Dimitry A. Kharkevich

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Transport of the hexapeptide dalargin across the blood-brain barrier was accomplished using a nanoparticle formulation. The formulation consisted of dalargin bound to poly(butyl cyanoacrylate) nanoparticles by sorption, coated with polysorbate 80. Intravenous injection of this formulation to mice resulted in an analgesic effect. All controls, including a(More)
Purpose. The possibility of using polysorbate 80-coated nanoparticles for the delivery of the water insoluble opioid agonist loperamide across the blood-brain barrier was investigated. The analgesic effect after i.v. injection of the preparations was used to indicate drug transport through this barrier. Methods. Loperamide was incorporated into PBCA(More)
The possibility of using polysorbate 80-coated polybutylcyanoacrylate nanoparticles to deliver low molecular polar hydrophilic drugs to the CNS has been studied. Tubocurarine (a quaternary ammonium salt) does not penetrate the normal intact blood-brain barrier. However, the injection of this drug directly into the cerebral ventricles of the brain provokes(More)
The comparative sensitivity of acetylcholine receptors of different skeletal muscles--m. masseter, m. gastrocnemius, m. triceps brachii, mm. obliquus et transversus abdominis, mm. intercostales, m. phrenicus to neuromuscular blocking agents was investigated. Experiments were performed on cats anesthetized with urethane (600 mg/kg, i.v.) and chloralose (70(More)
Clinical and experimental data indicate that the cerebral cortex plays an important role in pain perception and endogenous antinociceptive system function. Moreover, the enhancement of descending inhibitory cortical control may be involved in the mechanisms of analgetic effect of some agents. The present study was designed to investigate the effect of(More)
Thyrotropin-releasing hormone (TRH) was reported to stimulate respiration and abolish the respiratory depressant effect of morphine-like analgesics. Some TRH analogs which have a diminished hormonal activity may be of interest as potential non-specific opioid antagonists. The mechanism of this effect of TRH and its analogs is still unclear. Thus, in the(More)
The drug targeting to the brain by polysorbate 80-coated nanoparticles was studied. The leu-enkephalin analog dalargin was used as a model drug for investigating the drug penetration through the blood-brain barrier. The nociceptive threshold was measured by the tail flick test. The intravenous injection of dalargin bound by sorption to(More)
In a p reced ing communicat ion [1] a desc r ip t ion was given of a number of d i t e r t i a r y sa l t s of b i s (alkylamino) e s t e r s of a t r u x i l l i c acid, I, X = O , obtained for compara t ive tes t s of the i r c u r a r e l i k e ac t iv i ty . The compounds synthes ized we re d is t inguished by the d i s tance between the two cat ionic(More)