Figure - PMC

Skip to main content

An official website of the United States government

Here's how you know

Here's how you know

Official websites use .gov
A .gov website belongs to an official government organization in the United States.

Secure .gov websites use HTTPS
A lock ( ) or https:// means you've safely connected to the .gov website. Share sensitive information only on official, secure websites.

View full-text article in PMC

. 2020 Jun 22;10:10078. doi: 10.1038/s41598-020-66821-0

Search in PMC
Search in PubMed
View in NLM Catalog
Add to search

© The Author(s) 2020

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

PMC Copyright notice

Compound 018 is a competitive antagonist at α₄β₁δ receptors and displaces [³H]muscimol binding. (A) Schild plot of 018 at α₄β₁δ receptors determined in the FMP assay showing a right shift of the GABA concentration-response curve with increasing concentrations of 018 without affecting efficacy. Shown are pooled data from five independent experiments with three technical replicates given as means ± SEM. (B) Schild plot of data displayed in (A) showing a Schild slope of 1.03 indicative of competitive antagonism. (C) Concentration-dependent inhibition of [³H]muscimol binding by 018 and 2027 in rat cortical homogenate, with GABA as reference, showing a competitive profile of the compounds. Data are given as means ± SEM from four independent experiments performed in technical triplicates. The K_i of GABA is 0.049 μM, data from Krall et al.⁴⁸.