PHARMACOLOGICAL AND BIOCHEMICAL-STUDIES ON A NEW POTENTIAL NEUROLEPTIC, N-(1-BENZYL-3-PYRROLIDINYL)-5-CHLORO-2-METHOXY-4-METHYLAMINOBENZAMIDE (YM-08050)

  • 1 January 1979
    • journal article
    • research article
    • Vol. 241  (1) , 68-78
Abstract
Pharmacological and biochemical properties of a novel compound, N-(1-benzyl-3-pyrrolidinyl)-5-chloro-2-methoxy-4-methylaminobenzamide (YM-08050) were compared with those of haloperidol (HPD) and chlorpromazine (CPZ) in animals [mice, rats, dogs]. YM-08050 was more potent than HPD or CPZ in inhibitory effects on a variety of behaviors, i.e., apomorphine-induced stereotyped behavior and emesis, methamphetamine-induced stereotyped behavior, conditioned avoidance response and open field behavior. YM-08050 induced catalepsy only at much higher doses than to exhibit the inhibitory activities. The inhibitory effects of YM-08050 on [3H]dopamine binding and dopamine-sensitive adenylate cyclase in the synaptic membrane fractions of the canine caudate nucleus were much greater than those of HPD and CPZ. YM-08050, a potent central dopaminergic blocker, is a potential antipsychotic drug with less extrapyramidal side effects than those of HPD and CPZ.

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