Publisher Summary This chapter elaborates on antipsychotic and antianxiety agents. The reported contribution of pyrrole nuclei to the sedative action of ketone derivatives encouraged the synthesis of relatives of ketone derivatives in which the benzene ring was replaced by pyrrole. A new indole derivative, U-22394, incorporates a part of the iboga alkaloid structure. U-22394 antagonizes the aggressiveness of fighting mice, is active in blocking conditioned avoidance, is hypothermic and anorexigenic and displays tryptamine-like activity in mice. The studies with the effective antihypertensive drug Catapres (2-(2,6-dichlorophenylamine)-2-imidazoline, 9) uncovered useful antianxiety effects at 1 mg per day and decreased agitation in psychotic patients at higher doses. Chlorethate was as selective as meprobamate in suppressing rage activity in mice without producing ataxia. In studies conducted in outpatient populations given medication for anxiety psychoneurosis, chlorethate was found to be more effective than phenobarbital and equivalent in efficacy to meprobamate.