Related Experiment Video
Updated: Mar 21, 2026

Tracking Drug-induced Changes in Receptor Post-internalization Trafficking by Colocalizational Analysis
Published on: July 3, 2015
[PHARMACOLOGICAL STUDY OF NEW COMPOUNDS ACTING AS REGULATORS OF 18-KDA TRANSLOCATOR PROTEIN LIGANDS]
Abstract:
The interaction of new original 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamide derivatives with mitochondrial translocator protein (MTP) 18 kDa has been studied by radioligand binding assay. Compounds GML-1 (Ki = 5.2 x 10⁻⁸ M) and GML-3 (Ki = 5.3 x 10⁻⁷ M) exhibit high binding affinity for MTP. GML-1 and GML-3 in a dose range of 0.1-1 mg/kg (i.p.) demonstrated anxiolytic-like effects in the elevated plus-maze test in CD-1 mice, which were blocked by the MTP selective antagonist PK11195. The data obtained on the molecular target, anxiolytic-like effects and low toxicity GML-1 and GML-3 suggest that these compounds are promising for further investigation as anxiolytics.
More Related Videos
07:16Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
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
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Drugs Affecting Neurotransmitter Release or Uptake
The Two-State Receptor Model
The binding affinity of a drug determines its interaction with...
Carrier-Mediated Transport
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
The Significance of Membrane Transport
Transporters facilitate either an active or passive movement of solutes. They can allow a single-molecule transport down its...
Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters