Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.
In the course of studies on tranquilizers, new non-benzodiazepine-like compounds were synthesized. These are 1-(3,4,5-trimethoxyphenoxy)-3-[4-(2-methoxyphenyl)piperazinyl]prop an-2-ol (INN: enciprazine) and derivatives thereof which were screened pharmacologically in order to evaluate their central nervous system activity. Compounds with marked antiaggressive and anxiolytic properties but without dependence potential could be detected. Enciprazine was selected for clinical investigations.
Engel
J
J
ASTA Pharma AG, Frankfurt, FRG.
Fleischhauer
I
I
Jakovlev
V
V
Kleemann
A
A
Kutscher
B
B
Nickel
B
B
Rauer
H
H
Werner
U
U
Szelenyi
I
I
Johanson
C E
CE
D000374:Aggression / Q000187:drug effects; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D001522:Behavior, Animal / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D005106:Exploratory Behavior / Q000187:drug effects; D005260:Female; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D012646:Self Administration; D013329:Structure-Activity Relationship; D019966:Substance-Related Disorders
D014151:Anti-Anxiety Agents; D010879:Piperazines; C057238:enciprazine