Application of the in vitro metabolic stability assay in the evaluation of candidates for drugs with potential nootropic activity

• Grant number: 18/21287-0
• Support type: Scholarships in Brazil - Scientific Initiation
• Effective date (Start): March 01, 2019
• Effective date (End): December 31, 2019
• Field of knowledge: Health Sciences - Pharmacy - Toxicological Analysis
• Principal researcher: Rosangela Gonçalves Peccinini
• Grantee: Vitor Mesquita Pereira dos Santos
• Home Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

Metabolic instability is one of the main pharmacokinetic processes whose inadequate characteristics may impair the development of a drug candidate, since it affects parameters such as clearance, half-life and bioavailability, and is also related to toxicity. In vitro metabolism assay may be performed with cells or cell animal model in which the pharmacokinetic assay is planned, or with cells or human fractions, allowing the correlation of the clearances observed in vitro and in vivo for the animal model, and predicted human clearance calculation. Due to increased of life expectancy, aging has been related to neuronal changes associated with the appearance of a series of disorders of the central nervous system that affect cognitive processes, and may be associated with some situations such as dementia associated with Parkinson's Disease and Alzheimer's, schizophrenia, depression, head trauma, epilepsy among others. The present work aims to carry out in vitro metabolism tests in the Laboratory of the Research Group on Pharmacokinetics and Toxicology of New Drugs and Medications of the FCFAr / UNESP to obtain relevant information to the pre-clinical trials for the candidate drug molecules with potential application in the central nervous system disorders.