(Q38025166)

English

Second generation CB1 receptor blockers and other inhibitors of peripheral endocannabinoid overactivity and the rationale of their use against metabolic disorders

scientific article published on 11 July 2012

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scholarly article

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

Second generation CB1 receptor blockers and other inhibitors of peripheral endocannabinoid overactivity and the rationale of their use against metabolic disorders (English)

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

endocannabinoids

0 references

Vincenzo Di Marzo

2

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

Cristoforo Silvestri

object named as

Cristoforo Silvestri

1

0 references

language of work or name

0 references

publication date

11 July 2012

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

Expert Opinion on Investigational Drugs

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

21

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

9

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

1309-1322

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

Prevalence and trends in obesity among US adults, 1999-2008

1 reference

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21 January 2018

The medical complications of obesity

1 reference

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21 January 2018

Discovery of endocannabinoids and some random thoughts on their possible roles in neuroprotection and aggression

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Endocannabinoids: synthesis and degradation

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

The endocannabinoid system: a general view and latest additions

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Endocannabinoids and the regulation of their levels in health and disease

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Endogenous cannabinoids in the brain and peripheral tissues: regulation of their levels and control of food intake.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Cannabinoids and appetite: food craving and food pleasure

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Endocannabinoid levels in rat limbic forebrain and hypothalamus in relation to fasting, feeding and satiation: stimulation of eating by 2-arachidonoyl glycerol

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Leptin-regulated endocannabinoids are involved in maintaining food intake

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

CB1 cannabinoid receptor-mediated modulation of food intake in mice

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

The anti-obesity effect of rimonabant is associated with an improved serum lipid profile

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Anti-obesity effect of SR141716, a CB1 receptor antagonist, in diet-induced obese mice

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

The endogenous cannabinoid system affects energy balance via central orexigenic drive and peripheral lipogenesis

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

CB1 cannabinoid receptor knockout in mice leads to leanness, resistance to diet-induced obesity and enhanced leptin sensitivity

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Endocannabinoid control of food intake and energy balance

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

The cannabinoid CB1 receptor antagonist SR141716 increases Acrp30 mRNA expression in adipose tissue of obese fa/fa rats and in cultured adipocyte cells

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Regulation, function, and dysregulation of endocannabinoids in models of adipose and beta-pancreatic cells and in obesity and hyperglycemia

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Dysregulation of peripheral endocannabinoid levels in hyperglycemia and obesity: Effect of high fat diets

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

The emerging role of the endocannabinoid system in endocrine regulation and energy balance

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

CB1 antagonism exerts specific molecular effects on visceral and subcutaneous fat and reverses liver steatosis in diet-induced obese mice

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

CB(1) signaling in forebrain and sympathetic neurons is a key determinant of endocannabinoid actions on energy balance

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Blood levels of the endocannabinoid anandamide are increased in anorexia nervosa and in binge-eating disorder, but not in bulimia nervosa

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Activation of the peripheral endocannabinoid system in human obesity

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Dysregulation of the peripheral and adipose tissue endocannabinoid system in human abdominal obesity

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Cannabinoid CB1 receptor expression in relation to visceral adipose depots, endocannabinoid levels, microvascular damage, and the presence of the Cnr1 A3813G variant in humans.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Adipose tissue dysfunction in obesity, diabetes, and vascular diseases

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Abdominal obesity and metabolic syndrome

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Peripheral effects of the endocannabinoid system in energy homeostasis: adipose tissue, liver and skeletal muscle

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Hepatic CB1 receptor is required for development of diet-induced steatosis, dyslipidemia, and insulin and leptin resistance in mice

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Overactive endocannabinoid signaling impairs apolipoprotein E-mediated clearance of triglyceride-rich lipoproteins

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Effect of rimonabant on the high-triglyceride/ low-HDL-cholesterol dyslipidemia, intraabdominal adiposity, and liver fat: the ADAGIO-Lipids trial

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Changes in plasma endocannabinoid levels in viscerally obese men following a 1 year lifestyle modification programme and waist circumference reduction: associations with changes in metabolic risk factors

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Paracrine activation of hepatic CB1 receptors by stellate cell-derived endocannabinoids mediates alcoholic fatty liver

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Cannabinoid type 1 receptor blockade promotes mitochondrial biogenesis through endothelial nitric oxide synthase expression in white adipocytes.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Effects of the cannabinoid CB1 antagonist rimonabant on hepatic mitochondrial function in rats fed a high-fat diet

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Cannabinoids and ghrelin have both central and peripheral metabolic and cardiac effects via AMP-activated protein kinase.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Cannabinoid receptor stimulation impairs mitochondrial biogenesis in mouse white adipose tissue, muscle, and liver: the role of eNOS, p38 MAPK, and AMPK pathways.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Pathogenesis of insulin resistance in skeletal muscle

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Peripheral, but not central, CB1 antagonism provides food intake-independent metabolic benefits in diet-induced obese rats

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Cannabinoid receptor signaling directly inhibits thermogenesis and alters expression of adiponectin and visfatin

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

The cannabinoid CB1 receptor antagonist rimonabant (SR141716) inhibits cell proliferation and increases markers of adipocyte maturation in cultured mouse 3T3 F442A preadipocytes

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Effects of in vitro antagonism of endocannabinoid-1 receptors on the glucose transport system in normal and insulin-resistant rat skeletal muscle

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

The cannabinoid CB1 receptor antagonist rimonabant stimulates 2-deoxyglucose uptake in skeletal muscle cells by regulating the expression of phosphatidylinositol-3-kinase

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Regulation of MAP kinase-directed mitogenic and protein kinase B-mediated signaling by cannabinoid receptor type 1 in skeletal muscle cells

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Inverse agonism or neutral antagonism at G-protein coupled receptors: a medicinal chemistry challenge worth pursuing?

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Inverse agonism and neutral antagonism at cannabinoid CB1 receptors

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Oral bioavailability of the novel cannabinoid CB1 antagonist AM6527: effects on food-reinforced behavior and comparisons with AM4113.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

A neutral CB1 receptor antagonist reduces weight gain in rat.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

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%2F13543784.2012.704019

21 January 2018

The CB1 inverse agonist AM251, but not the CB1 antagonist AM4113, enhances retention of contextual fear conditioning in rats

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Potential anxiogenic effects of cannabinoid CB1 receptor antagonists/inverse agonists in rats: comparisons between AM4113, AM251, and the benzodiazepine inverse agonist FG-7142.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

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%2F13543784.2012.704019

21 January 2018

Inverse agonism of cannabinoid CB1 receptors potentiates LiCl‐induced nausea in the conditioned gaping model in rats

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Novel thioamide derivatives as neutral CB1 receptor antagonists

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Endocannabinoids, feeding and suckling--from our perspective

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Molecular interaction of the antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1- (2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide with the CB1 cannabinoid receptor

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

The cannabinoid 1-receptor silent antagonist O-2050 attenuates preference for high-fat diet and activated astrocytes in mice

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Delta(9)-tetrahydrocannabinol enhances an increase of plasma corticosterone levels induced by forced swim-stress.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB(1) receptor antagonist.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Ligand Binding Sensitivity of the Extracellular Loop Two of the Cannabinoid Receptor 1.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Suppression of feeding, drinking, and locomotion by a putative cannabinoid receptor 'silent antagonist'.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Evidence for both inverse agonism at the cannabinoid CB1 receptor and the lack of an endogenous cannabinoid tone in the rat and guinea-pig isolated ileum myenteric plexus-longitudinal muscle preparation

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Central versus peripheral antagonism of cannabinoid CB1 receptor in obesity: effects of LH-21, a peripherally acting neutral cannabinoid receptor antagonist, in Zucker rats.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Antiobesity effects of the novel in vivo neutral cannabinoid receptor antagonist 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole--LH 21.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Anti-obesity efficacy of LH-21, a cannabinoid CB(1) receptor antagonist with poor brain penetration, in diet-induced obese rats

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Pharmacological evaluation of LH-21, a newly discovered molecule that binds to cannabinoid CB1 receptor

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Endocannabinoid signal in the gut controls dietary fat intake.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Peripherally acting CB1-receptor antagonist: the relative importance of central and peripheral CB1 receptors in adiposity control

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

A novel peripherally restricted cannabinoid receptor antagonist, AM6545, reduces food intake and body weight, but does not cause malaise, in rodents

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Central mediation and differential blockade by cannabinergics of the discriminative stimulus effects of the cannabinoid CB1 receptor antagonist rimonabant in rats

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

The novel cannabinoid CB1 antagonist AM6545 suppresses food intake and food-reinforced behavior

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

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%2F13543784.2012.704019

21 January 2018

Towards rational design of cannabinoid receptor 1 (CB1) antagonists for peripheral selectivity

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Design and synthesis of cannabinoid receptor 1 antagonists for peripheral selectivity

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Sensory circumventricular organs: central roles in integrated autonomic regulation

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Delta9-tetrahydrocannabinol selectively acts on CB1 receptors in specific regions of dorsal vagal complex to inhibit emesis in ferrets

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Cannabinoid1 receptor in the dorsal vagal complex modulates lower oesophageal sphincter relaxation in ferrets

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Leptin regulation of neuroendocrine systems

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Deficiency of CB2 cannabinoid receptor in mice improves insulin sensitivity but increases food intake and obesity with age.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Cannabinoid CB2 receptor potentiates obesity-associated inflammation, insulin resistance and hepatic steatosis

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Synthesis and pharmacological activity of a potent inhibitor of the biosynthesis of the endocannabinoid 2-arachidonoylglycerol

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

2-arachidonoylglycerol signaling in forebrain regulates systemic energy metabolism

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Development of the first potent and specific inhibitors of endocannabinoid biosynthesis

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Incorporation of EPA and DHA into plasma phospholipids in response to different omega-3 fatty acid formulations--a comparative bioavailability study of fish oil vs. krill oil.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Lipids, membrane receptors, and enzymes: effects of dietary fatty acids

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Effect of polyunsaturated fatty acids on endocannabinoid and N-acyl-ethanolamine levels in mouse adipocytes.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Dietary linoleic acid elevates endogenous 2-AG and anandamide and induces obesity

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Krill oil significantly decreases 2-arachidonoylglycerol plasma levels in obese subjects

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Effect of dietary krill oil supplementation on the endocannabinoidome of metabolically relevant tissues from high-fat-fed mice.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Endocannabinoids may mediate the ability of (n-3) fatty acids to reduce ectopic fat and inflammatory mediators in obese Zucker rats.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Hepatic cannabinoid receptor-1 mediates diet-induced insulin resistance via inhibition of insulin signaling and clearance in mice

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Moderate doses of EPA and DHA from re-esterified triacylglycerols but not from ethyl-esters lower fasting serum triacylglycerols in statin-treated dyslipidemic subjects: Results from a six month randomized controlled trial.

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Leptin controls adipose tissue lipogenesis via central, STAT3-independent mechanisms

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Central endocannabinoid signaling regulates hepatic glucose production and systemic lipolysis

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2012.704019

21 January 2018

Identifiers

10.1517/13543784.2012.704019

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

27 August 2017

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