[HTML][HTML] The therapeutic potential of second and third generation CB1R antagonists

R Cinar, MR Iyer, G Kunos - Pharmacology & therapeutics, 2020 - Elsevier
Endocannabinoids acting via CB 1 receptors (CB 1 R) play a critical role in regulating
energy homeostasis, which was the rationale for the pharmaceutical development of CB 1 R …

CB1 receptor antagonism: biological basis for metabolic effects

V Di Marzo - Drug discovery today, 2008 - Elsevier
The endocannabinoid system (ECS) is a complex physiologic system that affects metabolic
pathways. A dysregulated ECS has been demonstrated in animal models of obesity and the …

Pharmacotherapeutic targeting of the endocannabinoid signaling system: drugs for obesity and the metabolic syndrome

VK Vemuri, DR Janero, A Makriyannis - Physiology & behavior, 2008 - Elsevier
Endogenous signaling lipids (“endocannabinoids”) functionally related to Δ9-
tetrahydrocannabinol, the psychoactive ingredient of marijuana (Cannabis), are important …

Overcoming the psychiatric side effects of the cannabinoid CB1 receptor antagonists: current approaches for therapeutics development

T Nguyen, BF Thomas, Y Zhang - Current topics in medicinal …, 2019 - ingentaconnect.com
The Cannabinoid CB1 Receptor (CB1R) is involved in a variety of physiological pathways
and has long been considered a golden target for therapeutic manipulation. A large body of …

The current status and future perspectives of studies of cannabinoid receptor 1 antagonists as anti-obesity agents

HK Lee, EB Choi, CS Pak - Current topics in medicinal …, 2009 - ingentaconnect.com
Since the discovery of rimonabant (Acomplia: 1), a large effort has been directed at the
discovery of new, potent and selective CB1R antagonists that serve as anti obesity drugs. As …

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

C Silvestri, V Di Marzo - Expert opinion on investigational drugs, 2012 - Taylor & Francis
Introduction: Excessive abdominal obesity along with other risk factors results in the
metabolic syndrome, which can lead to heart disease, Type-2 diabetes, and death. The …

Human CB1 receptor isoforms, present in hepatocytes and β-cells, are involved in regulating metabolism

I González-Mariscal, SM Krzysik-Walker, ME Doyle… - Scientific reports, 2016 - nature.com
Therapeutics aimed at blocking the cannabinoid 1 (CB1) receptor for treatment of obesity
resulted in significant improvements in liver function, glucose uptake and pancreatic β-cell …

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

TM Fong, SB Heymsfield - International journal of obesity, 2009 - nature.com
Rimonabant and taranabant are two extensively studied cannabinoid-1 receptor (CB1R)
inverse agonists. Their effects on in vivo peripheral tissue metabolism are generally well …

CB1 antagonists for obesity—what lessons have we learned from rimonabant?

V Di Marzo, JP Després - Nature Reviews Endocrinology, 2009 - nature.com
When compared with other modifiable cardiovascular risk factors, such as hypertension,
dyslipidemia and smoking, obesity remains a surprisingly puzzling condition to prevent and …

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

JG Horswill, U Bali, S Shaaban, JF Keily… - British journal of …, 2007 - Wiley Online Library
Background and purpose: Rimonabant (AcompliaTM, SR141716A), a cannabinoid CB1
receptor inverse agonist, has recently been approved for the treatment of obesity. There are …