title: Potential histidine decarboxylase inhibitors. 1. alpha- and beta-substituted histidine analogues.
abstract: Histidine analogues with alkyl substitution at Calpha and Cbeta were prepared as potential inhibitors of specific histidine decarboxylase. Activity was assessed in vitro using extracts of rat pyloric stomach and a radioisotopic assay of 14CO2 evolved from carboxyl-14C-labeled histidine. alpha-Substituted analogues (C2-C4) including 2-hydroxyethyl were less potent than alpha-methylhistidine; the alpha-n-butyl analogue was completely inactive at 10(-3) M. Similarly, beta,beta-dimethylhistidine and homohistidine failed to exhibit activity at 10(-3) M.
mesh_terms: D000818:Animals; D002262:Carboxy-Lyases / Q000037:antagonists & inhibitors*; D006639:Histidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006640:Histidine Decarboxylase / Q000037:antagonists & inhibitors*; D066298:In Vitro Techniques; D051381:Rats; D013270:Stomach / Q000201:enzymology; D013329:Structure-Activity Relationship
chemical_list: D006639:Histidine; D002262:Carboxy-Lyases; D006640:Histidine Decarboxylase