Dose-related effects of the synthetic met-enkephalin analogue FK 33-824 on esophageal motor activity in healthy humans.
The effects of FK 33-824, a methionine enkephalin analogue, 313, 625, 1250, 2500, and 5000 ng/kg body wt intramuscularly, on esophageal motor activity and cardiovascular and central nervous functions were studied in 8 healthy men. In the lower one-third of the esophagus, amplitude and duration of swallow contractions increased dose-dependently within 15 min after administration. In the middle one-third, amplitudes increased only slightly, whereas no systematic changes occurred in the upper one-third. The propagation velocity of the deglutitive wave accelerated dose-dependently between 15 and 10 cm as well as between 10 and 5 cm above the lower esophageal sphincter, the acceleration being more pronounced in the distal segment. Heart rate and systolic and diastolic blood pressure increased dose-relatedly, while no effects were found on electroencephalogram and reaction time. These results, together with earlier findings, support the notion of a participation of enkephalins in the regulation of the smooth muscle esophagus.
D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D005405:D-Ala(2),MePhe(4),Met(0)-ol-enkephalin; D003679:Deglutition / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004569:Electroencephalography; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives* / Q000494:pharmacology; D004947:Esophagus / Q000187:drug effects*; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D008297:Male; D008365:Manometry; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D012119:Respiration / Q000187:drug effects
D004744:Enkephalin, Methionine; D005405:D-Ala(2),MePhe(4),Met(0)-ol-enkephalin