Biomedical subjects
Publications and source records attributed to O F Dmitrieva.
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Daily administration of 12 mg of dexamethasone to monkeys during 10 days resulted in decrease of the levels of alpha- and gamma-endorphins and cortisol 7 days after the first injection. The titers of these peptides in plasma of monkeys. exposed to two hours of immobilization stress were elevated twice above basal levels. The maximum elevation took place 6 hours after the beginning of immobilization. This effect wasn't detected in monkeys, which received 12 mg of dexamethasone during 10 days.
Blood gamma-endorphin concentrations were repeatedly measured, using an original radioimmunoassay, in patients with myocardial infarction. In the early days of acute myocardial infarction, high levels of this opioid peptide were observed, then plasma gamma-endorphin concentration gradually decreased by the time of discharge. In patients with grave complications, gamma-endorphin level was significantly lower, as compared to patients with uncomplicated infarction.
Naloxone partially inhibited skin wound contraction and completely blocked acceleration of wound healing in rats with stimulated lacrimal glands. Endorphins were detected in lacrimal glands. Alteration of functional activity of the lacrimal glands produces a considerable effect on pain sensitivity and endorphin blood concentration. Opioid peptides have a considerable effect on the functioning of the lacrimal apparatus and are involved in injury-induced reactions, regulating pain sensitivity, structural homeostasis and producing an anti-stress effect.
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.
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Pharmacokinetics of a new anti-ulcer drug, synthetic opioid hexapeptide dalargin (Tyr-D-Ala-Gly-Phe-Leu-Arg), which is an analogue of Leu-enkephalin, was studied in rats. Distribution and metabolism of 3H-Tyr-dalargin were examined after intravenous administration at a dose of 150 mg/kg. Main Tyr-containing metabolites of dalargin were detected and dynamics of their concentrations was evaluated in blood within 1 hr after administration. Kinetic curve of dalargin was described as three-exponential function.