AGONIST-ANTAGONIST PROPERTIES OF 5, 7-ETHANO-4, 5, 5a, 6, 7, 11b-HEXAHYDRO-2, 6, 7-TRIMETHYL-1H-BENZO [g] HOMOQUINOLIN-9-OL AND 4, 6-ETHANO-3, 4, 4a, 5, 6, 10b-HEXAHYDRO-2, 5, 6-TRIMETHYLBENZO [f] QUINOLIN-8-OL

AGONIST-ANTAGONIST PROPERTIES OF 5, 7-ETHANO-4, 5, 5a, 6, 7, 11b-HEXAHYDRO-2, 6, 7-TRIMETHYL-1H-BENZO [g] HOMOQUINOLIN-9-OL AND 4, 6-ETHANO-3, 4, 4a, 5, 6, 10b-HEXAHYDRO-2, 5, 6-TRIMETHYLBENZO [f] QUINOLIN-8-OL

Agonistic and antagonistic properties of novel tetracyclic benzomorphans (1-4) were evaluated in vivo and in vitro opioid receptor interaction tests. Seven-membered derivatives (1, 3) showed synergism with morphine analgesia. Six-membered derivatives (2, 4) demonstrated antagonist opioid characters.

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Veröffentlicht in:Chemical & pharmaceutical bulletin 1983/07/25, Vol.31(7), pp.2520-2522
Hauptverfasser: Hori, Mikio, Kataoka, Tadashi, Shimizu, Hiroshi, Imai, Eiji, Suzuki, Yoshinari, Kawamura, Norihiro, Fujimura, Hajime, Nozaki, Masakatsu, Niwa, Masayuki
Format: Artikel
Sprache:eng
Schlagworte:
Analgesics
Animals
Chemical reactivity
Chemistry
Exact sciences and technology
Mice
Narcotic Antagonists
Organic chemistry
Pentazocine - analogs & derivatives
Pentazocine - pharmacology
Reactivity and mechanisms
stracture activity relationship
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Zusammenfassung:Agonistic and antagonistic properties of novel tetracyclic benzomorphans (1-4) were evaluated in vivo and in vitro opioid receptor interaction tests. Seven-membered derivatives (1, 3) showed synergism with morphine analgesia. Six-membered derivatives (2, 4) demonstrated antagonist opioid characters.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.31.2520