Synthesis and pharmacologic properties of pyridoyl derivatives of 3-methylaminoindole 2-methyltryptamine and isotryptamine.

Six new pyridoyl derivatives of 3-methylaminoindole, 2-methyltryptamine and isotryptamine were synthesized by condensation with chlorides of nicotinic and isonicotinic acids. The central action of these compounds seems to depress the central nervous system, as they reduce spontaneous motility (I, II, IV, V, VI) and amphetamine hypermotility (II, IV, V), prolong hexobarbital sleeping time (II, IV, V, VI), display analgesic action in the "writhing test" (all compounds) and in the "hot plate test" (IV, V). The compounds do not change body temperature and display no anticonvulsant action.

4-Aryl-1-piperazinylalkyl derivatives of 1,2,3,4-tetrahydro-beta-carboline ring system. Synthesis and preliminary in vivo studies.

Three series of compounds containing a 4-aryl-1-piperazinylalkyl fragment attached to a different position of the indole (A) or 1,2,3,4-tetrahydro-beta-carboline (B, C) have been prepared. The quantitative relationship between the structure of some derivatives and their sedative effect was found using the Free-Wilson approach.

Structure-activity relationship studies of CNS agents. Part 4: 2-[3-(4-aryl-1-piperazinyl)propyl]-1,2,3,4-tetrahydro-beta-carbolin+ ++ -1-one derivatives as potential central anti-serotonin agents.

Seven derivatives of 1,2,3,4-tetrahydro-beta-carbolin-1-one have been prepared. Three of them showed significant central anti-serotonin activity, comparable with that of trazodone or etoperidone. Some structural features were found to be important for the central antiserotonin activity of the investigated class of compounds.

Structure-activity relationship studies of CNS agents. Part 1: The Free-Wilson analysis of acute toxicity and sedative effect of some 1,2,3,4-tetrahydro-beta-carbolines.

It has been found that 3-alkoxycarbonyl-beta-carbolines are almost non-toxic and showed a sedative effect. The quantitative relationship between the structure of some 1,2,3,4-tetrahydro-beta-carbolines and their acute toxicity and sedative effect was found using the Free-Wilson approach.

Structure-activity relationship studies of CNS agents. Part 9: 5-HT1A and 5-HT2 receptor affinity of some 2- and 3-substituted 1,2,3,4-tetrahydro-beta-carbolines.

The 5-HT1A and 5-HT2 receptor affinity of 2- and 3-substituted 1,2,3,4-tetrahydro-beta-carbolines 1-8, 10 and 12-15 has been determined. It has been found that the specific 5-HT1A affinity of the protonated form (KiAH+) 2-n-hexyl derivatives 4, 8, 14 and (+)-LSD is of the same order. It has been shown by means of molecular modelling methods that pharmacophores of all the active compounds can adopt a common position at the 5-HT1A receptor model. The model also offers an explanation for the observed stereoselectivity chiral compounds.

5-HT1A and 5-HT2A receptor affinity and functional profile of some N-[3-(4-aryl-1-piperazinyl)propyl] derivatives of indolin-2(1H)-one, quinolin-2(1 H)-one and isoquinolin-1(2H)-one. Part 30: Structure-activity relationship studies of CNS agents.

A series of new 1-aryl-4-propylpiperazines containing the modified terminal amide fragment 9, 15-19, 21, 23 and 25 were synthesized and their 5-HT1A and 5-HT2A receptor affinities were determined. All the compound were highly potent 5-HT1A receptor ligands with a diverse 5-HT2A receptor affinity. It was found that the 5-HT2A receptor affinity depends on the dipole moment and lipophilicity of amide moiety. Compound 9b was found to be a 5-HT2A receptor antagonist and a weak 5-HT1A receptor agonist.

[Various lipid components in the serum of alcoholics]. / Zachowanie sie niektórych skladników lipidowych w surowicy krwi u osób naduzywajacych alkoholu.

In a group of 57 alcoholics, patients of disaccustoming ward, and a group of 61 controls the level of adipose bodies in blood serum was determined. The comparison showed a significantly higher level of cholesterol and triglycerides in alcoholics than in controls. Other lipid components, beta lpoproteides, total lipids and fatty acids exhibited similar values in both groups. The authors analyse, basing on a survey of literature, the expected mechanism of changes responsible for disturbed metabolism of fats in chronic alcoholism.

[Local use of cyclosporin in nonbacterial corneal ulceration]. / Miejscowe zastosowanie cyklosporyny w niebakteryjnych owrzodzeniach rogówki.

The authors present the results of local use of cyclosporin solution in 6 patients with corneal ulcerations occurring in Sjögren disease, rheumatic disease and after corneal transplantation. The ulceration was healed in all patients. The cyclosporin, locally applied, has no side effects and may be an efficient way in the treatment of some immunological diseases of cornea.

[Examination of the visual system in boxers]. / Badania ukladu wzrokowego zawodników klubów bokserskich.

Ophthalmological examinations were performed in 139 boxers. They showed that the injuries concerned most frequently the ocular adnexa and not the eye globe itself. Only two contestants who practiced boxing for more than 10 years exhibited peripheral opacities of the lens and pale foci with shifting of the pigment at the fundus periphery connected with a deepening of the filtration angle; this could be caused by a contusion of the eye. It was demonstrated that the introduction of safety helmets distinctly reduced the number of eye injuries in boxing.