Novel pyridazino[4,5-b] [1,5]oxazepines and -thiazepines as 5-HT(1A) receptor ligands

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 22, 1997, Pages 2857-2862

  Matyus P ^a,b   Varga, I ^a   Zara E ^a   Mezei, A ^a   Behr, A ^a   Simay, A ^a   Haider, N ^c   Boros, S ^a   Bakonyi, A ^a   Horvath E ^a   Horvath K ^a  

^a Institute for Drug Research Budapest   (Hungary)

^b SEMMELWEIS UNIVERSITY OF MEDICINE   (Hungary)

^c UNIVERSITY OF VIENNA   (Austria)

Author keywords

[No Author keywords available]

Indexed keywords

PYRIDAZINE DERIVATIVE; PYRIDAZINONE DERIVATIVE; SEROTONIN 1A RECEPTOR;

ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; DRUG RECEPTOR BINDING; HYDROGEN BOND; MALE; NONHUMAN; RAT; RECEPTOR BINDING;

ANIMALIA;

EID: 0343052545     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)10089-0     Document Type: Article

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5. HU Pat. 93 00091.
6. 6) 1-59 (d. 3H), 1.97-2.30 (m. 2H), 3.38 (m. 2+1H), 3.60 (d. 3H), 3.72; 3.94 (2×m. 2×lH), 3.77 (s. 3H), 4.36 (m, 4H), 6.97 (m, 4H), 7.72, 8.16 (2×s, hindered rotation, 2×0,5H )
7. Konecny, V.; Kovac. S.; Varkonda, S. Collect. Czech. Chem. Commun. 1985, 50, 492.
8. 3H|-yohimbine (3089 GBq/mmol specific activity) used at a concentration of 2 nM in the presence or absence of several concentrations of the competing drug in a final volume of 0. 25 ml of buffer (50 mM TR1S-HC1. 5 mM EDTA. 100 mM NaCl pH=7.2). Non-specific binding was determined with 1 mM yohimbine. Separation was carried out by filtering through a Whatman GF/C filter.