[The synthesis of phosphates of long-chain omega-hydroxyalkyl esters of 11-deoxyprostaglandin E1]. / Sintez fosfatov dlinnotsepochechnykh omega-gidroksialkilovykh éfirov 11-dezoksiprostaglandina E1.

Di(p-methylbenzyl) phosphates of omega-hydroxyalkyl esters of 11-deoxyprostaglandin E1 were synthesized from disubstituted 1,10-decane and 1,22-docosane derivatives for studying permeability of bilayer membranes. The English version of the paper.

[Total synthesis and properties of prostaglandins. XXXVIII. Synthesis of 11-deoxyprostaglandin-E1 derivatives with amino acids and amines]. / Total'nyi sintez i svoistva prostaglandinov. XXXVIII. Sintez proizvodnykh 11-dezoksiprostaglandina-D1 s aminokislotami i aminami.

In order to study the physiological functions of 11-deoxyprostaglandin E1-alpha, a series of its amide derivatives with amino acids and some amines were synthesized using mixed anhydride technique. The myotropic properties of newly synthesized compounds were investigated.

[Total synthesis and properties of prostaglandins. XXXI. Synthesis of pyranylated and glycosidated omega-hydroxyalkyl ethers of 11- deoxyprostaglandin E1]. / Total'nyi sintez i svoistva prostaglandinov. XXXI. Sintez piranilirvannykh i glikozidirovannykh omega-gidroksialkilovykh éfirov 11-dezoksiprostaglandina E1.

Four methods of the synthesis of model glycosides with 11-deoxyprostaglandin E1 and a connecting polymethylene chain as the aglycone are compared. Interaction of potassium salt of prostaglandin PG with omega-iodoalkylglycosides is the most promising approach.

[Total synthesis and properties of prostaglandins. XXIV. Synthesis of glycerides with prostaglandin acyl residues]. / Total'nyi sintez i svoistva prostaglandinov. XXIV. Sintez glitseridov s prostaglandinovym atsil'nym ostatkom.

Synthesis of a number of model triglycerides and lysoglycerides bearing the acyl moieties of 11-deoxyprostaglandin E1, and palmitic acid residues has been carried out.

[Complete synthesis and properties of prostaglandins. X. Hydroxyl-containing esters of 11-deoxyprostaglandin E1]. / Polnyi sintez i svoistva prostaglandinov. X. Gidroksilsoderzhashchieéfiry 11-dezoksiprostaglandina E1.

Hydroxyl-containing 11-deoxyprostaglandin E1 esters were synthesised by using the methods of mixed anhydrides and nucleophilic displacement.

[Action of polymethylene-bis-quaternary compounds on the muscarinic and nicotinic cholinoreceptors]. / Deistvie nekotorykh polimetilen-bis-chetvertichnykh soedinenii na muskarinovye i nikotinovye cholinoretseptory.

The action of compounds with general formula (formula: see text) on the frog heart ventricle, cat blood pressure, guinea pig ileum and frog rectus abdominis was studied. With dioxolane radicals (type F-2268) a strong muscarinomimetic action on the cat arterial blood pressure and guinea pig ileum was observed, with maximum marked action at n = 10, which was more pronounced at an even than at odd number of methylene groups. On the frog heart the compounds with an odd number of "n" elicited an atropine-like action. The compounds with pentyl radicals produced no effect on blood pressure and a weak cholinolytic effect on the frog heart. On the ileum they exhibited a cholinomimetic effect. All compounds studied acted as noncompetitive cholinolytics on the frog rectus.

[A comparative study of the stereoselectivity of cholinoreceptors]. / Sravnitel'noe izuchenie stereoselektivnosti kholinoretseptorov.

Muscarine-sensitive cholinoreceptors (M-ChR) of higher vertebrates exhibit high stereoselectivity which is also revealed with respect to enantiomers of a very potent muscarinomimetic methyldilvasen (F-2268), the stereospecific index (SSI) being about 100. M-ChRs in the neuronal membrane of the gastropod mollusc Planorbarius corneus and in the hearts of the bivalve molluscs Mercenaria stimpsoni and Anadara broughtoni are highly sensitive to methyldilvasen (10(-9)-10(-10) M), but their sensitivity to its enantiomers is identical. In heart atria of the tortoise Testudo horsfieldi, frog Rana temporaria, and fishes Siluris glanis, Cyprinus carpio, as well as in ventricles of tadpoles, high SSI was revealed. These data are consistent with a hypothesis that during evolution of vertebrates no significant changes took place in the active center of M-ChR. Possibly, the lack of stereoselectivity in the investigated molluscan M-ChRs, together with their other peculiarities (they are not blocked by atropine), indicate "immaturity" of these receptors.

[Comparative findings on the stereoselectivity of cholinoreceptors]. / Sravnitel'nye dannye o stereoselektivnosti kholinoretseptorov

The potency of the optical isomers of the muscarinomimetic agent 2-methyl-4-dimethylaminomethyl-1.3-dioxolane methiodide (F-2268) was compared on cholinoreceptors, (ChR) of different animals. The greatest difference between optical isomers was observed on the muscarinic ChR of guinea pig ileum smooth muscle cis-L(+)isomer being more than hundred times as potent as cis-D(-)isomer. On the ChR of muscarinic type in the holothuria Cucumaria japonica retractor muscle, cis-L(+)isomer was 25 times as efficient as cis-D(-)isomer. On the ChR of sea urchin and sipunculid locomotor muscles, optical isomers differ only 3 to 5 times. There was no difference between the effect of optical isomers on the ChR of muscarinic type which mediate hyperpolarization in the neurones of the gastropod mollusc Planorbarius corneus. This suggest that some changes in ChR stereoselectivity may occur in the course of evolution.

[Pharmacokinetics of dioxonium]. / Farmakokinetika dioksoniia

An investigation in the pharmacokinetics of a new peripheral muscle relaxant dioxonium and of its carbon-labeled analogue (with respect to the N-methyl groups) was carried out. An intravenous administration of dioxonium-C14 was found to bring about a biphasic change in radioactivity of the blood plasma. The stoppage of curarization, irrespective of a dioxonium dose, is seen to occur at a definite radioactivity level in the blood plasma. Major radioactivity following introduction of dioxonium-C14 is observed in the organism of the rats in the skeletal muscles and in the kidneys. The drug is eliminated from the organism through the kidneys in an unchanged and pharmacologically active form.