Cannabinoid-1 receptor (CB1R) blockers as medicines: beyond obesity and cardiometabolic disorders to substance abuse/drug addiction with CB1R neutral antagonists (Q37984087)

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scientific article published on 16 February 2012

Language	Label	Description	Also known as
English	Cannabinoid-1 receptor (CB1R) blockers as medicines: beyond obesity and cardiometabolic disorders to substance abuse/drug addiction with CB1R neutral antagonists	scientific article published on 16 February 2012

Statements

scholarly article

1 reference

Europe PubMed Central

26 August 2017

Cannabinoid-1 receptor (CB1R) blockers as medicines: beyond obesity and cardiometabolic disorders to substance abuse/drug addiction with CB1R neutral antagonists (English)

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Europe PubMed Central

26 August 2017

substance dependence

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cannabinoid receptor

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author name string

David R Janero

1

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Europe PubMed Central

26 August 2017

language of work or name

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publication date

16 February 2012

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Europe PubMed Central

26 August 2017

Expert Opinion on Emerging Drugs

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Europe PubMed Central

26 August 2017

17

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Europe PubMed Central

26 August 2017

1

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Europe PubMed Central

26 August 2017

17-29

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Europe PubMed Central

26 August 2017

Cannabinoid 1 G protein-coupled receptor (periphero-)neutral antagonists: emerging therapeutics for treating obesity-driven metabolic disease and reducing cardiovascular risk

1 reference

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The case for peripheral CB₁ receptor blockade in the treatment of visceral obesity and its cardiometabolic complications

1 reference

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21 January 2018

A new perspective of cannabinoid 1 receptor antagonists: approaches toward peripheral CB1R blockers without crossing the blood-brain barrier.

1 reference

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21 January 2018

Rimonabant redux and strategies to improve the future outlook of CB1 receptor neutral-antagonist/inverse-agonist therapies

1 reference

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21 January 2018

The pharmacology of the endocannabinoid system: functional and structural interactions with other neurotransmitter systems and their repercussions in behavioral addiction.

1 reference

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21 January 2018

The endocannabinoid system in brain reward processes

1 reference

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21 January 2018

The endocannabinoid system and nondrug rewarding behaviours

1 reference

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21 January 2018

Common cellular and molecular mechanisms in obesity and drug addiction

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21 January 2018

New horizons for therapeutics in drug and alcohol abuse

1 reference

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Risk of serious adverse cardiovascular events associated with varenicline: a systematic review and meta-analysis

1 reference

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Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery

1 reference

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21 January 2018

When simple agonism is not enough: emerging modalities of GPCR ligands.

1 reference

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Functional selectivity in CB(2) cannabinoid receptor signaling and regulation: implications for the therapeutic potential of CB(2) ligands.

1 reference

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Targeted modulators of the endogenous cannabinoid system: future medications to treat addiction disorders and obesity

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21 January 2018

Functionally selective cannabinoid receptor signalling: therapeutic implications and opportunities

1 reference

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21 January 2018

The neutral cannabinoid CB₁ receptor antagonist AM4113 regulates body weight through changes in energy intake in the rat.

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity

1 reference

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21 January 2018

Theme and variations on kinetics of GPCR activation/deactivation

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21 January 2018

How inverse can a neutral antagonist be? Strategic questions after the rimonabant issue

1 reference

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21 January 2018

Endocannabinoid tone versus constitutive activity of cannabinoid receptors

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Inverse agonism and neutral antagonism at cannabinoid CB1 receptors

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Inhibitory effects of SR141716A on G-protein activation in rat brain

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

The endocannabinoid system: its general strategy of action, tools for its pharmacological manipulation and potential therapeutic exploitation

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB₁ and CB₂

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Functional interactions between endogenous cannabinoid and opioid systems: focus on alcohol, genetics and drug-addicted behaviors.

1 reference

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21 January 2018

Functional interactions between stress and the endocannabinoid system: from synaptic signaling to behavioral output.

1 reference

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21 January 2018

Cannabinoid receptors in brain: pharmacogenetics, neuropharmacology, neurotoxicology, and potential therapeutic applications

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Characterization and distribution of binding sites for [3H]-SR 141716A, a selective brain (CB1) cannabinoid receptor antagonist, in rodent brain

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Dopaminergic modulation of endocannabinoid-mediated plasticity at GABAergic synapses in the prefrontal cortex

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Ligand-induced regulation and localization of cannabinoid CB1 and dopamine D2L receptor heterodimers

1 reference

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21 January 2018

Changes in endocannabinoid contents in the brain of rats chronically exposed to nicotine, ethanol or cocaine

1 reference

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21 January 2018

Chronic exposure to morphine, cocaine or ethanol in rats produced different effects in brain cannabinoid CB(1) receptor binding and mRNA levels

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Methamphetamine neurotoxicity increases brain expression and alters behavioral functions of CB₁ cannabinoid receptors.

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Human cannabinoid receptor 1: 5' exons, candidate regulatory regions, polymorphisms, haplotypes and association with polysubstance abuse

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Cannabinoid receptor 1 gene association with nicotine dependence

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Association of polymorphisms of the cannabinoid receptor (CNR1) and fatty acid amide hydrolase (FAAH) genes with heroin addiction: impact of long repeats of CNR1.

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

The endocannabinoid system, eating behavior and energy homeostasis: the end or a new beginning?

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

An evidence based review of acute and long-term effects of cannabis use on executive cognitive functions

1 reference

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21 January 2018

Cannabinoid agonist-induced sensitisation to morphine place preference in mice

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Cannabinoid agonists but not inhibitors of endogenous cannabinoid transport or metabolism enhance the reinforcing efficacy of heroin in rats

1 reference

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21 January 2018

Subchronic cannabinoid agonist (WIN 55,212-2) treatment during cocaine abstinence alters subsequent cocaine seeking behavior.

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Suppression of food intake and food-reinforced behavior produced by the novel CB1 receptor antagonist/inverse agonist AM 1387.

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

AM 251 differentially effects food-maintained responding depending on food palatability.

1 reference

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A selective cannabinoid-1 receptor antagonist, PF-95453, reduces body weight and body fat to a greater extent than pair-fed controls in obese monkeys

1 reference

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21 January 2018

Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents

1 reference

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21 January 2018

Cannabinoid CB1 receptor antagonist AM251 inhibits cocaine-primed relapse in rats: role of glutamate in the nucleus accumbens.

1 reference

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21 January 2018

Effects of CB1 receptor antagonist within the nucleus accumbens on the acquisition and expression of morphine-induced conditioned place preference in morphine-sensitized rats.

1 reference

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21 January 2018

SLV330, a cannabinoid CB(1) receptor antagonist, attenuates ethanol and nicotine seeking and improves inhibitory response control in rats.

1 reference

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Acute blockade of CB1 receptor leads to reinstatement of MDMA-induced conditioned place preference.

1 reference

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The discovery of taranabant, a selective cannabinoid-1 receptor inverse agonist for the treatment of obesity

1 reference

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Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists

1 reference

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Effects of adolescent nicotine and SR 147778 (Surinabant) administration on food intake, somatic growth and metabolic parameters in rats.

1 reference

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21 January 2018

CB1 receptor blockade and its impact on cardiometabolic risk factors: overview of the RIO programme with rimonabant

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Pleiotropic effects of rimonabant: clinical implications

1 reference

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21 January 2018

A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

An overview of the metabolic effects of rimonabant in randomized controlled trials: potential for other cannabinoid 1 receptor blockers in obesity

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https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Efficacy and safety of CP-945,598, a selective cannabinoid CB1 receptor antagonist, on weight loss and maintenance

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Cannabinoid receptor 1 blocker rimonabant (SR 141716) for treatment of alcohol dependence: results from a placebo-controlled, double-blind trial

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Randomized, controlled, double-blind trial of taranabant for smoking cessation

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21 January 2018

A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

A clinical trial assessing the safety and efficacy of the CB1R inverse agonist taranabant in obese and overweight patients: low-dose study

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

End of the line for cannabinoid receptor 1 as an anti-obesity target?

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action and unanswered questions

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https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Central and peripheral consequences of the chronic blockade of CB1 cannabinoid receptor with rimonabant or taranabant

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https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Central side-effects of therapies based on CB1 cannabinoid receptor agonists and antagonists: focus on anxiety and depression

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21 January 2018

Blockade of the cannabinoid CB1 receptor and alcohol dependence: preclinical evidence and preliminary clinical data

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21 January 2018

The future of endocannabinoid-oriented clinical research after CB1 antagonists.

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21 January 2018

Participation of the cannabinoid system in the regulation of emotional-like behaviour

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https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Impairments in endocannabinoid signaling and depressive illness

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https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Cannabinoid effects on anxiety-related behaviours and hypothalamic neurotransmitters

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https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Effects of the cannabinoid CB1 receptor antagonist rimonabant in models of emotional reactivity in rodents

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21 January 2018

Modulation of anxiety by acute blockade and genetic deletion of the CB(1) cannabinoid receptor in mice together with biogenic amine changes in the forebrain

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21 January 2018

Presence of conspecifics and their odor-impregnated objects reverse stress-decreased neurogenesis in mouse dentate gyrus

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21 January 2018

Genes differentially expressed in CB1 knockout mice: involvement in the depressive-like phenotype.

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21 January 2018

Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier

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21 January 2018

Rational design of a novel peripherally-restricted, orally active CB(1) cannabinoid antagonist containing a 2,3-diarylpyrrole motif

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21 January 2018

Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Energy balance regulation by endocannabinoids at central and peripheral levels

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https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Blood-brain barrier: structural components and function under physiologic and pathologic conditions

1 reference

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21 January 2018

The acyclic CB1R inverse agonist taranabant mediates weight loss by increasing energy expenditure and decreasing caloric intake

1 reference

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21 January 2018

Alterations in blood-brain barrier function by morphine and methamphetamine.

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https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Alteration of blood-brain barrier function by methamphetamine and cocaine

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21 January 2018

Alterations in blood-brain barrier function and brain pathology by morphine in the rat. Neuroprotective effects of antioxidant H-290/51.

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https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Defaecation, intestinal fluid accumulation and motility in rodents: implications of cannabinoid CB1 receptors

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21 January 2018

Cannabinoid receptor agonism inhibits transient lower esophageal sphincter relaxations and reflux in dogs.

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21 January 2018

Differential effects of CB(1) neutral antagonists and inverse agonists on gastrointestinal motility in mice

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21 January 2018

Cannabinoids and the gut: new developments and emerging concepts

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21 January 2018

A neutral CB1 receptor antagonist reduces weight gain in rat.

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Cannabinoid CB1 receptor inverse agonists and neutral antagonists: effects on food intake, food-reinforced behavior and food aversions

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats

1 reference

https://api.crossref.org/works/10.1517%2F14728214.2012.660916

21 January 2018

Novel thioamide derivatives as neutral CB1 receptor antagonists

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21 January 2018

Biphasic suppression of appetite by cannabinoid CB1 receptor antagonists with distinct functional activities.

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21 January 2018

The endocannabinoid system in the processing of anxiety and fear and how CB1 receptors may modulate fear extinction

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21 January 2018

Endocannabinoid-mediated modulation of stress responses: physiological and pathophysiological significance

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21 January 2018

Endocannabinoids and stress

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21 January 2018

Obesity: genes, brain, gut, and environment

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21 January 2018

Leptin-regulated endocannabinoids are involved in maintaining food intake

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21 January 2018

Behavioral pharmacology of cannabinoids with a focus on preclinical models for studying reinforcing and dependence-producing properties

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21 January 2018

Animal models of cannabinoid reward

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Zebrafish models to study drug abuse-related phenotypes

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21 January 2018

Animal models of neuropsychiatric disorders.

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21 January 2018

PSNCBAM-1, a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats

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21 January 2018

Cannabinoid CB1 receptor-interacting proteins: novel targets for central nervous system drug discovery?

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21 January 2018

Brain cannabinoid CB₂ receptors modulate cocaine's actions in mice

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21 January 2018

CB1 receptor-independent actions of SR141716 on G-protein signaling: coapplication with the mu-opioid agonist Tyr-D-Ala-Gly-(NMe)Phe-Gly-ol unmasks novel, pertussis toxin-insensitive opioid signaling in mu-opioid receptor-Chinese hamster ovary cells

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Retrospective. Ralph M. Steinman (1943-2011).

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21 January 2018

Identifiers

10.1517/14728214.2012.660916

1 reference

Europe PubMed Central

26 August 2017

1 reference

Europe PubMed Central

26 August 2017

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