Selective and antagonist-dependent µ-opioid receptor activation by the combination of 2-{[2-(6-chloro-3,4-dihydro-1(2H)-quinolinyl)-2-oxoethyl]sulfanyl}-5-phenyl-4,6-(1H,5H)-pyrimidinedione and naloxone/naltrexone

Autor:	Shu-Yu Lin, Ya-Wen Tien, Yi-Yu Ke, Yung-Chiao Chang, Hsiao-Fu Chang, Li-Chin Ou, Ping-Yee Law, Jing-Hua Xi, Pao-Luh Tao, Horace H. Loh, Yu-Sheng Chao, Chuan Shih, Chiung-Tong Chen, Shiu-Hwa Yeh, Shau-Hua Ueng
Rok vydání:	2021
Předmět:	Analgesics Opioid Sulfonamides Naloxone Organic Chemistry Drug Discovery Receptors Opioid Imidazoles Thiophenes Molecular Biology Biochemistry Naltrexone
Zdroj:	Bioorganic chemistry. 128
ISSN:	1090-2120
Popis:	We identified, via high-throughput screening using a FLIPR® calcium assay, compound 1, which incorporated a dihydroquinolinyl-2-oxoethylsulfanyl-(1H,5H)-pyrimidinedione core and activated the μ-opioid receptor (MOR) in the presence of naloxone or naltrexone. A structure-activity relationship study of the analogs of 1 led to the design of compound 21, which activated MOR in the presence of naloxone with an EC
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60a5add0e18ce226db7cddf6d10fe250 https://pubmed.ncbi.nlm.nih.gov/35710525 Zobrazit plný text záznamu Full Text from ScienceDirect