Effect of acylation with eleostearic acids on the monoamine oxidase inhibitory potency of some hydrazine antidepressants in mice.
The effect of incorporation of an eleostearoyl group into molecules of aralkylhydrazines on their monoamine oxidase inhibitory potency was investigated in vitro and in vivo. The results showed that on a molar basis the hydrazides possessed an in vitro potency lower than and an in vivo potency and acute toxicity comparable to those of the corresponding aralkylhydrazines. The sequence of the relative potency of aralkylhydrazines and their hydrazides was similar. The overall pharmacological profile indicated that these aralkylhydrazines retained their monoamine oxidase inhibitory properties when the free hydrazine nitrogen was acylated with an eleostearoyl group.
D000215:Acylation; D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D001763:Blepharoptosis / Q000517:prevention & control; D001921:Brain / Q000201:enzymology; D001923:Brain Chemistry / Q000187:drug effects; D004295:Dihydroxyphenylalanine / Q000494:pharmacology; D004298:Dopamine / Q000032:analysis; D004357:Drug Synergism; D005231:Fatty Acids, Unsaturated / Q000494:pharmacology*; D006834:Hydrazines / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D008042:Linolenic Acids / Q000494:pharmacology; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology* / Q000633:toxicity; D009043:Motor Activity / Q000187:drug effects; D009638:Norepinephrine / Q000032:analysis; D012110:Reserpine / Q000037:antagonists & inhibitors; D012701:Serotonin / Q000032:analysis; D013329:Structure-Activity Relationship
D000928:Antidepressive Agents; D005231:Fatty Acids, Unsaturated; D006834:Hydrazines; D008042:Linolenic Acids; D008996:Monoamine Oxidase Inhibitors; D012701:Serotonin; D004295:Dihydroxyphenylalanine; D012110:Reserpine; D004298:Dopamine; D009638:Norepinephrine