The pyrido[2,1-c][1,4]benzothiazines 1a-t and the pyrido[2,1-c][1,4]thiazines 7a,b were prepared and tested for their ability to displace specific [3H]diazepam binding from rat brain membranes. Some of the examined compounds of type 1 and 7b showed moderate binding affinity for the benzodiazepine receptor.