in inducing a VR1-mediated stimulation of [Ca2+]i in CB1-VR1-HEK cells than in VR1-HEK cells, and part of its effect on the former cells was blocked by SR141716A (0.5 microM). Rimonabant 234-243 cannabinoid receptor 1 Homo sapiens 26-29 12813001-5 2003 The toxicity of Delta(9)- THC was inhibited by the CB1 receptor antagonist SR141716A but not by the CB2 receptor antagonist SR144528. Rimonabant 75-84 cannabinoid receptor 1 Homo sapiens 51-54 12823468-3 2003 The excitatory effect of anandamide was potentiated by the CB1 receptor antagonist SR141716A. Rimonabant 83-92 cannabinoid receptor 1 Homo sapiens 59-62 12570386-0 2003 Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity. Rimonabant 62-70 cannabinoid receptor 1 Homo sapiens 97-125 12890515-10 2003 The CB1 receptor antagonist/inverse agonist SR141716 enhanced ACh release in the human neocortex (by 38%) and prevented the inhibitory effect of WIN55212-2. Rimonabant 44-52 cannabinoid receptor 1 Homo sapiens 4-7 12399252-1 2003 Because the CB1 receptor antagonist SR141716 was previously reported to modulate food intake in rodents, we studied its efficacy in reducing obesity in a diet-induced obesity (DIO) model widely used for research on the human obesity syndrome. Rimonabant 36-44 cannabinoid receptor 1 Homo sapiens 12-15 12890515-19 2003 SR141716 acts as a competitive CB1 receptor antagonist. Rimonabant 0-8 cannabinoid receptor 1 Homo sapiens 31-34 12381672-7 2002 The CB1 receptor ligand [3H]-SR141716A and the CB1/CB2 receptor ligand [3H]-CP55940 did not specifically bind to parental HEK293 cells. Rimonabant 29-38 cannabinoid receptor 1 Homo sapiens 4-7 12435794-0 2002 N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A) interaction with LYS 3.28(192) is crucial for its inverse agonism at the cannabinoid CB1 receptor. Rimonabant 97-106 cannabinoid receptor 1 Homo sapiens 193-196 12435794-2 2002 In contrast, in neurons expressing CB1 with a K-->A mutation at residue 3.28(192) (i.e., K3.28A), SR141716A competitively antagonizes the effects of WIN55212-2, but behaves as a neutral antagonist by producing no current effects itself. Rimonabant 101-110 cannabinoid receptor 1 Homo sapiens 35-38 12435794-5 2002 Binding affinities suggested that K3.28 is involved in a strong interaction with SR141716A in WT CB1, but does not interact with VCHSR. Rimonabant 81-90 cannabinoid receptor 1 Homo sapiens 97-100 12435794-6 2002 Thermodynamic cycle calculations indicated that a direct interaction occurs between the C3 substituent of SR141716A and K3.28 in WT CB1. Rimonabant 106-115 cannabinoid receptor 1 Homo sapiens 132-135 12038810-5 2002 The selective CB1 receptor antagonist SR141716, which had no effect in the absence of (+)WIN 55,212-2, competitively antagonised its inhibition of electrical field stimulation contractions, unlike the selective CB2 antagonist SR144528. Rimonabant 38-46 cannabinoid receptor 1 Homo sapiens 14-17 11698062-0 2001 The cannabinoid CB1 receptor antagonist SR 141716A reverses the antiemetic and motor depressant actions of WIN 55, 212-2. Rimonabant 40-50 cannabinoid receptor 1 Homo sapiens 16-19 11358910-8 2001 Findings that the CB1 selective antagonist/inverse agonist SR141716A produces in vivo and in vitro signs of increased motility of rodent small intestine probably reflect the presence in the enteric nervous system of a population of CB1 receptors that are precoupled to their effector mechanisms. Rimonabant 59-68 cannabinoid receptor 1 Homo sapiens 18-21 11358910-8 2001 Findings that the CB1 selective antagonist/inverse agonist SR141716A produces in vivo and in vitro signs of increased motility of rodent small intestine probably reflect the presence in the enteric nervous system of a population of CB1 receptors that are precoupled to their effector mechanisms. Rimonabant 59-68 cannabinoid receptor 1 Homo sapiens 232-235 11236843-8 2001 RESULTS: In the ethanol condition, the CB1 receptor antagonist SR141716A (0.3-3.0 mg/kg, ip) produced dose-related decreases in the probability of response requirement completion without significantly affecting latency to first lever press or overall lever press rate. Rimonabant 63-72 cannabinoid receptor 1 Homo sapiens 39-42 11397872-9 2001 However, simultaneous application of CRF and WIN 55,212--2 resulted in a synergistic effect on ACTH secretion, and this effect could be abolished by SR 141716A, demonstrating a CB1-mediated effect. Rimonabant 149-159 cannabinoid receptor 1 Homo sapiens 177-180 11296091-0 2001 Blockade of effects of smoked marijuana by the CB1-selective cannabinoid receptor antagonist SR141716. Rimonabant 93-101 cannabinoid receptor 1 Homo sapiens 47-50 11296091-1 2001 BACKGROUND: SR141716, a recently developed CB1 cannabinoid receptor antagonist, blocks acute effects of Delta-9-tetrahydrocannabinol (THC) and other CB1 cannabinoid agonists in vitro and in animals. Rimonabant 12-20 cannabinoid receptor 1 Homo sapiens 43-46 11296091-1 2001 BACKGROUND: SR141716, a recently developed CB1 cannabinoid receptor antagonist, blocks acute effects of Delta-9-tetrahydrocannabinol (THC) and other CB1 cannabinoid agonists in vitro and in animals. Rimonabant 12-20 cannabinoid receptor 1 Homo sapiens 149-152 11081515-7 2000 In support of this conclusion, the CB1 antagonist SR141716A enhances capsaicin-evoked bronchospasm and cough. Rimonabant 50-59 cannabinoid receptor 1 Homo sapiens 35-38 10871313-10 2000 SR141716A, a selective antagonist for CB1, inhibited the cannabinoid agonist-induced migratory responses in a concentration-dependent manner. Rimonabant 0-9 cannabinoid receptor 1 Homo sapiens 38-41 11067978-2 2000 WIN-2 (20-40 nM) produced an average 45% decrease in I(K) amplitude across all voltage steps, which was prevented by SR141716A, the CB1 receptor antagonist. Rimonabant 117-126 cannabinoid receptor 1 Homo sapiens 132-135 10698714-4 2000 Transfection of ECV304 cells with CB1 receptor antisense, but not sense, oligonucleotides caused the same pattern of inhibition as SR141716A. Rimonabant 131-140 cannabinoid receptor 1 Homo sapiens 34-37 10531431-8 1999 In SCG neurons microinjected with a lower concentration of hCB1 cDNA, the effect of SR 141716A was reduced, and the response to NE and SOM was partially restored. Rimonabant 84-94 cannabinoid receptor 1 Homo sapiens 59-63 10974429-10 2000 Furthermore, the cannabinoid antagonist SR141716A completely prevented the HU210-induced excitation whilst having no effect on its own, thus indicating a CB1-receptor mediated mechanism for the observed increase in firing. Rimonabant 40-49 cannabinoid receptor 1 Homo sapiens 154-157 10716447-8 2000 The exacerbation of these signs after antagonism of the CB1 and CB2 receptors, notably the CB1 receptor, using SR141716A and SR144528 (ref. Rimonabant 111-120 cannabinoid receptor 1 Homo sapiens 91-94 10614630-4 2000 The effect of anandamide was blocked by the CB1 receptor antagonist, SR141716A, but not by the CB2 receptor antagonist, SR144528. Rimonabant 69-78 cannabinoid receptor 1 Homo sapiens 44-47 10612710-6 1999 The CB1 antagonist, SR141716A, differentially blocks Delta(9)-THC versus AEA. Rimonabant 20-29 cannabinoid receptor 1 Homo sapiens 4-7 10493099-4 1999 The N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazo le-carboxamide (SR141716A)-mediated attenuation of spinal antinociception imparted by the various cannabinoids indicates cannabinoid CB1 receptor involvement. Rimonabant 93-102 cannabinoid receptor 1 Homo sapiens 210-213 10493099-6 1999 The release of dynorphin A was also attenuated by SR141716A suggesting it is cannabinoid CB1 receptor-mediated. Rimonabant 50-59 cannabinoid receptor 1 Homo sapiens 89-92 10469889-3 1999 Since its discovery in 1994, the selective CB1 antagonist SR 141716 has became a major pharmacological tool to elucidate the physiological role of the CB1 cannabinoid receptor and its endogenous ligand. Rimonabant 58-67 cannabinoid receptor 1 Homo sapiens 43-46 10469889-3 1999 Since its discovery in 1994, the selective CB1 antagonist SR 141716 has became a major pharmacological tool to elucidate the physiological role of the CB1 cannabinoid receptor and its endogenous ligand. Rimonabant 58-67 cannabinoid receptor 1 Homo sapiens 151-154 10494885-3 1999 The inhibition by CP55,940 and anandamide was abolished by the CB1 receptor antagonists SR141716A (1 microM) and LY320135 (1 microM). Rimonabant 88-97 cannabinoid receptor 1 Homo sapiens 63-66 10433501-10 1999 The inhibition was reversed by the CB1 receptor selective antagonist, SR141716 (3 microM). Rimonabant 70-78 cannabinoid receptor 1 Homo sapiens 35-38 10362691-8 1999 The inhibitory effects of both ligands on peak L-type Ca2+ currents were abolished by pertussis toxin pretreatment and application of the CB1-receptor antagonist SR-141716A (100 nM, n = 5). Rimonabant 162-172 cannabinoid receptor 1 Homo sapiens 138-141 10217281-6 1999 Treatment with the CB1-specific inverse agonist SR141716A inhibited the basal accumulation of cAMP in the presence of pertussis toxin, establishing that the effect is CB1 mediated. Rimonabant 48-57 cannabinoid receptor 1 Homo sapiens 19-22 10341254-9 1999 In contrast, the CB1 cannabinoid receptor antagonist SR 141716A (1 microM) prevented this effect, whereas by itself it did not change the outflow of [3H]GABA. Rimonabant 53-63 cannabinoid receptor 1 Homo sapiens 17-20 10217281-6 1999 Treatment with the CB1-specific inverse agonist SR141716A inhibited the basal accumulation of cAMP in the presence of pertussis toxin, establishing that the effect is CB1 mediated. Rimonabant 48-57 cannabinoid receptor 1 Homo sapiens 167-170 10394995-2 1999 OBJECTIVE: The present study investigated whether SR 141716, a selective CB1 receptor antagonist, was able to reduce the hyperactivity induced in gerbils by various stimulant drugs known to produce or exacerbate schizophrenic symptoms. Rimonabant 50-59 cannabinoid receptor 1 Homo sapiens 73-76 10323591-13 1999 The CB1 cannabinoid receptor antagonist SR141716A (1 microM) only produced a marginal reduction of the mobilization of Ca2+ produced by 5 microM anandamide. Rimonabant 40-49 cannabinoid receptor 1 Homo sapiens 4-7 11741201-2 1999 This compound is an analog of the potent, CB1 receptor selective antagonist SR141716A [N-(piperidin-1-yl)-1-(2,4-dichlorophenyl)-5-(4-chlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide]. Rimonabant 76-85 cannabinoid receptor 1 Homo sapiens 42-45 9933150-5 1999 Coupled to our previous observation that the CB1 receptor antagonist SR141716A opposes EDHF-mediated relaxation, the present observations point to the involvement of a cannabinoid receptor, which may be CB or CB1-like, in EDHF-mediated vasorelaxation. Rimonabant 69-78 cannabinoid receptor 1 Homo sapiens 45-48 9933150-5 1999 Coupled to our previous observation that the CB1 receptor antagonist SR141716A opposes EDHF-mediated relaxation, the present observations point to the involvement of a cannabinoid receptor, which may be CB or CB1-like, in EDHF-mediated vasorelaxation. Rimonabant 69-78 cannabinoid receptor 1 Homo sapiens 209-212 10392859-5 1999 The effect was maximal at 100 nM anandamide and was reversed by the selective antagonist of the CB1 subtype of mammalian cannabinoid receptors, SR 141716A (50-100 nM). Rimonabant 144-154 cannabinoid receptor 1 Homo sapiens 96-99 9884065-4 1998 The cannabinoid CB1 receptor antagonist SR 141716 (pA2 8.2), but not the CB2 receptor antagonist, SR 144528, competitively antagonized twitch inhibition by (+)WIN-55212-2. Rimonabant 40-49 cannabinoid receptor 1 Homo sapiens 16-19 9884065-8 1998 SR 141716 is a potent and competitive antagonist of cannabinoid CB1 receptors naturally expressed in the human gut. Rimonabant 0-9 cannabinoid receptor 1 Homo sapiens 64-67 9685157-6 1998 In agreement with this possibility, the CB1 antagonist SR141716A and the CB2 antagonist SR144528 prolong and enhance the pain behaviour produced by tissue damage. Rimonabant 55-64 cannabinoid receptor 1 Homo sapiens 40-43 9653194-8 1998 Moreover, anandamide cytostatic effect was inhibited by the selective CB1 receptor antagonist SR 141716A. Rimonabant 94-104 cannabinoid receptor 1 Homo sapiens 70-73 9268384-3 1997 These activities could be blocked by the CB1-selective ligand, SR 141716A, that functions as an inverse agonist. Rimonabant 63-73 cannabinoid receptor 1 Homo sapiens 41-44 9688276-7 1998 The CB1 receptor selective antagonist SR 141716A (0.5 microM) reversed the effect of both arachidonoylethanolamide and oleamide. Rimonabant 38-48 cannabinoid receptor 1 Homo sapiens 4-7 9690851-0 1998 Evidence for inverse agonism of SR141716A at human recombinant cannabinoid CB1 and CB2 receptors. Rimonabant 32-41 cannabinoid receptor 1 Homo sapiens 75-78 9690851-1 1998 The cannabinoid receptor antagonist SR141716A has been suggested to be an inverse agonist at CB1 receptors in some isolated intact tissues. Rimonabant 36-45 cannabinoid receptor 1 Homo sapiens 93-96 9690851-2 1998 We found that the basal incorporation of [35S]-GTPgammaS in Chinese hamster ovary cells expressing human recombinant CB1 and CB2 receptors was inhibited by SR141716A (mean pEC50s 8.26 and 6.00, respectively), whereas cannabinol (10 microM) had no significant effect at hCB1 receptors but inhibited the binding at hCB2 receptors. Rimonabant 156-165 cannabinoid receptor 1 Homo sapiens 117-120 9690851-2 1998 We found that the basal incorporation of [35S]-GTPgammaS in Chinese hamster ovary cells expressing human recombinant CB1 and CB2 receptors was inhibited by SR141716A (mean pEC50s 8.26 and 6.00, respectively), whereas cannabinol (10 microM) had no significant effect at hCB1 receptors but inhibited the binding at hCB2 receptors. Rimonabant 156-165 cannabinoid receptor 1 Homo sapiens 269-273 9346339-0 1997 SR141716A is an inverse agonist at the human cannabinoid CB1 receptor. Rimonabant 0-9 cannabinoid receptor 1 Homo sapiens 57-60 9268384-7 1997 Furthermore, SR 141716A inhibited guanosine 5"-0-(thiotriphosphate) uptake induced by CP-55,940 or Mas-7 in CHO-CB1 cell membranes. Rimonabant 13-23 cannabinoid receptor 1 Homo sapiens 112-115 9268384-8 1997 This indicates that, in addition to the inhibition of autoactivated CB1, SR 141716A can deliver a biological signal that blocks the Gi protein and consequently abrogates most of the Gi-mediated responses. Rimonabant 73-83 cannabinoid receptor 1 Homo sapiens 68-71 8856836-0 1996 Improvement of memory in rodents by the selective CB1 cannabinoid receptor antagonist, SR 141716. Rimonabant 87-96 cannabinoid receptor 1 Homo sapiens 50-53 9204917-6 1997 This augmentation was blocked by the CB1 receptor antagonist SR141716A or the D2 antagonist sulpride. Rimonabant 61-70 cannabinoid receptor 1 Homo sapiens 37-40 9204917-8 1997 The cannabinoid receptor-stimulated accumulation of cAMP was blocked in a concentration-dependent manner by SR141716A, suggesting that the response was regulated through the CB1 receptor. Rimonabant 108-117 cannabinoid receptor 1 Homo sapiens 174-177 9126878-7 1997 The CB1 antagonist, SR141716A, was effective in reducing the THC elevated levels of free arachidonate in these cells in agreement with the antisense data. Rimonabant 20-29 cannabinoid receptor 1 Homo sapiens 4-7 8768742-5 1996 The cannabinoid receptor antagonist SR 141716A also bound to CB1A (Ki = 43.3 nM) with slightly less affinity than to CB1 (Ki = 4.9 nM). Rimonabant 36-46 cannabinoid receptor 1 Homo sapiens 61-65 8768742-5 1996 The cannabinoid receptor antagonist SR 141716A also bound to CB1A (Ki = 43.3 nM) with slightly less affinity than to CB1 (Ki = 4.9 nM). Rimonabant 36-46 cannabinoid receptor 1 Homo sapiens 61-64 8856836-4 1996 SR 141716, a specific antagonist of CB1 receptors, dose-dependently reverses biochemical and pharmacological effects of cannabimimetics. Rimonabant 0-9 cannabinoid receptor 1 Homo sapiens 36-39 8856836-11 1996 As SR 141716 is not known to exhibit any pharmacological activity which is not mediated by CB1 receptors, the results strongly support the concept that blockade of CB1 receptors plays an important role in consolidation of short-term memory in rodents and suggest there may be a role for an endogenous cannabinoid agonist tone (anandaminergic) in forgetting. Rimonabant 3-12 cannabinoid receptor 1 Homo sapiens 164-167 8739546-1 1996 SR141716A (Sanofi Recherche), a pyrazole derivative with high affinity for rat and human CB1 cannabinoid receptors, has recently been reported to reverse biochemical, physiological and behavioral effects induced by cannabinoid agonists. Rimonabant 0-9 cannabinoid receptor 1 Homo sapiens 89-92 34326318-3 2021 A novel agent named TXX-1-10 derived from rimonabant, an antagonist of cannabinoid receptor 1 with anticancer effects, has been discovered to reduce HPIP expression and has greater inhibitory effects on breast cancer cell growth and metastasis in vitro and in vivo than rimonabant. Rimonabant 42-52 cannabinoid receptor 1 Homo sapiens 71-93 8526880-2 1995 Using stably transfected Chinese Hamster Ovary cells expressing human CB1 we show here that cannabinoid treatment induces both phosphorylation and activation of mitogen-activated protein (MAP) kinases, and that these effects are inhibited by SR 141716A, a selective CB1 antagonist. Rimonabant 242-252 cannabinoid receptor 1 Homo sapiens 70-73 8526880-2 1995 Using stably transfected Chinese Hamster Ovary cells expressing human CB1 we show here that cannabinoid treatment induces both phosphorylation and activation of mitogen-activated protein (MAP) kinases, and that these effects are inhibited by SR 141716A, a selective CB1 antagonist. Rimonabant 242-252 cannabinoid receptor 1 Homo sapiens 266-269 7565624-9 1995 SR141716A, a CB1 receptor antagonist, was a poor antagonist at the CB2 receptor in both binding and functional inhibition of cAMP accumulation experiments. Rimonabant 0-9 cannabinoid receptor 1 Homo sapiens 13-16 18802648-2 2008 Based on the bioisosteric replacement of the pyrazole C3-carboxamide of rimonabant with a 5-alkyl oxadiazole ring, a novel class of oxadiazole derivatives with promising biological activity towards CB1 receptors was discovered. Rimonabant 72-82 cannabinoid receptor 1 Homo sapiens 198-201 7775459-6 1995 The specific involvement of CB1 in Krox-24 induction was demonstrated in Chinese hamster ovary cells transfected with the human CB1 receptor and also in experiments using the CB1-selective cannabinoid antagonist SR 141716A. Rimonabant 212-222 cannabinoid receptor 1 Homo sapiens 28-31 33002729-4 2020 The utility of method was demonstrated to synthesize CB1 ligands including Rimonabant analogue 4c and LH-21 3 for modeling study. Rimonabant 75-85 cannabinoid receptor 1 Homo sapiens 53-56 32885412-8 2021 In summary, rimonabant can stimulate protein synthesis in C2C12 myotubes through a CB1-independent mechanism. Rimonabant 12-22 cannabinoid receptor 1 Homo sapiens 83-86 34064024-4 2021 The inhibitory effect of the cannabinoid receptor 1 (CB1) antagonist rimonabant on fat mass suggested that the endocannabinoid system can also have a peripheral action in addition to its effect on appetite reduction. Rimonabant 69-79 cannabinoid receptor 1 Homo sapiens 29-51 34064024-4 2021 The inhibitory effect of the cannabinoid receptor 1 (CB1) antagonist rimonabant on fat mass suggested that the endocannabinoid system can also have a peripheral action in addition to its effect on appetite reduction. Rimonabant 69-79 cannabinoid receptor 1 Homo sapiens 53-56 33931678-7 2021 Next, using the CB1-selective antagonist SR141716A, we observed an increase in excitatory, and to a lesser extent, inhibitory synaptogenesis as measured by confocal image analysis. Rimonabant 41-50 cannabinoid receptor 1 Homo sapiens 16-19 33573565-5 2022 Preclinical data suggest significant potential for the use of CB1 antagonists to treat AUD; however, a clinical phase I/II trial with SR14716A (rimonabant), a CB1 receptor antagonist/inverse agonist showed that it produced serious neuropsychiatric adverse events such as anxiety, depression, and even suicidal ideation. Rimonabant 144-154 cannabinoid receptor 1 Homo sapiens 62-65 33573565-5 2022 Preclinical data suggest significant potential for the use of CB1 antagonists to treat AUD; however, a clinical phase I/II trial with SR14716A (rimonabant), a CB1 receptor antagonist/inverse agonist showed that it produced serious neuropsychiatric adverse events such as anxiety, depression, and even suicidal ideation. Rimonabant 144-154 cannabinoid receptor 1 Homo sapiens 159-162 31925452-3 2020 Thus, CB1 antagonists such as SR141716A, also known as rimonabant, and AM251 act as GPR55 agonists in some cell types. Rimonabant 30-39 cannabinoid receptor 1 Homo sapiens 6-9 31925452-3 2020 Thus, CB1 antagonists such as SR141716A, also known as rimonabant, and AM251 act as GPR55 agonists in some cell types. Rimonabant 55-65 cannabinoid receptor 1 Homo sapiens 6-9 32927872-2 2020 The brain- and peripheral-cannabinoid receptor 1 (CB1R) antagonist rimonabant (RIM) has been shown to induce weight loss and improve glucose homeostasis. Rimonabant 67-77 cannabinoid receptor 1 Homo sapiens 50-54 32417279-2 2020 Unfortunately, SR1417116A (rimonabant), the first marketed inverse agonist of CB1R, produced CNS-related adverse effects including depression and suicidal ideation, and thus it was withdrawn from the market. Rimonabant 27-37 cannabinoid receptor 1 Homo sapiens 78-82 32512776-9 2020 Recent preclinical studies suggest that ligands targeting the CB1 may retain the therapeutic potential of rimonabant without the negative side effect profile. Rimonabant 106-116 cannabinoid receptor 1 Homo sapiens 62-65 31469511-8 2019 Administration of rimonabant, a CB1 antagonist, blunted collagen synthesis by tubular cells (P < .05). Rimonabant 18-28 cannabinoid receptor 1 Homo sapiens 32-35 31564385-0 2019 Divalent cannabinoid-1 receptor ligands: A linker attachment point survey of SR141716A for development of high-affinity CB1R molecular probes. Rimonabant 77-86 cannabinoid receptor 1 Homo sapiens 9-31 31564385-0 2019 Divalent cannabinoid-1 receptor ligands: A linker attachment point survey of SR141716A for development of high-affinity CB1R molecular probes. Rimonabant 77-86 cannabinoid receptor 1 Homo sapiens 120-124 31564385-1 2019 The cannabinoid-1 receptor (CB1R) inverse agonist SR141716A has proven useful for study of the endocannabinoid system, including development of divalent CB1R ligands possessing a second functional motif attached via a linker unit. Rimonabant 50-59 cannabinoid receptor 1 Homo sapiens 4-26 31564385-1 2019 The cannabinoid-1 receptor (CB1R) inverse agonist SR141716A has proven useful for study of the endocannabinoid system, including development of divalent CB1R ligands possessing a second functional motif attached via a linker unit. Rimonabant 50-59 cannabinoid receptor 1 Homo sapiens 28-32 31564385-1 2019 The cannabinoid-1 receptor (CB1R) inverse agonist SR141716A has proven useful for study of the endocannabinoid system, including development of divalent CB1R ligands possessing a second functional motif attached via a linker unit. Rimonabant 50-59 cannabinoid receptor 1 Homo sapiens 153-157 31981244-5 2020 Finally, we identified a cannabinoid receptor 1 inhibitor, rimonabant, as a candidate showing anti-HBV effect. Rimonabant 59-69 cannabinoid receptor 1 Homo sapiens 25-47 31917333-8 2020 Moreover, the CB1R inverse agonist SR 141716A attenuated the decrease in neurite outgrowth and ERK1/2 phosphorylation induced by 2AG and Delta9-THC. Rimonabant 35-45 cannabinoid receptor 1 Homo sapiens 14-18 31284863-3 2019 However, the first-in-class CB1R antagonist/inverse agonist, rimonabant, though demonstrating effectiveness for obesity treatment and smoking cessation, displays serious psychiatric side effects, including anxiety, depression and even suicidal ideation, resulting in its eventual withdrawal from the European market. Rimonabant 61-71 cannabinoid receptor 1 Homo sapiens 28-32 30687889-8 2019 After correction by effects on cell proliferation, the CB1R antagonist, SR141716, afforded an almost full neuroprotection in CB1R-expressing cells even when a selective agonist, ACEA, was present. Rimonabant 72-80 cannabinoid receptor 1 Homo sapiens 55-59 30687889-8 2019 After correction by effects on cell proliferation, the CB1R antagonist, SR141716, afforded an almost full neuroprotection in CB1R-expressing cells even when a selective agonist, ACEA, was present. Rimonabant 72-80 cannabinoid receptor 1 Homo sapiens 125-129 30649023-7 2019 Several larger controlled clinical trials using orally administered rimonabant, a CB1 receptor antagonist, have consistently shown relative improvements in weight and plasma levels of triglyceride and high-density lipoprotein cholesterol among patients receiving the treatment. Rimonabant 68-78 cannabinoid receptor 1 Homo sapiens 82-85 30262909-7 2018 Rimonabant, an antagonist of CB1, promotes human satellite cell differentiation in vitro, increases the number of regenerated myofibers, and prevents locomotor impairment in dystrophic mice. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 29-32 29792186-14 2018 Pharmacologically blocking the CB1 and CB2 receptors with their respective antagonists SR141716A and AM-630, followed by the WIN-55 treatment of RCC cells allowed uncovering the involvement of CB2, which led to an arrest in the G0/G1 phase of the cell cycle and apoptosis. Rimonabant 87-96 cannabinoid receptor 1 Homo sapiens 31-34 30077609-3 2018 The non-tissue selective CB1 antagonist rimonabant (2) was approved as a weight-loss agent in Europe but produced centrally mediated adverse effects in some patients including dysphoria and suicidal ideation leading to its withdrawal. Rimonabant 40-50 cannabinoid receptor 1 Homo sapiens 25-28 30460698-8 2018 Finally, AMPK phosphorylation/activation and VASP phosphorylation are significantly reduced by SR141716, the specific inhibitor of type 1 cannabinoid receptor (CB1). Rimonabant 95-103 cannabinoid receptor 1 Homo sapiens 160-163 29407764-0 2018 Rimonabant, a potent CB1 cannabinoid receptor antagonist, is a Galphai/o protein inhibitor. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 21-24 29407764-1 2018 Rimonabant is a potent and selective cannabinoid CB1 receptor antagonist widely used in animal and clinical studies. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 49-52 29407764-7 2018 Rimonabant prevented G protein-mediated GABAB and D2 dopamine receptor signaling to adenylyl cyclase in Human Embryonic Kidney 293 cells and to G protein-coupled inwardly rectifying K+ channels (GIRK) in midbrain dopamine neurons of CB1 KO mice. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 233-236 28947487-6 2017 Results indicate that CB1-related discriminative stimulus effects were produced by combined, but not selective, inhibition of FAAH and MGL, and that these effects were nonsurmountably antagonized by low doses of rimonabant. Rimonabant 212-222 cannabinoid receptor 1 Homo sapiens 22-25 29417597-10 2018 Treatment with 2 different CB1R antagonists (AM251 or SR141716) reversed both CB1R agonist and EtOH inhibition of adult neurogenesis. Rimonabant 54-62 cannabinoid receptor 1 Homo sapiens 27-31 29417597-10 2018 Treatment with 2 different CB1R antagonists (AM251 or SR141716) reversed both CB1R agonist and EtOH inhibition of adult neurogenesis. Rimonabant 54-62 cannabinoid receptor 1 Homo sapiens 78-82 29354056-4 2017 Rimonabant, originally synthesized as antagonist/inverse agonist of Cannabinoid Receptor 1, is able to inactivate Wnt signaling, both in vitro and in vivo, in CRC models, through inhibition of p300-histone acetyltransferase activity. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 68-90 28661046-6 2018 Finally, AMPKalpha activation, Cofilin, VASP, and MLCs phosphorylation are significantly reduced by SR141716, the specific inhibitor of type 1 cannabinoid (CB1) receptor, suggesting that the CB1 receptor is involved in the 2-AG effect. Rimonabant 100-108 cannabinoid receptor 1 Homo sapiens 156-159 28661046-6 2018 Finally, AMPKalpha activation, Cofilin, VASP, and MLCs phosphorylation are significantly reduced by SR141716, the specific inhibitor of type 1 cannabinoid (CB1) receptor, suggesting that the CB1 receptor is involved in the 2-AG effect. Rimonabant 100-108 cannabinoid receptor 1 Homo sapiens 191-194 29551963-7 2018 The effects were reversed by the Type 1 CB-R (CB1-R)-specific antagonist SR-141716A. Rimonabant 73-83 cannabinoid receptor 1 Homo sapiens 40-44 29551963-7 2018 The effects were reversed by the Type 1 CB-R (CB1-R)-specific antagonist SR-141716A. Rimonabant 73-83 cannabinoid receptor 1 Homo sapiens 46-51 28222356-5 2017 This process was context-dependent and could be blocked by pharmacological (3 mg/kg, s.c.; SR141716) or genetic (lack of cannabinoid CB1 receptors in neurons expressing dopamine D1 receptors) inactivation of CB1 receptors. Rimonabant 91-99 cannabinoid receptor 1 Homo sapiens 208-211 28564576-6 2017 The cannabinoid receptor 1 (CB1) inverse agonist rimonabant showed promising effects for smoking cessation but also caused psychiatric side effects and currently lacks regulatory approval. Rimonabant 49-59 cannabinoid receptor 1 Homo sapiens 4-26 28564576-6 2017 The cannabinoid receptor 1 (CB1) inverse agonist rimonabant showed promising effects for smoking cessation but also caused psychiatric side effects and currently lacks regulatory approval. Rimonabant 49-59 cannabinoid receptor 1 Homo sapiens 28-31 27208730-6 2016 Strikingly, this anti-insulin action of dexamethasone was also blocked by two CB1 cannabinoid receptor (CB1R) antagonists, O-2050 (500nM) and SR141716A (500nM), as well as by tetrahydrolipstatin (10muM), an inhibitor of diacylglycerol lipases-the enzymes responsible for the synthesis of the endocannabinoid, 2-arachidonoyl-glycerol (2-AG). Rimonabant 142-151 cannabinoid receptor 1 Homo sapiens 104-108 29308855-2 2017 However, rimonabant adverse effects include depression, anxiety, nausea, and dizziness which are apparently due to the blockade of central CB1 receptors. Rimonabant 9-19 cannabinoid receptor 1 Homo sapiens 139-142 25893829-9 2015 In all the experiments done, the quercetin action has proven to be reinforced by anandamide (Met-F-AEA), a CB1-R agonist, and partially counteracted by SR141716, a CB1-R antagonist. Rimonabant 152-160 cannabinoid receptor 1 Homo sapiens 164-169 26123153-6 2016 In rodents, treatment with the CB1 inverse agonist SR141716A (Rimonabant), or genetic deletion of CB1 leads to a reduction in voluntary ethanol drinking, ethanol-stimulated dopamine release in the nucleus accumbens, operant self-administration of ethanol, sensitization to the locomotor effects of ethanol, and reinstatement/relapse of ethanol-motivated behavior. Rimonabant 51-60 cannabinoid receptor 1 Homo sapiens 31-34 26123153-7 2016 Although the clinical utility of Rimonabant or other antagonists/inverse agonists for CB1 is limited due to negative neuropsychiatric side effects, negative allosteric modulators of CB1 and inhibitors of endocannabinoid catabolism represent therapeutic targets worthy of additional examination. Rimonabant 33-43 cannabinoid receptor 1 Homo sapiens 86-89 26803499-9 2016 Both AM404 self-administration behavior and reinstatement of drug seeking by AM404 were reduced by treatment with the cannabinoid CB1 receptor antagonist/inverse agonist rimonabant (0.3 mg/kg). Rimonabant 170-180 cannabinoid receptor 1 Homo sapiens 130-133 26157624-3 2015 We have previously shown that rimonabant (SR141716A) induces cell death in ex vivo isolated malignant lymphomas with high expression of CB1 receptors. Rimonabant 42-51 cannabinoid receptor 1 Homo sapiens 136-139 26365347-6 2015 Additionally, OLGly markedly increased the mRNA expression of CB1 receptor (CB1R) and the inhibition of CB1R by its antagonist SR141716 abolished the promotive effects of OLGly on lipid accumulation and the protein expression of PPARgamma and aP2. Rimonabant 127-135 cannabinoid receptor 1 Homo sapiens 104-108 26362774-1 2015 BACKGROUND: The cannabinoid cannabinoid type 1 (CB1) neutral antagonist tetrahydrocannabivarin (THCv) has been suggested as a possible treatment for obesity, but without the depressogenic side-effects of inverse antagonists such as Rimonabant. Rimonabant 232-242 cannabinoid receptor 1 Homo sapiens 48-51 26157624-11 2015 This is in contrast to the induction of cell death previously observed in CB1 expressing lymphoma cells in response to treatment with rimonabant in vitro. Rimonabant 134-144 cannabinoid receptor 1 Homo sapiens 74-77 26008966-0 2015 Cannabinoid receptor CB1 regulates STAT3 activity and its expression dictates the responsiveness to SR141716 treatment in human glioma patients" cells. Rimonabant 100-108 cannabinoid receptor 1 Homo sapiens 21-24 26008966-2 2015 This finding prompted us to investigate the therapeutic exploitation of CB1 inactivation by SR141716 treatment, with regard to its direct and indirect cell-mediated effects against gliomas. Rimonabant 92-100 cannabinoid receptor 1 Homo sapiens 72-75 26008966-6 2015 These results indicate that CB1 and STAT3 participate in a new oncogenic network in the complex biology of glioma and their expression levels in patients dictate the efficacy of the CB1 antagonist SR141716 in multimodal glioma destruction. Rimonabant 197-205 cannabinoid receptor 1 Homo sapiens 28-31 26008966-6 2015 These results indicate that CB1 and STAT3 participate in a new oncogenic network in the complex biology of glioma and their expression levels in patients dictate the efficacy of the CB1 antagonist SR141716 in multimodal glioma destruction. Rimonabant 197-205 cannabinoid receptor 1 Homo sapiens 182-185 24467410-10 2014 Only CB1 receptors were involved in the response because the effects of cannabinoids were antagonized by SR141716, but not by SR144528. Rimonabant 105-113 cannabinoid receptor 1 Homo sapiens 5-8 25859226-3 2015 The CB1 receptor inverse agonist/antagonist rimonabant (also known as SR141716) was effective to decrease nicotine-taking and nicotine-seeking in rodents, as well as the elevation of dopamine induced by nicotine in brain reward area. Rimonabant 44-54 cannabinoid receptor 1 Homo sapiens 4-7 25859226-3 2015 The CB1 receptor inverse agonist/antagonist rimonabant (also known as SR141716) was effective to decrease nicotine-taking and nicotine-seeking in rodents, as well as the elevation of dopamine induced by nicotine in brain reward area. Rimonabant 70-78 cannabinoid receptor 1 Homo sapiens 4-7 25411367-2 2015 However, the first generation of CB1 inverse agonists, represented by rimonabant (SR141716A), otenabant, and taranabant, are centrally active, with a high level of psychiatric side effects. Rimonabant 70-80 cannabinoid receptor 1 Homo sapiens 33-36 25411367-2 2015 However, the first generation of CB1 inverse agonists, represented by rimonabant (SR141716A), otenabant, and taranabant, are centrally active, with a high level of psychiatric side effects. Rimonabant 82-91 cannabinoid receptor 1 Homo sapiens 33-36 25411367-7 2015 LDK1229 exhibits efficacy comparable with SR141716A in antagonizing the basal G protein coupling activity of CB1, as indicated by a reduction in guanosine 5"-O-(3-thio)triphosphate binding. Rimonabant 42-51 cannabinoid receptor 1 Homo sapiens 109-112 25411367-10 2015 It offers new opportunities for developing novel CB1 inverse agonists through the optimization of molecular properties, such as the polar surface area and hydrophilicity, to reduce the central activity observed with SR141716A. Rimonabant 216-225 cannabinoid receptor 1 Homo sapiens 49-52 25713910-3 2014 Rimonabant (SR141716) is cannabinoid receptor type 1 (CB1) antagonist. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 54-57 25713910-3 2014 Rimonabant (SR141716) is cannabinoid receptor type 1 (CB1) antagonist. Rimonabant 12-20 cannabinoid receptor 1 Homo sapiens 54-57 25713910-16 2014 Moreover, rimonabant inhibited the expression of phosphorylated FAK and ERK and down-regulated CB1 mRNA expression. Rimonabant 10-20 cannabinoid receptor 1 Homo sapiens 95-98 25096297-1 2014 Using rimonabant, a potent inverse agonist for cannabinoid receptor type 1 (CB1R), as parent ligand, a series of novel univalent and bivalent ligands were designed by variation of spacer length and its chemical structure. Rimonabant 6-16 cannabinoid receptor 1 Homo sapiens 76-80 24692267-7 2014 The LPS-induced inhibition of DeltaPsim was prevented by the selective CB1 cannabinoid receptor antagonist, SR141716. Rimonabant 108-116 cannabinoid receptor 1 Homo sapiens 71-74 24747288-4 2014 Rimonabant, a diaryl pyrazole was the first potent and selective CB1 receptor antagonist that was introduced into the market in 2006 but was withdrawn in 2008 due to its psychiatric side effects. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 65-68 23452341-2 2014 Central CB1R antagonists, notably rimonabant, induced weight loss and improved the metabolic profile in obese individuals, but were discontinued due to psychiatric side-effects. Rimonabant 34-44 cannabinoid receptor 1 Homo sapiens 8-12 24366865-3 2014 In ligand displacement assays, ORG27569 can displace the CB1 antagonist/inverse agonist, N-(piperidiny-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide(SR141716A). Rimonabant 186-195 cannabinoid receptor 1 Homo sapiens 57-60 24041123-2 2013 However, to date, the only clinically approved CB1 receptor antagonist, rimonabant, was withdrawn because of adverse central nervous system (CNS)-related side effects. Rimonabant 72-82 cannabinoid receptor 1 Homo sapiens 47-50 23070073-3 2013 However, the first marketed CB1R antagonist/inverse agonist rimonabant was discontinued, as its use was occasionally associated with negative affect and suicidality. Rimonabant 60-70 cannabinoid receptor 1 Homo sapiens 28-32 22995906-0 2012 Probing the interaction of SR141716A with the CB1 receptor. Rimonabant 27-36 cannabinoid receptor 1 Homo sapiens 46-49 23278450-3 2013 The recent withdrawal of Rimonabant, which targets another closely related cannabinoid receptor (CB1), accentuates the importance of selectivity for the development of CB2 ligands in order to minimize their effects on the CB1 receptor. Rimonabant 25-35 cannabinoid receptor 1 Homo sapiens 97-100 23278450-3 2013 The recent withdrawal of Rimonabant, which targets another closely related cannabinoid receptor (CB1), accentuates the importance of selectivity for the development of CB2 ligands in order to minimize their effects on the CB1 receptor. Rimonabant 25-35 cannabinoid receptor 1 Homo sapiens 222-225 23441106-5 2013 The CB1 receptor in the RPE cells was inhibited with small interfering RNA (siRNA) or rimonabant (SR141716). Rimonabant 98-106 cannabinoid receptor 1 Homo sapiens 4-7 23441106-11 2013 Deleting the CB1 receptor or treating with the CB1 receptor antagonist rimonabant (SR141716) rescued RPE cells from hydrogen peroxide-induced oxidative damage. Rimonabant 71-81 cannabinoid receptor 1 Homo sapiens 47-50 23441106-11 2013 Deleting the CB1 receptor or treating with the CB1 receptor antagonist rimonabant (SR141716) rescued RPE cells from hydrogen peroxide-induced oxidative damage. Rimonabant 83-91 cannabinoid receptor 1 Homo sapiens 13-16 23441106-11 2013 Deleting the CB1 receptor or treating with the CB1 receptor antagonist rimonabant (SR141716) rescued RPE cells from hydrogen peroxide-induced oxidative damage. Rimonabant 83-91 cannabinoid receptor 1 Homo sapiens 47-50 23890208-4 2013 Rimonabant, a selective CB1 antagonist, was the first drug acting on the EC system approved for the treatment of obesity. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 24-27 23287700-1 2013 Cannabinoid receptor 1 (CB(1)) inverse agonists (e.g., rimonabant) have been reported to produce adverse effects including nausea, emesis, and anhedonia that limit their clinical applications. Rimonabant 55-65 cannabinoid receptor 1 Homo sapiens 0-29 23161546-3 2012 Recently, several synthetic CB1 receptor inverse agonists/antagonists, such as SR141716A, AM251, and AM281, were reported to activate GPR55. Rimonabant 79-88 cannabinoid receptor 1 Homo sapiens 28-31 22995906-1 2012 SR141716A binds selectively to the brain cannabinoid (CB1) receptor and exhibits a potent inverse agonist/antagonist activity. Rimonabant 0-9 cannabinoid receptor 1 Homo sapiens 54-57 22995906-5 2012 We found from the simulation of the CB1-SR141716A complex that SR141716A projects toward TM5 to interact tightly with the major binding pocket, replacing the coordinated water molecules, and secures the Trp-356(6.48) rotameric switch in the inactive state to promote the formation of an extensive water-mediated H-bonding network to the highly conserved SLAXAD and NPXXY motifs in TM2/TM7. Rimonabant 40-49 cannabinoid receptor 1 Homo sapiens 36-39 22995906-7 2012 Simulation of the F174(2.61)A mutant CB1-SR141716A complex demonstrates the perturbation of TM2 that attenuates SR141716A binding indirectly. Rimonabant 41-50 cannabinoid receptor 1 Homo sapiens 37-40 22995906-7 2012 Simulation of the F174(2.61)A mutant CB1-SR141716A complex demonstrates the perturbation of TM2 that attenuates SR141716A binding indirectly. Rimonabant 112-121 cannabinoid receptor 1 Homo sapiens 37-40 23449551-2 2012 Rimonabant, a cannabinoid receptor 1 blocker in the endocannabinoid (EC) system, was indicated in Europe for the treatment of obesity and overweight patients with associated risk factors but withdrawn on Jan, 2009 because of side effects. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 14-36 22743603-1 2012 CB1 antagonists, including rimonabant (SR 141716A), hold considerable therapeutic potential in the reduction of appetite and lipogenesis and in improving the metabolic profile of obese individuals and those with diabetes. Rimonabant 27-37 cannabinoid receptor 1 Homo sapiens 0-3 22743603-1 2012 CB1 antagonists, including rimonabant (SR 141716A), hold considerable therapeutic potential in the reduction of appetite and lipogenesis and in improving the metabolic profile of obese individuals and those with diabetes. Rimonabant 39-49 cannabinoid receptor 1 Homo sapiens 0-3 22771770-4 2012 AM-251 and rimonabant are CB1R antagonist/inverse agonists employed to validate opioid-cannabinoid interactions, presumed to act selectively at CB1Rs. Rimonabant 11-21 cannabinoid receptor 1 Homo sapiens 26-30 22780328-4 2012 Rimonabant (SR141716) was the first selective CB1 inverse agonist/antagonist marketed for the treatment of obesity; however, psychiatric side effects, which may result from its actions in the brain or its inverse agonism, resulted in its removal from the market. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 46-49 22780328-4 2012 Rimonabant (SR141716) was the first selective CB1 inverse agonist/antagonist marketed for the treatment of obesity; however, psychiatric side effects, which may result from its actions in the brain or its inverse agonism, resulted in its removal from the market. Rimonabant 12-20 cannabinoid receptor 1 Homo sapiens 46-49 22580290-6 2012 Pretreatment with 1 muM of CB1 antagonist SR141716A partially blocked, whereas pretreatment with either 1 muM of CB1 antagonist AM251 or 1 muM of CB2 antagonist SR144528 had no effect on abn-cbd induced enhancement of outflow facility. Rimonabant 42-51 cannabinoid receptor 1 Homo sapiens 27-30 22669247-8 2012 These effects were mediated by type 1 cannabinoid receptor (CB1) since they were fully counteracted by SR141716A (Rimonabant), a selective CB1 antagonist. Rimonabant 103-112 cannabinoid receptor 1 Homo sapiens 60-63 22669247-8 2012 These effects were mediated by type 1 cannabinoid receptor (CB1) since they were fully counteracted by SR141716A (Rimonabant), a selective CB1 antagonist. Rimonabant 103-112 cannabinoid receptor 1 Homo sapiens 139-142 22402754-2 2012 CB(1) antagonists such as Rimonabant have been used in clinic to inhibit food intake, and therefore reduce body weight in obese animals and humans. Rimonabant 26-36 cannabinoid receptor 1 Homo sapiens 0-5 22093909-1 2012 Rimonabant (SR141716) was the first potent and selective cannabinoid CB1 receptor antagonist synthesized. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 69-72 22428727-1 2012 Although the CB1 receptor antagonist/inverse agonist rimonabant has positive effects on weight loss and cardiometabolic risk factors, neuropsychiatric side effects have prompted researchers to develop peripherally acting derivatives. Rimonabant 53-63 cannabinoid receptor 1 Homo sapiens 13-16 22093909-1 2012 Rimonabant (SR141716) was the first potent and selective cannabinoid CB1 receptor antagonist synthesized. Rimonabant 12-20 cannabinoid receptor 1 Homo sapiens 69-72 21406493-0 2012 Effects of 7 days of treatment with the cannabinoid type 1 receptor antagonist, rimonabant, on emotional processing. Rimonabant 80-90 cannabinoid receptor 1 Homo sapiens 40-67 21406493-1 2012 Rimonabant is a cannabinoid type 1 receptor (CB1) antagonist formerly used to treat obesity, but which was withdrawn from the market in late 2008 because of its association with psychiatric adverse effects such as depression and anxiety. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 16-43 21406493-1 2012 Rimonabant is a cannabinoid type 1 receptor (CB1) antagonist formerly used to treat obesity, but which was withdrawn from the market in late 2008 because of its association with psychiatric adverse effects such as depression and anxiety. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 45-48 21803969-2 2011 Rimonabant, an inverse agonist of cannabinoid receptor type 1 (CB1), has been studied as an antiobesity drug. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 63-66 22087859-0 2011 Effect of the Cannabinoid Receptor-1 antagonist SR141716A on human adipocyte inflammatory profile and differentiation. Rimonabant 48-57 cannabinoid receptor 1 Homo sapiens 14-36 22087859-2 2011 SR141716A, a cannabinoid receptor 1 (CB1) antagonist, shows significant improvement in clinical status of obese/diabetic patients. Rimonabant 0-9 cannabinoid receptor 1 Homo sapiens 13-35 22087859-2 2011 SR141716A, a cannabinoid receptor 1 (CB1) antagonist, shows significant improvement in clinical status of obese/diabetic patients. Rimonabant 0-9 cannabinoid receptor 1 Homo sapiens 37-40 21386801-2 2011 The cannabinoid 1 receptor (CB1) antagonist SR141716 has been shown to improve obesity-associated metabolic complications in humans and rodent models. Rimonabant 44-52 cannabinoid receptor 1 Homo sapiens 4-26 21386801-2 2011 The cannabinoid 1 receptor (CB1) antagonist SR141716 has been shown to improve obesity-associated metabolic complications in humans and rodent models. Rimonabant 44-52 cannabinoid receptor 1 Homo sapiens 28-31 21803969-12 2011 In conclusion, rimonabant has an antilipogenic effect in hepatocytes by inhibiting LXRalpha-dependent SREBP-1c induction, as mediated by an increase in PKA activity and PKA-mediated LKB1 activation downstream of CB1-coupled Galpha(i/o) inhibition. Rimonabant 15-25 cannabinoid receptor 1 Homo sapiens 212-215 21963514-2 2011 Here we show that the specific CB1 cannabinoid receptor antagonist 5-(4-chlorophenyl)-1-(2,4-dichloro-phenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide (rimonabant or SR141716) blocks nonopioid placebo analgesic responses but has no effect on opioid placebo responses. Rimonabant 165-175 cannabinoid receptor 1 Homo sapiens 31-34 21963514-2 2011 Here we show that the specific CB1 cannabinoid receptor antagonist 5-(4-chlorophenyl)-1-(2,4-dichloro-phenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide (rimonabant or SR141716) blocks nonopioid placebo analgesic responses but has no effect on opioid placebo responses. Rimonabant 179-187 cannabinoid receptor 1 Homo sapiens 31-34 21934185-8 2011 SR141716 (rimonabant), a CB1 receptor antagonist, significantly lowers voluntary alcohol intake and motivation for its consumption in various experimental studies. Rimonabant 0-8 cannabinoid receptor 1 Homo sapiens 25-28 22646861-5 2011 The role of CB1R activity in hyperphagia and weight gain spurred the development of rimonabant (SR141716; Acomplia), the first-in-class CB1R antagonist/inverse agonist weight-loss drug. Rimonabant 84-94 cannabinoid receptor 1 Homo sapiens 136-140 22646861-9 2011 Laboratory studies demonstrate that CB1R neutral antagonists - whether readily accessible to the central nervous system or not (i.e., "periphero-neutral" antagonists) - retain the salient therapeutic effects of CB1R inverse agonists on hyperphagia, weight-gain, and obesity-driven metabolic abnormalities with the distinct advantage of being associated with significantly less preclinical adverse events than are conventional CB1R inverse agonists such as rimonabant. Rimonabant 456-466 cannabinoid receptor 1 Homo sapiens 36-40 21497918-2 2011 However, use of rimonabant (the first marketed CB1 receptor antagonist) has been suspended due to its anxiogenic and depressive side effects (including suicide risk). Rimonabant 16-26 cannabinoid receptor 1 Homo sapiens 47-50 21511945-7 2011 A number of CB1 receptor antagonists, including rimonabant, stimulated MRP2 and MRP3 transport activity at low substrate concentrations but inhibited E(2)17betaG transport at high substrate concentrations. Rimonabant 48-58 cannabinoid receptor 1 Homo sapiens 12-15 21373835-3 2011 Using genetic deletion or pharmacological inhibition of the CB(1) receptor with SR141716 (rimonabant) in a rodent model of diabetic retinopathy or in human primary retinal endothelial cells (HREC) exposed to high glucose, we explored the role of CB(1) receptors in the pathogenesis of diabetic retinopathy. Rimonabant 80-88 cannabinoid receptor 1 Homo sapiens 60-65 21373835-6 2011 RESULTS: Deletion of CB(1) receptor or treatment of diabetic mice with CB(1) receptor antagonist SR141716 prevented retinal cell death. Rimonabant 97-105 cannabinoid receptor 1 Homo sapiens 71-76 22091480-4 2010 Lysophosphatidylinositol (LPI; 1.2 muM) is representative of the recently identified endogenous GPR55 ligands and the CB1 inverse agonist/antagonists SR141716A (3.9 muM) and AM251 (9.6 muM), that are also GPR55 agonists, are representative of the cannabinoid receptor ligands that were screened against GPR55 when selectivity was not a consideration. Rimonabant 150-159 cannabinoid receptor 1 Homo sapiens 118-121 22091481-5 2010 There are no other known small molecule antagonists of GPR55 reported to date, only the CB1 inverse agonist/antagonists SR141716A (3.9 muM) and AM251 (9.6 muM). Rimonabant 120-129 cannabinoid receptor 1 Homo sapiens 88-91 21216016-3 2011 Here we show that the treatment of proteolipid protein (PLP)139-151-specific T cells with SR141716A, a CB1 inverse agonist and prototype of the diarylpyrazoles series, induced a strong inhibition of firm adhesion in inflamed brain venules in intravital microscopy experiments. Rimonabant 90-99 cannabinoid receptor 1 Homo sapiens 103-106 21216016-5 2011 In addition, two analogs of SR141716A and CB1 inverse agonists, AM251 and AM281 inhibited encephalitogenic T cell adhesion suggesting that selective CB1 inverse agonism interfere with lymphocyte trafficking in the CNS. Rimonabant 28-37 cannabinoid receptor 1 Homo sapiens 149-152 21328466-5 2011 Finally the anandamide effect on NO and cGMP levels, eNOS and AKT phosphorylation/activation were inhibited by SR141716, specific cannabinoid receptor 1 antagonist, supporting the involvement of anandamide binding to this receptor. Rimonabant 111-119 cannabinoid receptor 1 Homo sapiens 130-152 21256197-5 2011 This neuroprotective effect was blocked by SR141716 (SR-1), a selective CB1R antagonist, but not by SR144528 (SR-2), a selective CB2R antagonist, or capsazepine (CAP), a selective transient receptor potential cation channels, subfamily V, member 1 (TRPV1) receptor antagonist. Rimonabant 43-51 cannabinoid receptor 1 Homo sapiens 72-76 21863215-12 2011 Inhibition of CB1 by SR141716, or via genetic knock-out protects against alcoholic-induced fibrosis in vitro and in vivo. Rimonabant 21-29 cannabinoid receptor 1 Homo sapiens 14-17 21167293-5 2011 The proliferation inhibition was blocked by SR141716A (a selective CB1R antagonist) but not SR144528 (a selective CB2R antagonist), suggesting a CB1R-mediated inhibition mechanism. Rimonabant 44-53 cannabinoid receptor 1 Homo sapiens 67-71 21167293-5 2011 The proliferation inhibition was blocked by SR141716A (a selective CB1R antagonist) but not SR144528 (a selective CB2R antagonist), suggesting a CB1R-mediated inhibition mechanism. Rimonabant 44-53 cannabinoid receptor 1 Homo sapiens 145-149 21253513-1 2011 Rimonabant, a selective cannabinoid-1 (CB1) receptor antagonist, has been shown to reduce weight and enhance improvements in cardiometabolic risk parameters in Western populations. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 39-42 21037491-9 2011 CB1 receptor antagonist SR 141716A (1 muM) blocked this inhibitory effect of acetaminophen on SE, indicating that acetaminophen was mediating its anticonvulsant effects through CB1 receptors. Rimonabant 24-34 cannabinoid receptor 1 Homo sapiens 0-3 21037491-9 2011 CB1 receptor antagonist SR 141716A (1 muM) blocked this inhibitory effect of acetaminophen on SE, indicating that acetaminophen was mediating its anticonvulsant effects through CB1 receptors. Rimonabant 24-34 cannabinoid receptor 1 Homo sapiens 177-180 21886913-7 2011 By contrast, the inhibition of the cannabinoid system with the CB1 receptor antagonist rimonabant (SR141716) during ethanol withdrawal increased death of ethanol-withdrawn neurons without any modification of NMDA-stimulated calcium influx. Rimonabant 99-107 cannabinoid receptor 1 Homo sapiens 63-66 22016780-4 2011 Results showed that pretreatment with either the CB1 receptor antagonist/inverse agonist SR141716A or the neutral CB1 receptor antagonist O-2050 dose-dependently improved baseline inhibitory control in the 5-CSRTT. Rimonabant 89-98 cannabinoid receptor 1 Homo sapiens 49-52 20609360-3 2010 Rimonabant, a type 1 cannabinoid receptor (CB1) antagonist, produces anti-atherosclerotic effects in humans and animals by mechanisms which are not completely understood. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 43-46 20953204-6 2010 ACEA, a cannabinoid receptor subtype 1 (CB1) agonist, added before rimonabant abolished the former effects of rimonabant. Rimonabant 110-120 cannabinoid receptor 1 Homo sapiens 40-43 20426883-2 2010 The anti-obesity drug and cannabinoid type 1 receptor (CB(1)) antagonist, rimonabant, is associated with significant rates of depression and anxiety in clinical use and was recently withdrawn from the market because of these adverse effects. Rimonabant 74-84 cannabinoid receptor 1 Homo sapiens 26-60 21829686-4 2011 The CB1R involvement was studied by using the specific inhibitor (SR141716) or mimicking its activation by adding a permeable cAMP analogue (8Br-cAMP). Rimonabant 66-74 cannabinoid receptor 1 Homo sapiens 4-8 20953204-0 2010 Rimonabant inhibits TNF-alpha-induced endothelial IL-6 secretion via CB1 receptor and cAMP-dependent protein kinase pathway. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 69-72 20845959-2 2010 A library of bivalent ligands composed of two identical CB1 antagonist pharmacophores derived from SR141716 linked by spacers of various lengths were developed. Rimonabant 99-107 cannabinoid receptor 1 Homo sapiens 56-59 20417624-1 2010 Rimonabant (SR141716), a cannabinoid CB1 receptor antagonist known for anti-obesity activity, has more recently been shown to inhibit tumor cell growth. Rimonabant 0-10 cannabinoid receptor 1 Homo sapiens 37-40 20417624-1 2010 Rimonabant (SR141716), a cannabinoid CB1 receptor antagonist known for anti-obesity activity, has more recently been shown to inhibit tumor cell growth. Rimonabant 12-20 cannabinoid receptor 1 Homo sapiens 37-40 20590572-6 2010 The AEA- or HU210-induced cell death and MAPK activation were attenuated by CB(1) antagonists [SR141716 (rimonabant) and AM281], inhibitors of p38 and JNK-MAPKs or the antioxidant N-acetylcysteine. Rimonabant 95-103 cannabinoid receptor 1 Homo sapiens 76-81 20618416-3 2010 We evaluated whether the selective cannabinoid type 1 (CB1) receptor antagonists SR 141716 or AM 251 could modify induction of epileptiform activity produced by DHPG exposure. Rimonabant 81-90 cannabinoid receptor 1 Homo sapiens 55-58 20463657-3 2010 Superfusion of the cannabinoid receptor (CB1) agonist WIN55212-2 (WIN2) onto CeA neurons decreased evoked GABA(A) receptor-mediated inhibitory postsynaptic potentials (IPSPs) in a concentration-dependent manner, an effect prevented by the CB1 antagonists Rimonabant (SR141716, SR1) and AM251. Rimonabant 255-265 cannabinoid receptor 1 Homo sapiens 41-44 20463657-3 2010 Superfusion of the cannabinoid receptor (CB1) agonist WIN55212-2 (WIN2) onto CeA neurons decreased evoked GABA(A) receptor-mediated inhibitory postsynaptic potentials (IPSPs) in a concentration-dependent manner, an effect prevented by the CB1 antagonists Rimonabant (SR141716, SR1) and AM251. Rimonabant 267-275 cannabinoid receptor 1 Homo sapiens 41-44