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Jenrin Discovery Announces Recent Advances in Understanding of the Endocannabinoid System Using JD-5037


Philadelphia, Pa. – Sep 11, 2013

Mechanism of Action of Peripheral CB1 Inverse Agonists Suggests Potential Clinical Utility in Metabolic Disorders

Research published in Nature Medicine and Journal of Hepatology by scientists at the National Institutes of Health, using JD-5037, the best-in-class peripheral CB1 inverse agonist from Jenrin Discovery, LLC, has illuminated the mechanism of action for this class of drugs, providing a rationale for the potential therapeutic benefits seen when only peripheral endocannabinoid receptors are inhibited.

Data published in Nature Medicine reveal that blockade by JD-5037 of CB1 receptors on inflammatory cells infiltrating the pancreas prevented the death of insulin-producing beta cells by macrophage-derived cytokines. In a weight loss-independent rodent model of human type 2 diabetes, chronic treatment with JD-5037 improved glycemic control, and delayed the development of diabetes (Sept. 2013, Vol. 19, 1132-1140).

A separate study published in the Journal of Hepatology demonstrated that chronic treatment of obese mice with JD-5037 reduced body weight and reversed hepatic steatosis and insulin resistance. These effects are mediated by CB1 receptor-dependant blockade of bio-active long-chain ceramides in the liver (http://onlinelibrary.wiley.com/doi/10.1002/hep.26606/abstract).

“These insights on the MOA of CB1 in peripheral tissues further our belief in the potential clinical value of JD-5037 for patients with diabetes, NASH, and other disorders,” said John McElroy, Ph.D., President and Chief Scientific Officer at Jenrin Discovery.

Senior author and NIAAA scientific director George Kunos, M.D., Ph.D. stated, “JD-5037 was an ideal molecule to test whether the blockade of peripheral CB1 receptors on pancreatic macrophages might explain the anti-diabetic efficacy of this class of drugs. Results in pre-diabetic animals suggest the potential to slow and even reverse disease progression.

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