Studies on annelated 1,4-benzothiazines and 1,5-benzothiazepines. X--Synthesis and inhibition of benzodiazepine receptor binding of new 1,4-thiazine and 1,5-thiazepine polycondensed heterocycles with steroidal structure.
Some naphtho[1,2,-b]-s-triazolo[4,3-d]-1,4-thiazine and 1,5-thiazepine and s-triazolo[4', 3'-4,5]-1,4-thiazino[3,2-c]quinoline derivatives have been synthesized and tested for their ability to displace [3H]RO 15-1788 binding from bovine brain membranes. Several compounds showed moderate binding affinity for the benzodiazepine receptor.
Grandolini
G
G
Istituto di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia, Italy.
Ambrogi
V
V
Perioli
L
L
Giannaccini
G
G
Lucacchini
A
A
Martini
C
C
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002417:Cattle; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D005442:Flumazenil / Q000493:pharmacokinetics*; D018757:GABA Modulators / Q000493:pharmacokinetics*; D066298:In Vitro Techniques; D007700:Kinetics; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects*; D013843:Thiazines / Q000138:chemical synthesis* / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
D018757:GABA Modulators; D011804:Quinolines; D011963:Receptors, GABA-A; D013843:Thiazines; D014230:Triazoles; D005442:Flumazenil; D005680:gamma-Aminobutyric Acid