Studies on annelated 1,4-benzothiazines and 1,5-benzothiazepines. VII. Synthesis and inhibition of benzodiazepine receptor binding of some 4,5-dihydro-tetrazolo[5,1-d]-1,5-benzothiazepines and 5-phenyl-s-triazolo[3,4-d]-1,5-benzothiazepines.
The 4,5-dihydro-tetrazolo[5,1-d]-1,5-benzothiazepines 3a-k and the 5-phenyl-s-triazolo[3,4-d]-1,5-benzothiazepines 6a-f and 11a-c have been prepared and tested for their ability to displace [3H] flunitrazepam binding from bovine brain membranes. Some of the triazoloderivatives showed moderate binding affinity for the benzodiazepine receptor.
Ambrogi
V
V
Istituto di Chimica Farmaceutica e Tecnica Farmaceutica, Università di Perugia, Italy.
Grandolini
G
G
Perioli
L
L
Giusti
L
L
Lucacchini
A
A
Martini
C
C
D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D002417:Cattle; D005445:Flunitrazepam / Q000378:metabolism; D011963:Receptors, GABA-A / Q000378:metabolism; D013329:Structure-Activity Relationship; D013841:Thiazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism
D011963:Receptors, GABA-A; D013841:Thiazepines; D014230:Triazoles; D005445:Flunitrazepam