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

Farmaco. 1993 May;48(5):665-76.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • Binding, Competitive
  • Brain / metabolism
  • Cattle
  • Flunitrazepam / metabolism
  • Receptors, GABA-A / metabolism
  • Structure-Activity Relationship
  • Thiazepines / chemical synthesis*
  • Thiazepines / chemistry
  • Thiazepines / metabolism
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry
  • Triazoles / metabolism

Substances

  • Receptors, GABA-A
  • Thiazepines
  • Triazoles
  • Flunitrazepam