[Determination of free and bound phenol in urine during mass screening of the populace]. / Opredelenie svobodnogo i sviazannogo fenola v moche pri massovom obsledovanii naseleniia.

Quantitative estimation of phenol content in human urine involving Gibbs reagent was described in detail; the procedure was applied for screening test of people. The Gibbs reagent was synthesized from commonly available substances 2,6-dibromine-4-aminophenol and 4-nitrophenol. Estimation of total and bound forms of phenol was carried out in 0.5 ml of urine, while phenol conjugates were hydrolyzed by means of heating of urine samples containing 0.2 ml of 42% perchloric acid in boiling water bath and the phenol released was extracted by 3.0 ml of diethyl ether. Sensitivity of the procedure was about 0.1 micrograms of phenol in a sample, when microphotometer, applied in immunological studies, was used for measurement of optic density in the plates holes. Content of total phenol was estimated in urine of 15 children of 6-6.5 years old from Moscow using the procedure developed and it constitute from 2.5 micrograms/ml to 47.0 micrograms/ml, middle value was 9.5 micrograms/ml. In 47 children from Noyabrsk town these parameters constituted 1.5 micrograms/ml, 150 micrograms/ml and 19 micrograms/ml, respectively in adults - 1.5 micrograms/ml, 168 micrograms/ml and 167.7 micrograms/ml, respectively. The upper limit of the phenol normal concentration in urine was proposed to be as 50 micrograms/ml in screening test of people. Content of phenol in urine should be measured within a day during individual examination.

[Effect of N-(6-aminohexyl)-5-chloronaphthalene-1-sulfamide (W-7) and its analogs on the activity of soluble guanylate cyclase and on human platelet aggregation]. / Vliianie N-(6-aminogeksil)-5-khlornaftalin-1-sul'famida (W-7) i ego analogov na aktivnost' rastvorimoi formy guanilattsiklazy i agregatsiiu trombotsitov cheloveka.

The effect of N-(omega-aminoalkyl) derivatives of naphthalene-1-sulfamide on the activity of soluble guanylate cyclase and on human platelet aggregation at the first (reversible) step of the guanylate cyclase reaction was studied. Low (approximately 10(-7)-10(-6) M) concentrations of the above compounds were shown to stimulate the guanylate cyclase activity; some derivatives caused simultaneous inhibition of platelet aggregation induced by ADP. Some fragments of the chemical structure of the molecules responsible for the enzyme activity regulation in the tested systems were identified. The naphthalene-1-sulfamide derivatives carrying 6-aminohexyl or 8-amino-octyl groups of the sulfamide substituent as well as chlorine atom at positions 4 or 5 of the naphthalene ring appeared to be the most potent activators of platelet guanylate cyclase and inhibitors of platelet aggregation at the reversible step of the enzymatic reaction.

[Modulation of brain Ca2+-calmodulin-dependent phosphodiesterase activity by naphthalene sulfamides]. / Moduliatsiia fermentativnoi aktivnosti Ca2+-kalmodulin-zavisimoi fosfodiésterazy iz mozga soedineniiami naftalinsul'famidnogo riada.

Several W-7 analogs were synthesized. These compounds were shown to inhibit the calmodulin-activated phosphodiesterase. A comparative analysis of kinetic parameters of W-7 and its analogs was carried out. A hypothetical model of the effects of calmodulin inhibitors is proposed.