MSU Researchers granted Patent for the invention related to development of anti-obesity compound

A team of researchers from the Maharaja Sayajirao University of Baroda granted patent for the invention related to development of anti obesity compound. Led by Prof M. R. Yadav, Founder Dean, along with Dr Prashant R. Murumkar, Asst Professor, Mahesh Shidore and Jatin Machhi, research scholars from Faculty of Pharmacy has been granted a patent for their invention related to the development of novel molecules as selective 5-HT2C agonist used in the treatment of obesity, depression, anxiety and sexual dysfunction. This work has been published in the reputed international journal ‘RSC advances’ published by Royal Society of Chemistry.

The 5-HT2 receptors comprise of three members 5-HT2A, 5-HT2B and 5-HT2C, all belonging to the super family of G-protein coupled receptors. 5-HT2C receptors are located in the brain and their activation regulates appetite and food consumption by promoting satiety through appetite suppression by activation of 5-HT2C receptors.

Prof Yadav and his research team developed selective agents with high affinity for this receptor over 5-HT2B and 5-HT2A for the treatment of obesity and related diseases. Selective binding of the compounds to 5-HT2C receptor is crucial because 5-HT2A agonists can have potentially hallucinogenic and cardiovascular side effects while 5-HT2B agonism is linked with heart valvulopathy and pulmonary hypertension.

The study proved that the developed compounds are devoid of side effects as they are selectively binding with 5-HT2C receptors and are devoid of intrinsic activity for 5-HT2A and 5-HT2B receptors. The newly developed compounds were evaluated in vitro on the rat thoracic aortic strip and isolated rat fundus for their 5-HT2A and 5-HT2B receptors’ sensibilities. Further, these compounds were assessed for their desired biological activity of reducing food intake in the whole animal model.

A similar type of compound available in the market, Lorcaserin, marketed under the brand name Belviq is a weight-loss drug developed by Arena Pharmaceuticals. But it has been withdrawn from the market in the United States very recently in 2020 due to its increased risk of causing cancer. Currently, Dr Mahesh is working in R & D located at Hyderabad and Dr Jatin Macchi is working as Postdoctoral Research Associate, University of Nebraska Medical Centre, USA.