Unbound Brain-to-Plasma Partition Coefficient, K_p,uu,brain-a Game Changing Parameter for CNS Drug Discovery and Development.

ABSTRACT:

Purpose

More than 15 years have passed since the first description of the unbound brain-to-plasma partition coefficient (K_p,uu,brain) by Prof. Margareta Hammarlund-Udenaes, which was enabled by advancements in experimental methodologies including cerebral microdialysis. Since then, growing knowledge and data continue to support the notion that the unbound (free) concentration of a drug at the site of action, such as the brain, is the driving force for pharmacological responses. Towards this end, K_p,uu,brain is the key parameter to obtain unbound brain concentrations from unbound plasma concentrations.

Methods

To understand the importance and impact of the K_p,uu,brain concept in contemporary drug discovery and development, a survey has been co

SUBMITTER: Loryan I 

PROVIDER: S-EPMC9246790 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature