Synthesis and pharmacological screening of some N,N'-bis-[4-(4-aryl-1-piperazinyl)butyl]-substituted derivatives of 1,8-dimethylbicyclo-[2.2.2]oct-7-ene-2,3,5,6-tetracarboxydiimide.
The preparation of several derivatives of bicyclo[2.2.2]oct-7-ene- 2,3,5,6-tetracarboxydiimide on two routes has been described. Some of them display an expected anxiolytic activity. The 5-HT1A receptor affinities of tested compounds are comparable with that of buspirone.
Turło
J
J
Department of Medical Chemistry, Medical Academy, Warszawa, Poland.
Zawadowski
T
T
Rump
S
S
Jakowicz
I
I
Gidyńska
T
T
Gałecka
E
E
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D001667:Binding, Competitive; D001933:Brain Stem / Q000187:drug effects / Q000378:metabolism; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D002065:Buspirone / Q000378:metabolism / Q000494:pharmacology; D002234:Carbodiimides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003198:Computer Simulation; D003975:Diazepam / Q000494:pharmacology; D004326:Drinking / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D011985:Receptors, Serotonin / Q000378:metabolism*; D044263:Receptors, Serotonin, 5-HT1; D013329:Structure-Activity Relationship
C092626:1,8-dimethylbicyclo(2.2.2)oct-7-ene-2,3,5,6-tetracarboxydiimide; D014151:Anti-Anxiety Agents; D001643:Bridged Bicyclo Compounds; D002234:Carbodiimides; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D003975:Diazepam; D002065:Buspirone