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자료유형
학술저널
저자정보
Hye Jin Cha (Ministry of Food and Drug Safety) Yun Jeong Song (Ministry of Food and Drug Safety) Da Eun Lee (Ministry of Food and Drug Safety) Young-Hoon Kim (Ministry of Food and Drug Safety) Jisoon Shin (Ministry of Food and Drug Safety) Choon-Gon Jang (Sungkyunkwan University) Soo Kyung Suh (Ministry of Food and Drug Safety) Sung Jin Kim (Ministry of Food and Drug Safety) Jaesuk Yun (Wonkwang University)
저널정보
한국독성학회 Toxicological Research Toxicological Research Vol.35 No.1
발행연도
2019.1
수록면
37 - 44 (8page)

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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 Δ<SUP>9</SUP>-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<SUP>−13</SUP> M (JWH-210), 6.54 × 10<SUP>−12</SUP><SUP></SUP> M (JWH-250), 1.56 × 10<SUP>−11</SUP> M (Δ<SUP>9</SUP>-tetrahydrocannabinol), 2.75 × 10<SUP>−11</SUP> 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.

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Abstract
INTRODUCTION
MATERIALS AND METHODS
RESULTS
DISCUSSION
REFERENCES

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UCI(KEPA) : I410-ECN-0101-2019-513-000294567