Pharmacology of 1-(3,4-dichlorobenzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidone, a novel antidepressant compound with antianxiety activity

• Published in: Journal of pharmaceutical sciences 1980-10, Vol.69 (10), p.1198-1202
• Main Authors: Ellis, K.O., Wessels, F.L., Burns, R.H., Pong, S.F.
• Format: Article
• Language: English
• Subjects: 1-(3,4-Dichlorobenzyl) - 3,4,5,6-tetrahydro-2(1H)-pyrimidone—evaluation of antidepressant and antianxiety activity, in vitro and in vivo; 4-Dichlorobenzyl) - 3; 6-tetrahydro-2(1H)-pyrimidone; 6-tetrahydro-2(1H)-pyrimidone-evaluation of antidepressant and antianxiety activity; Animals; Anti-Anxiety Agents; Antidepressive Agents; Brain Chemistry - drug effects; Cats; CNS activity-1-; CNS activity—1-(3,4-dichlorobenzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidone, evaluation of antidepressant and antianxiety activity, in vitro and in vivo; evaluation of antidepressant and antianxiety activity; Female; Histamine H1 Antagonists; Humans; in vitro and in vivo; Lethal Dose 50; Male; Mice; Monoamine Oxidase Inhibitors; Neurotransmitter Agents - metabolism; Nictitating Membrane - drug effects; Parasympatholytics; Pentylenetetrazole - antagonists & inhibitors; Pyrimidinones - pharmacology; Rats; Stereotyped Behavior - drug effects; Tetrabenazine - antagonists & inhibitors
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.2600691021

1-(3,4-Dichlorobenzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidone (I) was evaluated in selected pharmacological tests, and its activity was compared to that of some clinically useful psychotropic drugs. Based on the results, it is evident that I has a unique profile of antidepressant and antianxiety activities that are evident in the same dose range. The mechanism of its antidepressant activity is proposed to be similar to the tricyclic antidepressants, that is, inhibition of norepinephrine uptake. Neither I nor the tricyclic antidepressants possess monoamine oxidase-inhibiting activity. However, unlike the tricyclic antidepressants, I is devoid of any significant anticholinergic activity and presumably is free of anticholinergic side effects.