| 摘要 |
Cis-tetrahydrospiro(cyclohexane-1,1'-pyrido[3,4-b]indol)-4-amine derivatives (I) and their salts and free bases are new. Cis-tetrahydrospiro(cyclohexane-1,1'-pyrido[3,4-b]indol)-4-amine derivatives of formula (I) and their salts and free bases are new. R 1> : H or CH 3; R 2>, R 3> : H or halo; R 4>, R 5> : H, halo or O-1-3C-alkyl; Q 1>-Q 2>- : -CH 2- or -CR 6>=CH-; and either R 6>, R 7> : H; or R 6>R 7> : a five membered ring. An independent claim is included for a composition comprising (I). [Image] ACTIVITY : Analgesic; Tranquilizer; Antidepressant; Anticonvulsant; Neuroprotective; Nootropic; Antialcoholic; Antiaddictive; Endocrine-Gen.; Cardiovascular-Gen.; Hypertensive; Hypotensive; Auditory; Antipruritic; Gastrointestinal-Gen.; Eating-Disorders-Gen.; Anabolic; Anorectic; Antidiarrheic; Uropathic. MECHANISM OF ACTION : Nociceptin receptor binder; mu -Opioid receptor binder. The ability of (I) to bind nociceptin receptor was tested using radio-binding assay. The results showed that 2',3',4',9'-tetrahydro-N,N-dimethyl-4-(3-fluorophenyl)-2'-(benzothiophen-2-yl)carbonylspiro[cyclohexan-1,1'(1'H)-pyrido[3,4-b]indol]-4-amine exhibited an inhibition constant value of 16 nM. |
