Merck & Co Inc is developing the cannabinoid receptor type 1 inverse agonist taranabant for the potential treatment of obesity and nicotine dependence. By October 2006, the drug had entered phase III trials for obesity, and by May 2008, a phase II study of taranabant as an aid to smoking cessation in chronic cigarette smokers had been completed.
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Basic Science and Pathogenesis.
Alzheimers Dement
December 2024
University of Florida College of Medicine, Gainesville, FL, USA.
Background: The presence of Tau pathology is strongly associated with the clinical symptoms and cognitive decline found in Alzheimer's disease (AD), suggesting that targeting pathological tau may be a more effective therapeutic approach. Microglia have been implicated in tauopathies as their activation is strongly related to the progression of tau phosphorylation and aggregation potentially due to dysfunctional lysosomal activity. Cannabinoid type 2 receptors (CB2) are highly expressed in immune cells and upregulated in activated microglia under conditions of neurologic disease, such as AD.
View Article and Find Full Text PDFNovel Orthosteric/Allosteric Ligands of Cannabinoid Receptors: An Unexpected Pharmacological Profile.
J Med Chem
January 2025
Department of Pharmacy, University of Pisa, 56126 Pisa, Italy.
The design of dualsteric/bitopic receptor ligands as compounds capable of simultaneously interacting with both the orthosteric and an allosteric binding site has gained importance to achieve enhanced receptor specificity and minimize off-target effects. In this work, we reported the synthesis and biological evaluation of a new series of compounds, namely, the series, obtained by chemically combining the CB1R ago-positive allosteric modulators (PAM) with the cannabinoid receptors (CBRs) orthosteric agonist . Therefore, compounds were designed as dualsteric/bitopic ligands for CB1R with the aim of obtaining stronger CB1R agonists or ago-PAMs, with improved receptor subtype selectivity and reduction of central side effects.
View Article and Find Full Text PDFDorsomedial Striatum CB1R signaling promotes Pavlovian devaluation sensitivity in male Long Evans rats and reduces DMS inhibitory synaptic transmission in both sexes.
eNeuro
January 2025
Program in Neuroscience, University of Maryland Baltimore, Baltimore, MD, 21201.
Cannabinoid receptor-1 (CB1R) signaling in the dorsal striatum regulates the shift from flexible to habitual behavior in instrumental outcome devaluation. Based on prior work establishing individual, sex, and experience-dependent differences in Pavlovian behaviors, we predicted a role for dorsomedial striatum (DMS) CB1R signaling in driving rigid responding in Pavlovian autoshaping and outcome devaluation. We trained male and female Long Evans rats in Pavlovian Lever Autoshaping (PLA).
View Article and Find Full Text PDFRisks of Dementia Associated With Anticholinergic Medication Compared to Beta-3 Agonist Among Older Patients With Overactive Bladder in Japan: The LIFE Study.
Int J Geriatr Psychiatry
January 2025
Department of Health Care Administration and Management, Kyushu University Graduate School of Medical Sciences, Fukuoka, Japan.
Article Synopsis
- Anticholinergic drugs may lead to cognitive impairment, and this study specifically examined their risk of causing dementia in older adults in Japan compared to beta-3 agonists.
- The study involved over 1.4 million participants, with nearly 13,500 taking anticholinergics and around 24,700 using beta-3 agonists, all aged 65 and older with overactive bladder.
- Results indicated that users of anticholinergic drugs had a 22% higher risk of developing dementia compared to those using beta-3 agonists, suggesting a significant association between anticholinergic use and increased dementia risk.
PPARα-ERRα crosstalk mitigates metabolic dysfunction-associated steatotic liver disease progression.
Metabolism
December 2024
Translational Nuclear Receptor Research, UGent Department of Biomolecular Medicine, VIB Center for Medical Biotechnology, Ghent, Belgium. Electronic address:
Background And Aims: Metabolic dysfunction-associated steatotic liver disease (MASLD), the most prevalent liver disease worldwide, continues to rise. More effective therapeutic strategies are urgently needed. We investigated how targeting two key nuclear receptors involved in hepatic energy metabolism, peroxisome proliferator-activated receptor alpha (PPARα) and estrogen-related receptor alpha (ERRα), ameliorates MASLD.
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