Functional screening of molecules with high potential in the treatment of mental disorders

• Grant number: 18/22551-2
• Support Opportunities: Research Grants - Innovative Research in Small Business - PIPE
• Duration: March 01, 2020 - May 31, 2021
• Field of knowledge: Biological Sciences - Pharmacology - Biochemical and Molecular Pharmacology
• Principal Investigator: Pedro Henrique Camargo Penna
• Grantee: Pedro Henrique Camargo Penna
• Host Company: Naiad Desenvolvimento Computacional de Fármacos Ltda
• CNAE: Desenvolvimento de programas de computador sob encomenda ; Pesquisa e desenvolvimento experimental em ciências físicas e naturais
• City: São Caetano do Sul
• Associated researchers: Claudio Miguel da Costa Neto
• Associated grant(s): 21/14674-0 - Functional screening and optimization of molecules acting on the oxytocin receptor with a focus on therapeutic applications, AP.PIPE

Abstract

The neuropeptide oxytocin (OXT) acts as a neurotransmitter and neuromodulator in several physiological processes in humans and other mammals, among them we can mention: maternal behavior, food intake, social memory, sexual behavior, stress response, anxiolytic action and promotion of pro-social behavior of trust. Because it is involved in various physiological processes, the drug formulation using OXT as a major component, or the development of new drugs having the cellular receptor (OXTR) in which it interacts as a target has gained interest in the pharmaceutical industry. Currently there are different clinical studies using OXT as a drug, such as: autism, Prader-Willi syndrome, schizophrenia, posttraumatic stress disorder and borderline personality disorder. Interesting results were obtained regarding the effect of oxytocin on the reduction of drug abuse dependence. Here we propose the development of new agonists of the oxytocin receptor with agonistic tendentious activity - activating the Gq protein pathway in a selective and sustained way, without significantly activating the Beta-Arrestin 2 pathway - which may generate drugs that have fewer adverse effects and more persistent effects for application in mental disorders and associated clinical indications. This market is very broad, with mood stabilizers moving around 2 billion reais / year and antidepressants around 1 billion reais / year. The market for generalized anxiety disorders is expected to reach $ 7.5 billion by 2025. It is important to note that there is currently no small molecule in the market for the oxytocin receptor, and that molecules with a biased or biased effect come increasingly being pointed out as the future of the development of drugs acting on G protein coupled receptors. (AU)