[Radioimmunologic and radioreceptor studies of the pharmacokinetics of the enkephalin analog dalargin in man].
Pharmacokinetics of dalargin, an opioid hexapeptide, was investigated on 7 males by two approaches. Dalargin radioimmunoassay was performed using a highly specific antiserum reacting only with the whole molecule. In radioreceptor assay lyophilized rat brain membranes containing opiate receptors were used. 2-6 min after intravenous introduction of 1-10 mg dalargin, immunoreactive dalargin blood concentration was lower than 0.5 ng/ml. The results of radioreceptor assay were presented as a biexponential curve with a fast main phase of activity changes (90%, characteristic time 1.5-5.0 min) and a slow "clearance" phase (10% of the substance, characteristic time 85-200 min). Prolonged presence of receptor-active substances in the blood can be attributed to the products of dalargin degeneration, namely its N-terminal penta- and tetrapeptides.
D000328:Adult; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives* / Q000097:blood; D016308:Enkephalin, Leucine-2-Alanine / Q000031:analogs & derivatives*; D006801:Humans; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D011863:Radioimmunoassay; D011869:Radioligand Assay
D004743:Enkephalin, Leucine; D016308:Enkephalin, Leucine-2-Alanine; C040996:enkephalin-Leu, Ala(2)-Arg(6)-
Radioimmunnoe i radioretseptornoe izuchenie farmakokinetiki analoga énkefalinov dalargina u cheloveka.