Researchers at the University of Maryland School of Medicine in Baltimore have discovered functioning bitter taste receptors (TAS2Rs) on bronchial smooth muscle. Although identical to receptors on the tongue, the receptors in the bronchi are not clustered in buds and…
Blog Archives
Dial M3 for Memory
The cognitive improvement in Alzheimer’s disease patients brought about by treatment with acetyl cholinesterase inhibitors has been largely attributed to enhanced M1-muscarinic receptor signalling. Recently, however, studies with M1-receptor knockout mice and with more selective M1-receptor modulators have suggested that…
New Obesity Target
The presence of multiple redundant and compensatory pathways controlling energy homeostasis has, so far, limited the effectiveness of anti-obesity treatments and suggests that combination therapy may be the best approach for treating the worldwide obesity epidemic. Writing in the journal…
Arrestin’ Osteoporosis
Osteoporosis is the result of an imbalance between bone resorption and bone formation in the constant matrix remodelling process that occurs in healthy bone. Bone remodelling is regulated by parathyroid hormone (PTH) which stimulates bone formation by binding to PTH…
Another Way to Control GLP-1
The incretin, glucagon-like peptide-1 (GLP-1), is an intestinal hormone that stimulates production and release of insulin from pancreatic beta cells. Consequently there has been considerable interest in mimicking the activity of GLP-1 for treatment of metabolic disorders such as Type-II…
Still Signalling from Below the Surface
Compounds acting at G-protein coupled receptors (GPCRs) form the largest class of drug molecules but, although the biochemical steps involved in GPCR signalling are known in some detail, the location of these events in space and time in living cells…
Cannabinoids – Are They a Pain?
Many groups developing cannabinoid receptor agonists for the treatment of pain have sought to identify selective CB2 receptor agonists to avoid the psychotropic effects associated with CB1 receptor agonists and a recent report in the journal Science may provide another…
PF-3845 – A Potent and Selective FAAH Inhibitor
The discovery of the cannabis receptors CB1 and CB2 and the subsequent discovery of anandamide (N-arachidonoylethanolamine), the first endogenous agonist of both receptors, provided a rationale for the known analgesic properties of Cannabis sativa. Anandamide is rapidly hydrolyzed and inactivated…
Peptide CB1 Agonists Discovered
Although cannabis has a long history of use in rituals, as a medicine and as a psychoactive agent, it wasn’t until the late 1980s that the first receptor for the major psychoactive component, Δ9-tetrahydrocannabinol, was identified. This receptor, which came…
Oral MC4 Receptor Antagonists as Treatment for Cachexia
Cachexia affects many different chronically ill patient populations, including those with cancer. It results in loss of body weight, particularly of lean body mass (LBM), and is estimated to be responsible for over 20% of all cancer-related deaths. Currently, available…
