RIMONABANT/ACOMPLIA/SR141716/ SR1 – a CB1 & CB2 antagonist


SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. (abst – 1994)                                           http://www.ncbi.nlm.nih.gov/pubmed/8070571


The CB1 cannabinoid receptor antagonist SR 141716A affects A9 dopamine neuronal activity in the rat.                                               (abst – 1995)        http://www.ncbi.nlm.nih.gov/pubmed/7488739


Cannabinoids enhance human B-cell growth at low nanomolar concentrations. (abst – 1995)                                            http://www.ncbi.nlm.nih.gov/pubmed/7544292


Biochemical and pharmacological characterisation of SR141716A, the first potent and selective brain cannabinoid receptor antagonist.                                                                    (abst – 1995)  http://www.ncbi.nlm.nih.gov/pubmed/7776817


Cannabinoid precipitated withdrawal by the selective cannabinoid receptor antagonist, SR 141716A.     (abst – 1995)                                  http://www.ncbi.nlm.nih.gov/pubmed/7498260


Activation of peripheral CB1 cannabinoid receptors in haemorrhagic shock. (abst – 1997)                                             http://www.ncbi.nlm.nih.gov/pubmed/9394002


SR 141716, a CB1 cannabinoid receptor antagonist, selectively reduces sweet food intake in marmoset. (abst – 1998)  http://www.ncbi.nlm.nih.gov/sites/entrez/10065938?dopt=Abstract&holding=f1000,f1000m,isrctn


Anandamide induces overeating: mediation by central cannabinoid (CB1) receptors (abst – 1999)                                        http://link.springer.com/article/10.1007%2Fs002130050953


The cannabinoid CB1 receptor antagonist SR 141716A reverses the antiemetic and motor depressant actions of WIN 55, 212-2                                                           (abst – 2001)  http://www.ncbi.nlm.nih.gov/pubmed/11120402


Cannabinoid receptor type 1 modulates excitatory and inhibitory neurotransmission in mouse colon         (full – 2003)



Overeating, Alcohol and Sucrose Consumption Decrease in Cb1 Receptor Deleted Mice. (abst – 2004)                                            http://www.ncbi.nlm.nih.gov/pubmed/12770700


Ethanol Induces Higher Bec in Cb1 Cannabinoid Receptor Knockout Mice While Decreasing Ethanol Preference.                                                                 (full – 2005)  http://alcalc.oxfordjournals.org/content/40/1/54.long


Activation of the Peripheral Endocannabinoid System in Human Obesity            (full – 2005)



Enhancing Cannabinoid Neurotransmission Augments the Extinction of Conditioned Fear (full – 2005)                                         http://www.nature.com/npp/journal/v30/n3/full/1300655a.html


The analgesic activity of paracetamol is prevented by the blockade of cannabinoid CB1 receptors            (abst – 2005)                    http://www.sciencedirect.com/science/article/pii/S0014299905013178


The Cannabinoid Cb1 Receptor Antagonist Rimonabant Attenuates the Hypotensive Effect of Smoked Marijuana in Male Smokers.                                                             (full – 2006)  http://www.ahjonline.com/article/S0002-8703%2805%2901013-6/fulltext


Weight Control in Individuals With Diabetes                (full – 2006)  http://care.diabetesjournals.org/content/29/12/2749.full?maxtoshow=&hits=80&RESULTFORMAT=&full  text=cannabis&searchid=1&FIRSTINDEX=2000&resourcetype=HWCIT


Anxiolytic-like properties of the anandamide transport inhibitor AM404.              (full – 2006)



Lack of tolerance to the suppressing effect of rimonabant on chocolate intake in rats. (abst – 2006)                                      http://www.ncbi.nlm.nih.gov/pubmed/16491428


Acomplia may be dangerous for women of reproductive age             (news – 2006)



Obesity – Acomplia: loss of a few kilos, many questions                 (news – 2006)



Big Pharma’s Strange Holy Grail: Cannabis Without Euphoria?              (news – 2006)



Cross-sensitization and cross-tolerance between exogenous cannabinoid antinociception and endocannabinoid-mediated stress-induced analgesia                                                    (full – 2007)  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2771679/?tool=pubmed


Single and multiple doses of rimonabant antagonize acute effects of smoked cannabis in male cannabis users.     (full – 2007)  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2689519/?tool=pubmed


Rimonabant (SR141716) exerts anti-proliferative and immunomodulatory effects in human peripheral blood mononuclear cells                                                      (full – 2007)  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2267266/?tool=pmcentrez


Cannabinoid CB1 receptors in the paraventricular nucleus and central control of penile erection: immunocytochemistry, autoradiography and behavioral studies                             (abst – 2007)  http://www.ncbi.nlm.nih.gov/pubmed/17507169


Rimonabant: safety issues                (news – 2007)



European watchdog warns about dangers of Acomplia              (news – 2007)



Three Long-Term Diet Pills Show Poor Performance, Study Suggests              (news – 2007)



FDA Advisory Panel Rejects Obesity Drug                (news – 2007)  http://firstwatch.jwatch.org/cgi/content/full/2007/615/2?maxtoshow=&hits=80&RESULTFORMAT=&full   text=cannabinoid&searchid=1&FIRSTINDEX=2800&resourcetype=HWCIT


Differential response to a selective cannabinoid receptor antagonist (SR141716: rimonabant) in female mice from lines selectively bred for high voluntary wheel-running behaviour.  (abst – 2008)                                http://www.ncbi.nlm.nih.gov/pubmed/19020416


Caution Urged With New Anti-Obesity Drug In Kids               (news – 2008)



The psychiatric side-effects of rimonabant.                (full – 2009)  http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1516-  44462009000200012&lng=en&nrm=iso&tlng=en


Effects of the cannabinoid CB1 receptor antagonist rimonabant on distinct measures of impulsive behavior in rats.                                                         (full – 2009)  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1915592/?tool=pubmed


The endocanabinnoid system and diabetes – critical analyses of studies conducted with rimonabant         (full – 2009)  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2770455/?tool=pmcentrez


Cannabinoids for clinicians: the rise and fall of the cannabinoid antagonists (full – 2009)  http://www.eje-




Evaluation of Prevalent Phytocannabinoids in the Acetic Acid Model of Visceral Nociception    (full – 2009)  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2765124/?tool=pubmed


Systematic review and meta-analysis on the adverse events of rimonabant treatment: Considerations for its potential use in hepatology                                                                 (full – 2009)  http://www.biomedcentral.com/1471-230X/9/75


Impairments in Endocannabinoid Signaling and Depressive Illness              (full – 2009)



Effects of cannabinoid drugs on the reinforcing properties of food in gestationally undernourished rats.  (abst – 2009)                                      http://www.ncbi.nlm.nih.gov/pubmed/19602424


Endocannabinoids and cardiovascular prevention: real progress?               (abst – 2009)



International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2                                                               (full – 2010)  http://pharmrev.aspetjournals.org/content/62/4/588.full.pdf+html


Therapeutical use of the cannabinoids in psychiatry                 (full – 2010)  http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1516-  44462010000500009&lng=en&nrm=iso&tlng=en


GPR55 ligands promote receptor coupling to multiple signalling pathways. (full – 2010)                                     http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2931561/?tool=pubmed


Rehashing endocannabinoid antagonists: can we selectively target the periphery to safely treat obesity and type 2 diabetes?                                                      (full – 2010)  http://www.jci.org/articles/view/44099?search[abstract_text]=&search[article_text]=cannabinoid&search[a   uthors_text]=&search[fpage]=&search[title_text]=&search[volume]=


Perspectives of CB1 Antagonist in Treatment of Obesity: Experience of RIO-Asia (full – 2010)                                    http://www.hindawi.com/journals/jobes/2011/957268/


Energetic Metabolism and Human Sperm Motility: Impact of CB1 Receptor Activation (full – 2010)                                    http://endo.endojournals.org/content/151/12/5882.full


The Effects of Rimonabant on Brown Adipose Tissue in Rat: Implications for Energy Expenditure          (full – 2010)                       http://www.nature.com/oby/journal/v17/n2/full/oby2008509a.html


The Endocannabinoid System Tonically Regulates Inhibitory Transmission and Depresses the Effect of Ethanol in Central Amygdala                                                                       (abst – 2010)  http://www.nature.com/npp/journal/v35/n9/abs/npp201070a.html


Rimonabant-induced Delta9-tetrahydrocannabinol withdrawal in rhesus monkeys: discriminative stimulus effects and other withdrawal signs.                                                                 (abst – 2010)  http://www.unboundmedicine.com/medline/ebm/record/20375197/abstract/Rimonabant_induced_Delta9_te trahydrocannabinol_withdrawal_in_rhesus_monkeys:_discriminative_stimulus_effects_and_other_withdra wal_signs_


Anxiety-like effects of SR141716-precipitated delta9-tetrahydrocannabinol withdrawal in mice in the elevated plus-maze.                                                   (abst – 2010)  http://www.unboundmedicine.com/medline/ebm/record/20363293/abstract/Anxiety_like_effects_of_SR141  716_precipitated_delta9_tetrahydrocannabinol_withdrawal_in_mice_in_the_elevated_plus_maze_


Reduced neural response to reward following 7 days treatment with the cannabinoid CB1 antagonist rimonabant in healthy volunteers                                                         (abst – 2010)  http://journals.cambridge.org/action/displayAbstract?fromPage=online&aid=7873271&fulltextType=RA&f   ileId=S1461145710000453


Suicides in other trials led to early termination of trial into effects of weight loss drug rimonabant on cardiovascular outcomes (CRESCENDO study)                                                                 (news – 2010)  http://www.eurekalert.org/pub_releases/2010-08/l-sio081110.php


Risk of suicide spurs rimonabant trial to end.               (news – 2010)



Endocannabinoid system protects against cryptogenic seizures.              (full – 2011)



The role of the cannabinoid system in the pathogenesis and treatment of alcohol dependence       (link to PDF – 2011)  http://www.doaj.org/doaj?func=abstract&id=825351&q1=cannabinoid&f1=all&b1=and&q2=&f2=all&rec No=22&uiLanguage=en


Psychiatric adverse effects of rimonobant in adults with Prader Willi syndrome. (abst – 2011)                                    http://www.ncbi.nlm.nih.gov/pubmed/20965292


Bioactivation Pathways of the Cannabinoid Receptor 1 Antagonist Rimonabant (abst – 2011)



Effects of Chronic Oral Rimonabant Administration on Energy Budgets of Diet-Induced Obese C57BL/6 Mice.                                                 (abst – 2011)     http://www.ncbi.nlm.nih.gov/pubmed/22173576


The identification of rimonabant polymorphs, sibutramine and analogues of both in counterfeit Acomplia bought on the internet.                                                                  (abst – 2011)  http://www.ncbi.nlm.nih.gov/pubmed/20828968


Pro-epileptic effects of the cannabinoid receptor antagonist SR141716 in a model of audiogenic epilepsy.                                             (abst – 2011)      http://www.ncbi.nlm.nih.gov/pubmed/21733658


Pharmacological activation/inhibition of the cannabinoid system affects alcohol withdrawal-induced neuronal hypersensitivity to excitotoxic insults.                                                              (abst – 2011)  http://www.ncbi.nlm.nih.gov/pubmed/21886913


Antagonist-elicited cannabis withdrawal in humans.               (abst – 2011)



Intracellular Cannabinoid Type 1 (CB1) Receptors Are Activated by Anandamide (abst – 2011)



Effects of the cannabinoid antagonist SR 141716 on sexual and motor behavior in receptive female rats. (abst – 2011)                                        http://www.ncbi.nlm.nih.gov/pubmed/21848907


CB(1) -independent mechanisms of Δ(9) -THCV, AM251 and SR141716 (rimonabant). (abst – 2011)                                      http://www.ncbi.nlm.nih.gov/pubmed/21740450


CB1 receptors mediate rimonabant-induced pruritic responses in mice: investigation of locus of action.   (abst – 2011)  http://www.unboundmedicine.com/medline/ebm/record/21340468/abstract/CB1_receptors_mediate_rimon abant_induced_pruritic_responses_in_mice:_investigation_of_locus_of_action_


Chronic Δ⁹-tetrahydrocannabinol treatment in rhesus monkeys: differential tolerance and

cross-tolerance among cannabinoids.        (abst – 2011)

http://www.unboundmedicine.com/medline/ebm/record/21091643/abstract/Chronic_%CE%94%E2%81%B 9_tetrahydrocannabinol_treatment_in_rhesus_monkeys:_differential_tolerance_and_cross_tolerance_amon g_cannabinoids_


CB1 cannabinoid receptor mediates glucocorticoid effects on hormone secretion induced by volume and osmotic changes.                                                         (abst – 2011)  http://www.ncbi.nlm.nih.gov/pubmed/22211674


Fatty acid amide hydrolase blockade attenuates the development of collagen-induced arthritis and related thermal hyperalgesia in mice.                                                              (abst – 2011)  http://www.ncbi.nlm.nih.gov/pubmed/21740924


Naloxone and rimonabant reduce the reinforcing properties of exercise in rats. (abst – 2011)                                     http://www.ncbi.nlm.nih.gov/pubmed/21707193


Smoking marijuana not linked to obesity: study               (news – 2011)



Part of placebo effect ascribed to cannabinoids                (news – 2011)



To Be or Not To Be—Obese                (full – 2012)



Relationships between glucose, energy intake and dietary composition in obese adults with type 2 diabetes receiving the cannabinoid 1 (CB1) receptor antagonist, rimonabant (full – 2012)                                   http://www.nutritionj.com/content/11/1/50


GPR18 in microglia: implications for the CNS and endocannabinoid system signaling (full – 2012)                                   http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2012.02019.x/full


Angiotensin II induces vascular endocannabinoid release, which attenuates its vasoconstrictor effect via CB1 cannabinoid receptors.                                                                  (full – 2012)  http://www.jbc.org/content/early/2012/07/11/jbc.M112.346296.full.pdf+html


The role of CB2 receptor ligands in human eosinophil function                (full – 2012)



The cannabinoid receptor CB1 modulates the signaling properties of the lysophosphatidylinositol receptor GPR55.                                                                                     (full – 2012)  http://www.jbc.org/content/early/2012/11/16/jbc.M112.364109.long


The inverse agonist effect of rimonabant on G protein activation is not mediated by the cannabinoid CB1 receptor: Evidence from postmortem human brain. (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/22093909


Rimonabant reduces the essential value of food in the genetically obese Zucker rat: An exponential demand analysis.                                              (abst – 2012)      http://www.ncbi.nlm.nih.gov/pubmed/22019829


Extinction learning of rewards in the rat: is there a role for CB1 receptors? (abst – 2012)                                     http://www.ncbi.nlm.nih.gov/pubmed/21519986


Cannabinoids ameliorate disease progression in a model of multiple sclerosis in mice, acting preferentially through CB(1) receptor-mediated anti-inflammatory effects. (abst – 2012)   http://www.ncbi.nlm.nih.gov/pubmed/22342378


Effects of amphetamine on dopamine release in the rat nucleus accumbens shell region depend on cannabinoid CB1 receptor activation.                                                              (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/22426202


Rimonabant eliminates responsiveness to workload changes in a time-constrained food- reinforced progressive ratio procedure in rats.                                                               (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/22425597


Anti-obesity effects of the combined administration of CB1 receptor antagonist rimonabant and melanin-concentrating hormone antagonist SNAP-94847 in diet-inudced obese mice.         (abst – 2012)                                 http://www.ncbi.nlm.nih.gov/pubmed/22473329


Photoperiodic Changes in Endocannabinoid Levels and Energetic Responses to Altered Signalling at CB1 Receptors in Siberian Hamsters                                               (abst – 2012)  http://onlinelibrary.wiley.com/doi/10.1111/j.1365-2826.2012.02312.x/abstract


Hypothalamic CB1 Cannabinoid Receptors Regulate Energy Balance in Mice (abst – 2012)



Induction of Glucose Intolerance by Acute Administration of Rimonabant. (abst – 2012)                                       http://www.ncbi.nlm.nih.gov/pubmed/22678147


Antipsychotic Profile of Cannabidiol and Rimonabant in an Animal Model of Emotional Context Processing in Schizophrenia.                                                   (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/22716146


Sex Differences in Cannabinoid 1 vs. Cannabinoid 2 Receptor-Selective Antagonism of Antinociception Produced by Δ9-Tetrahydrocannabinol and CP55,940 in the Rat

(abst – 2012)



Cannabinoid receptor 1 in the vagus nerve is dispensable for body weight homeostasis but required for normal gastrointestinal motility.                                                          (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/22836266


Structural analogs of pyrazole and sulfonamide cannabinoids: Effects on acute food intake in mice.        (abst – 2012)                              http://www.ncbi.nlm.nih.gov/pubmed/22975289


Probing the Interaction of SR141716A with the CB1 Receptor.             (abst – 2012)



Anandamide regulates the expression of GnRH1, GnRH2, and GnRH-Rs in frog testis (abst – 2012)                                        http://www.ncbi.nlm.nih.gov/pubmed/22669247


Cannabinoid CB(1) receptor in the modulation of stress coping behaviour in mice: the role of serotonin and different forebrain neuronal subpopulations.                                                   (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/23000076


Expression of fatty acid amide hydrolase (FAAH) in human, mouse, and rat urinary bladder and effects of FAAH inhibition on bladder function in awake rats.                                                           (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/21930339


Bioactivation of the Cannabinoid Receptor Antagonist Rimonabant to a Cytotoxic Iminium Ion Metabolite.                                                       (abst – 2012)         http://www.ncbi.nlm.nih.gov/pubmed/23234359


The effects of fasting duration on gastric emptying in man, an exploration of the role of the endocannabinoid system and inter-individual responsiveness                                                   (abst – 2012)  http://onlinelibrary.wiley.com/doi/10.1111/j.1365-2982.2012.01954.x/abstract


Pharmacological modulation of the endocannabinoid signalling alters binge-type eating behaviour in female rats                                                        (abst – 2012)  http://onlinelibrary.wiley.com/doi/10.1111/bph.12014/abstract


Reports of the death of CB1 antagonists have been greatly exaggerated: recent preclinical findings predict improved safety in the treatment of obesity.                                         (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/22743603


Fatty acid flux and oxidation are increased by rimonabant in obese women. (abst – 2012)                                      http://www.ncbi.nlm.nih.gov/pubmed/22445512


How Weed Can Protect Us From Cancer and Alzheimer’s               (book excerpt – 2012)



Cannnabinoids, Breast Milk, and Development                  (news – 2012)



WIN55, 212-2 promotes differentiation of oligodendrocyte precursor cells and improve remyelination through regulation of the phosphorylation level of the ERK 1/2 via cannabinoid receptor 1 after stroke-induced demyelination.                                                                                            (abst – 2013)  http://www.ncbi.nlm.nih.gov/pubmed/23148948


Cannabis and Δ(9)-tetrahydrocannabinol (THC) for weight loss?                         (abst – 2013)



Stimulatory and Inhibitory Roles of Brain 2-Arachidonoylglycerol in Bombesin-Induced Central Activation of Adrenomedullary Outflow in Rats.                                                           (abst – 2013)  http://www.ncbi.nlm.nih.gov/pubmed/23386378

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