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The pharmacological activities of salsolinol (Sal) and salsoline (San) were compared by their abilities to displace 3H-dopamine and 3H-D-ala2-met-enkephalinamide from specific binding sites of rat striatal membrane preparations. Sal was more potent in receptor tests than San. Consequently, methylation by using catechol-O-methyltransferase is the process of its partial inactivation. Sal affinity for D3-receptors was higher than for opiate receptors (IC50 was 1.1 mumol/l for the former and 88 mumol/l for the latter). It was concluded that dopamine-like mechanisms of action of simple tetrahydroisoquinolines are possible to exist.

The authors studied combined action of ethanol, pyridoxine (3 mg/kg), and a mixture of thiamine (5 mg/kg), riboflavin (5 mg/kg), pyridoxine (3 mg/kg) and pantothenate (15 mg/kg) on the free amino acid reserve in the tissues of rats. Ethanol was given to the animals with a liquid semisynthetic diet (its calorific value comprised 36%) during 30 days. Both pyridoxine and the complex of vitamin B group produce normalizing action on the free amino acid pool by correcting the shifts induced by ethanol. It is especially manifested in the decreased levels of urea, isoleucine and GABA in the brain. The data obtained have shown that prevention with vitamins of shifts in the amino acid metabolism induced by ethanol, especially in respect to the central nervous system, should be recommended.

Mast cells of the gastric mucous membrane were assayed in 30 gastric cancer patients and in 190 patients with pretumor lesions of the stomach. For the control 208 patients were taken with functional gastric disturbances, chronic gastroduodenitis, of hypersthenic type, ulcerous disease of the duodenum and 30 practically healthy persons. It was stated that the development of chronic atrophic gastritis with the mucous membrane degeneration of intestinal type, a tendency to malignization of callous and persistently unhealed ulcers are preceded by degradation of mast cells, manifested in their reduction, considerable "rejuvenescence" and practically complete disappearance of mucopolysaccharide saturated mast cells. Analogous changes in mast cells were revealed in the mucous membrane of gastric cancer patients. It is suggested to use the morphometric criteria of mast cells as the criteria of pretumor lesions.

Sucralfate (55 patients), cimetidine (25 patients), ranitidine (30 patients), antacids and cholinolytics (32 patients) were studied and compared in open clinical trials for the efficacy in the treatment of ulcer disease of the stomach and duodenum. During 5 weeks, ulcers completely healed in 100% of the patients given sucralfate (in 94.5% for 4 weeks), in 90% of the patients treated with ranitidine, in 84% on cimetidine, and in 78% of the patients undergoing treatment with antacids and cholinolytics.

Using the method of competitive displacement of 3H-labelled naloxone, (D-ala2)-met enkephalinamide or (D-ala2)-D-leu-enkephalin by salsolinol, 1-methyl-6-hydroxy-1, 2, 3, 4-tetrahydro-beta-carboline or 1-methyl-6-methoxy-1, 2, 3, 4-tetrahydro-beta-carboline from opiate receptors, it was shown that the alkaloids studied were capable to cause specific interactions with rat hypothalamus and midbrain however, exhibiting distinctly less affinity as compared with morphine or its analogs. The sodium ratios, determined from the effective doses of the tetrahydroisoquinoline alkaloids corresponding to the alkaloid concentrations, which induce 50% displacement of 3H-naloxone from the opiate receptors in the presence or absence of 100 mM NaCl, have been found to be 0.75 for salsolinol and 3.6 for beta-carbolines studied. The data obtained suggest that salsolinol, similar to naloxone, is a "pure" morphine antagonist, whereas the beta-carbolines studied may be classified with the agonist-antagonist type. A considerable decrease in the affinity of mu-type opiate receptors has been found in presence of salsolinol in the incubation medium. The possible mechanisms of pharmacological action of the alkaloids and their relation to development of alcohol dependence and tolerance are discussed.

The content of free sulfhydril groups in yeast thiamine pyrophosphokinase (EC 2.7.6.2) was studied. Their blocking was found not to affect considerably the enzyme activity. N-bromsuccinimide developes the inhibitory effect only if taken in excessive concentrations, which indicates that tryptophane has no key position for the enzyme-substrate complex formation. On account of high speed of photoinactivation with Rose bengale and methilene blue, sigmoid dependence of activity loss on pH under irradiation, characteristic narrowing of the modified enzyme absorption spectrum, it is suggested that imidazole residue of the histidine is one of the functional groups of thiamine pyrophosphokinase.

A method is suggested for a quantitative determination of sulphydryl and imidazole groups in proteins. The method is based on the capacity of Zn2+ and Co2+ to bind selectivity with sulphur and nitrogen atoms in bioligands. The mentioned reactions are fixed by one of most sensitive methods of the electrochemical analysis, the inversiochronopotentiometric titration. The method was tested with the solutions of amino acids and proteins. The sensitivity of the method is 10(-8)M, a relative error is +/- 1.5%.

Histochemical and morphometric analysis of mast cells of the gastric and duodenal mucosa of rats given dyphenhydramine and suprastin for a long period of time (up to 45 days) revealed an increase in their functional activity that manifested in the enhancement of the processes of neoformation and maturation of juvenile mast cells and in the increased break down of mature cellular forms.

A decrease of alcohol intake by ethanol-preferring rats under free choice conditions after intraperitoneal administration of lithium chloride (35 mg/kg) was accompanied by an activation of aldehyde dehydrogenase in the brain stem, a decrease of dopamine and salsolinol levels in the striatum and normalization of 11-hydroxycorticosteroids contents in the blood and adrenal glands.