✦ LIBER ✦

Design and synthesis of 10-oxo derivative of N-cyclopropylmethyl (−)-6β-acetylthiodihydro-normorphine, a potentially κ-selective opioid receptor ligand

✍ Scribed by Takeshi Sagara; Sawako Ozawa; Emi Kushiyama; Katsuo Koike; Issei Takayanagi; Ken Kanematsu

Publisher: Elsevier Science
Year: 1995
Tongue: English
Weight: 227 KB
Volume: 5
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(95)00239-p

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✦ Synopsis

The design and synthesis of 10-oxo derivative of N-cyclopropylmethyl-(-)-613-acetylthio dihydronormorphine (4) are described. The result of pharmacological assays indicate that compound 4 acts as a tt-opioid receptor antagonist and K-opioid receptor agonist which is suggested to be more potent analgesic action than that of 1 and morphine through an activation of ~-opioid receptors.