Measurement of the pharmacokinetics and pharmacodynamics of neuroactive compounds
Related Experiment Video
Updated: Jun 19, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
Published on: February 11, 2019
Mohammad S Alavijeh1, Alan M Palmer
1Pharmidex Pharmaceutical Services Ltd., 72 New Bond Street, London, W1S 1RR, UK.
Abstract:
The need to discover and develop safe and effective new medicines is greatest for disorders of the CNS. A core requirement for an effective neurotherapeutic agent is an ability to cross the blood-brain barrier and remain in the brain interstitial fluid (ISF) for a sufficient duration and concentration to evoke the desired therapeutic effect. Measuring the free concentration of a neuroactive compound in brain ISF is therefore an essential step in the critical path towards the development of a CNS medicine. In vivo microdialysis provides a powerful method for the measurement of endogenous and exogenous substances in the ISF surrounding the probe and so it represents an important tool in CNS drug discovery. It can also be used to measure the pharmacodynamic response of neuroactive compounds by measuring neurotransmitters and second messengers. Another approach to measure both pharmacokinetics and the pharmacodynamics of neuroactive compounds is the measurement of receptor occupancy, which has the advantage of being applicable to the study of humans as well as experimental animals. Measurement of the pharmacokinetics and pharmacodynamics of neuroactive compounds clearly improve understanding of the efficacy and safety of drug candidates, which improves both the efficiency and the effectiveness of CNS medicines research.
More Related Videos
07:56A Plate-Based Assay for the Measurement of Endogenous Monoamine Release in Acute Brain Slices
Published on: August 11, 2021
11:26Assessment of Dopaminergic Homeostasis in Mice by Use of High-performance Liquid Chromatography Analysis and Synaptosomal Dopamine Uptake
Published on: September 21, 2017
Related Concept Videos
Measurement of Bioavailability: Pharmacodynamic Methods
Measurement of Bioavailability: Pharmacokinetic Methods
Pharmacodynamic Responses: Different Types
Drug Concentrations: Measurements
Plasma —...
Pharmacodynamics: Overview and Principles
Most drugs' effects result from their interactions with drug receptors or targets within the body. These interactions trigger specific responses at the cellular or systemic level. Drug receptors can be found on the surfaces of cells or within...
Pharmacokinetic–Pharmacodynamic Relationship: Dose to Pharmacological Effect