Receptor Binding Affinities of Synthetic Cannabinoids Determined by Non-Isotopic Receptor Binding Assay
Toxicological Research 2019;35:37−44
Published online January 15, 2019;  https://doi.org/10.5487/TR.2019.35.1.037
© 2019 Korean Society of Toxicology.

Hye Jin Cha1, Yun Jeong Song1, Da Eun Lee1, Young-Hoon Kim1, Jisoon Shin1, Choon-Gon Jang2, Soo Kyung Suh1, Sung Jin Kim3 and Jaesuk Yun4,ψ

1Pharmacological Research Division, Toxicological Evaluation and Research Department, National Institute of Food and Drug Safety Evaluation, Ministry of Food and Drug Safety, Chungju, Korea, 2Department of Pharmacology, School of Pharmacy, Sungkyunkwan University, Suwon, Korea, 3Cosmetics Policy Division, Ministry of Food and Drug Safety, Chungju, Korea, 4Neuroimmunology Lab, College of Pharmacy, Wonkwang University, Iksan, Korea
Hye Jin Cha, Pharmacological Research Division, Toxicological Evaluation and Research Department, National Institute of Food and Drug Safety Evaluation, Ministry of Food and Drug Safety, Chungju 28159, Korea, E-mail: chahj1@korea.kr
Received: May 23, 2018; Revised: August 7, 2018; Accepted: August 21, 2018
This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract
A major predictor of the efficacy of natural or synthetic cannabinoids is their binding affinity to the cannabinoid type I receptor (CB1) in the central nervous system, as the main psychological effects of cannabinoids are achieved via binding to this receptor. Conventionally, receptor binding assays have been performed using isotopes, which are inconvenient owing to the effects of radioactivity. In the present study, the binding affinities of five cannabinoids for purified CB1 were measured using a surface plasmon resonance (SPR) technique as a putative non-isotopic receptor binding assay. Results were compared with those of a radio-isotope-labeled receptor binding assay. The representative natural cannabinoid Δ9-tetrahydrocannabinol and four synthetic cannabinoids, JWH-015, JWH- 210, RCS-4, and JWH-250, were assessed using both the SPR biosensor assay and the conventional isotopic receptor binding assay. The binding affinities of the test substances to CB1 were determined to be (from highest to lowest) 9.52 × 10−13 M (JWH-210), 6.54 × 10−12 M (JWH-250), 1.56 × 10−11 M (Δ9-tetrahydrocannabinol), 2.75 × 10−11 M (RCS-4), and 6.80 ×10−11 M (JWH-015) using the non-isotopic method. Using the conventional isotopic receptor binding assay, the same order of affinities was observed. In conclusion, our results support the use of kinetic analysis via SPR in place of the isotopic receptor binding assay. To replace the receptor binding affinity assay with SPR techniques in routine assays, further studies for method validation will be needed in the future.
Keywords : Δ9-THC, Human cannabinoid type I receptor (CB1), Receptor binding assay, Surface plasmon resonance, Synthetic cannabinoids


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