Related Experiment Video
Updated: Aug 11, 2026

Systemic and Local Drug Delivery for Treating Diseases of the Central Nervous System in Rodent Models
Published on: August 16, 2010
Medicinal chemical properties of successful central nervous system drugs
Hassan Pajouhesh1, George R Lenz
1Department of Medicinal Chemistry, Neuromed Technologies Inc., Vancouver, British Columbia, Canada V6T 1Z4. hpajouhesh@neuromed.com
Abstract:
Fundamental physiochemical features of CNS drugs are related to their ability to penetrate the blood-brain barrier affinity and exhibit CNS activity. Factors relevant to the success of CNS drugs are reviewed. CNS drugs show values of molecular weight, lipophilicity, and hydrogen bond donor and acceptor that in general have a smaller range than general therapeutics. Pharmacokinetic properties can be manipulated by the medicinal chemist to a significant extent. The solubility, permeability, metabolic stability, protein binding, and human ether-ago-go-related gene inhibition of CNS compounds need to be optimized simultaneously with potency, selectivity, and other biological parameters. The balance between optimizing the physiochemical and pharmacokinetic properties to make the best compromises in properties is critical for designing new drugs likely to penetrate the blood brain barrier and affect relevant biological systems. This review is intended as a guide to designing CNS therapeutic agents with better drug-like properties.
More Related Videos
07:02A 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
11:44Cellular Membrane Affinity Chromatography Columns to Identify Specialized Plant Metabolites Interacting with Immobilized Tropomyosin Kinase Receptor B
Published on: January 19, 2022
Related Concept Videos
CNS Stimulants: Cocaine, Amphetamines and Cannabinoids
CNS Stimulants: Psychedelic Agents
Drugs Affecting Neurotransmitter Release or Uptake
Neurochemical Transmission: Sites of Drug Action
Spasmolytic Agents: Chemical Classification
A major class of centrally acting spasmolytics is the α2-agonist, such as tizanidine. These drugs bind to α2-adrenoceptors, inhibiting the release of the excitatory neurotransmitter glutamate. They also promote...
An Overview of Psychoactive Drugs
Stimulants such as cocaine, amphetamines, and nicotine enhance brain activity, leading to increased alertness, attention, and energy. These drugs typically raise heart rate, blood pressure, and body temperature. While they can induce feelings of euphoria, their misuse can result in severe health...