Pharmacological action of FD-008, a new dopamine-beta-hydroxylase inhibitor. III. Effects on endogenous biogenic amine levels in rats.
Effect of a new dopamine beta-hydroxylase inhibitor, 5-(4'-chlorobutyl)-picolinic acid (FD-008) on endogenous amine levels in various tissue of normotensive and spontaneously hypertensive rats were determined in comparison with its mother compound, fusaric acid, and disulfiram. FD-008 decreased norepinephrine (NE) levels in the brain and heart with a slight increase of dopamine (DA) level in the brain. NE lowering activity of FD-008 was stronger than that of fusaric acid. Disulfiram was less active and the activity was one-tenth of FD-008. FD-008 lowered NE level even when DA was increased by pretreatment with L-DOPA or iproniazid but did not cause a further significant reduction of NE when catecholamines were practically depleted by pretreatment with reserpine.
D000311:Adrenal Glands / Q000032:analysis / Q000187:drug effects; D000818:Animals; D001679:Biogenic Amines / Q000032:analysis*; D001923:Brain Chemistry / Q000187:drug effects; D002531:Cerebellum / Q000032:analysis; D004221:Disulfiram / Q000494:pharmacology; D004298:Dopamine / Q000032:analysis; D004299:Dopamine beta-Hydroxylase / Q000037:antagonists & inhibitors*; D005669:Fusaric Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D006321:Heart / Q000187:drug effects; D006973:Hypertension / Q000378:metabolism; D007490:Iproniazid / Q000494:pharmacology; D007980:Levodopa / Q000494:pharmacology; D008297:Male; D009206:Myocardium / Q000032:analysis; D009638:Norepinephrine / Q000032:analysis; D009830:Olfactory Bulb / Q000032:analysis; D010848:Picolinic Acids / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D012110:Reserpine / Q000494:pharmacology; D012701:Serotonin / Q000032:analysis
D001679:Biogenic Amines; D010848:Picolinic Acids; D012701:Serotonin; D007980:Levodopa; D012110:Reserpine; D007490:Iproniazid; D004299:Dopamine beta-Hydroxylase; D005669:Fusaric Acid; D004221:Disulfiram; D004298:Dopamine; D009638:Norepinephrine