title: Ramipril inhibition of rabbit (Oryctolagus cuniculus) small intestinal brush border membrane angiotensin converting enzyme.
abstract: 1. Rabbit small intestinal brush border membranes possessed prominent angiotensin converting enzyme (ACE) activity. 2. Intestinal ACE was located on the lumen surface, as verified by ACE co-enrichment with brush border membrane marker enzymes. 3. Hydrolysis kinetics of rabbit intestinal ACE were comparable to the lung, utilizing the substrate (N-[3-(2-furyl)acryloyl]-L-phenylalanylglycylglycine; the Vmax = 543 +/- 51 mumol/min/g and Km = 0.62 +/- 0.09 mmol/l. 4. Intestinal brush border ACE activity was strongly inhibited by the antihypertensive drug Ramipril, which yielded an IC50 value of 5 nmol/l; the ACE activity remained completely inhibited during 15 days after a single dose of 10 mumol/l Ramipril.
authors.affiliation: Department of Physiology, College of Medicine, University of Florida, Gainesville 32610.
authors.forename: B R
authors.initials: BR
authors.lastname: Stevens
authors.forename: M I
authors.initials: MI
authors.lastname: Phillips
authors.forename: A
authors.initials: A
authors.lastname: Fernandez
mesh_terms: D000806:Angiotensin-Converting Enzyme Inhibitors / Q000494:pharmacology*; D000818:Animals; D001643:Bridged Bicyclo Compounds / Q000494:pharmacology*; D001952:Bridged-Ring Compounds / Q000494:pharmacology*; D006868:Hydrolysis; D007421:Intestine, Small / Q000187:drug effects* / Q000201:enzymology / Q000648:ultrastructure; D007700:Kinetics; D008871:Microvilli / Q000187:drug effects / Q000378:metabolism; D011817:Rabbits; D017257:Ramipril
chemical_list: D000806:Angiotensin-Converting Enzyme Inhibitors; D001643:Bridged Bicyclo Compounds; D001952:Bridged-Ring Compounds; D017257:Ramipril