[Molecular aspects of pharmacological activity of naltrexone and naloxone].

Naltrexone and naloxone, being competitive antagonists of opioid receptors, have found therapeutic applications in medicine. The experiments with mutant receptors showed that many amino acid residues within transmembrane domains play an important role in binding these drugs. Using the site-directed mutagenesis technique, it was established that even single mutations (replacing single amino acid residues) can significantly modify the affinity of antagonists to receptors, sometimes even imparting agonist-like properties to the compounds studied.

[Neurochemical basis of ultra rapid opioid detoxication].

Ultra rapid opioid detoxification (UROD) is a new technique with the use of mu-opioid receptor antagonists to precipitate withdrawal. The scientific literature on UROD techniques in opiate addicts are reviewed, but little has been published on its neurochemical aspects. It is discussed that exposure to naloxone ore naltrexone during UROD is associated with development of increasing in opioidergic neurotransmission.

[Anti-inflammatory effect of fensulkal].

Experiments on various animals showed that fensulkal, a new phenylglyoxylic acid derivative, possesses a high antiinflammatory activity and low toxicity, markedly exceeding butadion in the therapeutic index. The mechanism of the antiphlogistic effect of fensulkal is due to its antagonism with respect to mediators of the inflammatory process and the ability of suppressing the increased permeability of capillaries and is partly related to the adrenal cortex. The drug is registered and recommended for application as antiinflammatory remedy in the form of ointment to be used for the treatment of some gynecological disorders.

[Effect of synthetic fragments of thymic peptide hormones on learning and memory processes].

Seven synthetic peptide fragments of thymic hormones were investigated using behavioral and electrophysiological methods. Splenopentin was shown to increase markedly learning capacities and memory. In contrast, alpha 1-thymosin fragment decreased them.