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The problems with separation of amino acid mixtures in reversed-phase mode are the result of their hydrophilic nature. The derivatisation of the amino group of mentioned above solutes leads to their solution. For this purpose, 9-fluorenylmethoxycarbonyl chloroformate (f-moc-Cl) as the derivatisation reagent is often used. In our study, the separation of some f-moc- amino acid derivatives (alanine, phenylalanine, leucine, methionine, proline and tryptophan) with the use of micellar systems of reversed-phase high-performance thin-layer chromatography (HPTLC) and pressurized planar electrochromatography (PPEC) is investigated. The effect of surfactant concentration, its type (anionic, cationic and non-ionic) and mobile phase buffer pH on the discussed above solute migration distances are presented. Our work reveals that the increase of sodium dodecylsulphate concentration in the mobile phase has a different effect on solute retention in HPTLC and PPEC. Moreover, it also affects the order of solutes in both techniques. In PPEC, in contrast to the HPTLC technique, the mobile phase pH affects solute retention. The type of surfactant in the mobile phase also impacts solute retention and migration distances. A mobile phase containing SDS improves system efficiency in both techniques. Herein, such an effect is presented for the first time.

Three series of new unsubstituted or 2-acyl 1,2,3,4-tetrahydro-beta-carbolines (THBC), connected to 1-(o-methoxyphenyl)piperazine by 2-, 3- or 4-membered alkylene spacer (3, 4 or 5, respectively) in position 9, were synthesized and their 5-HT1A/5-HT2A receptor affinities and functional in vivo activities were investigated. Radioligand binding studies showed that unsubstituted (a) and acyl (b-f) derivatives with prop-1,3-ylene (4) and particularly with but-1,4-ylene (5) spacer had a high 5-HT1A receptor affinity (Ki = 30-110 nM), whereas the 5-HT1A affinity of derivatives with ethylene spacer (3) was low. All those compounds (except 5c, Ki = 44 nM) did not distinctly bind to 5-HT2A receptors. The obtained results indicated that the length of an alkylene chain was a crucial parameter for determining 5-HT1A receptor affinities of the tested compounds, while acyl substituents in position 2 of THBC were not important for their 5-HTIA/5-HT2A activities. It was also demonstrated that the few selected compounds (4d, 5a-c and 5e) with the highest affinity (Ki up to 50 nM) for 5-HT1A receptors, administered at doses of 10-20 mg/kg, behaved like antagonists of postsynaptic 5-HT1A receptors, as they reduced the 8-OH-DPAT (5-HT1A agonist)-induced lower lip retraction and behavioral syndrome in rats. Moreover, 4d seemed to be an agonist of presynaptic 5-HT1A receptors, since the hypothermia induced by its administration was attenuated by WAY 100635 (5-HT1A antagonist). Compound 5c, 5-HT2A receptor ligand, demonstrated an antagonistic activity, as it inhibited the (+/-)DOI (5-HT2A agonist)-induced head twitches in mice. The obtained results of in vivo studies suggest that introduction of different acyl substituents in position 2 of THBC with propylene or butylene spacer between tricyclous and arylpiperazine moiety is insignificant for the postsynaptic 5-HTIA receptor activity of the compounds tested in vivo. On the other hand, only compound 5c with an acryloyl group and a butylene chain behaved like a 5-HT1A/5-HT2A antagonist.

A series of 1-¿omega-(4-aryl-1-piperazinyl)alkyl]indolin-2(1H)-one derivatives 2-14 was synthesized in order to obtain ligands with a dual 5-HT1A/5-HT2A activity. The majority of those compounds (2-5, 7, 10-13) exhibited a high 5-HT1A (Ki = 2-44 nM) and/or 5-HT2A affinity (Ki = 51 and 39 for 5 and 7, respectively). Induction of lower lip retraction (LLR) and behavioral syndrome and inhibition of these effects evoked by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) were used for determination the agonistic and antagonistic activity, respectively, at 5-HT1A receptors. The 5-HT2A antagonistic activity was assessed by the blocking effect on the head twitches induced by (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) in mice. Two of the tested compounds, 1-¿3-[4-(3-chlorophenyl)-1-piperazinyl]propyl¿-6-fluoroindolin-2(1 H)-one (5) and 1-¿3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl¿indolin-2(1H)-one (7), demonstrated a high 5-HT1A/5-HT2A affinity and an in vivo antagonistic activity towards both receptor subtypes.

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.

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.

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.

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.

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.

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.

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.

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.

Four new derivatives of 1,2,3,4-tetrahydro-beta-carboline 2a--d were synthetized with the pyridoxal moiety in position 1; there were also obtained four Schiff bases 1a--d which are intermediate products in this synthesis. Schiff bases 1a--d revealed a sedative and analgesic action, and compound 1b also had potential antidepressive properties. The derivatives of tetrahydro-beta-carboline 2a--d were inactive in the carried out tests.

Eight amide compounds were obtained by condensation of appriopriate acid chlorides with homotryptamine and its 5-methoxyderivative. The effects of these compounds on the central nervous system were tested. m-Nitrobenzoylhomotryptamine showed the strongest sedative, anticonvulsive and analgesic properties.

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.

By modifying the method of Abramovitch for preparation of tryptamine, a way to obtain N-acyl derivatives of tryptamine 3a-g without the necessity of isolating free tryptamine was found. The hydrolysis of the appropriate acyl derivatives gave 5-nitro- and 5-benzyloxytryptamines.

Five derivatives of 2-(3-aminopropionyl)-1-(3-pyridyl)-1,2,3,4-tetrahydro-beta-carboline (2a-e) were obtained, which yielded, as a result of reduction with LiAlH4, five respective 2-aminopropyl-derivatives (3a-e). Pharmacological studies revealed that phenylpiperazine-derivatives 2d, 2e, 3d and 3e have sedative and analgesic properties. All compounds are devoided of neuroleptic, antidepressant, anxiolytic and antiparkinsonic activity.

N-Nicotinoyl-tryptamine was synthetized by acylation of tryptamine with mixed nicotinic anhydride. The synthesis of tryptamine via DL-tryptophan decarboxylation in cyclohexanol, in the presence of tetraline oxidation products as the catalyst, was described as well.

A series of aminoalkylderivatives of 1,2,3,4-tetrahydro-beta-carboline-1-spiro-4'-N'-benzylpiperidine were synthesized by means of chloroacetylation of the title compound and substitution of chlorine atom with various heterocyclic amines in DMSO, followed by LAH reduction of the carbonyl group. Of the ten tested compounds (4a-4e, 5a-5e), compound 5d given ip, but not orally, showed an anxiolytic activity in the four-plate test in mice and in the conflict test in rats. Compound 5d is devoid of an anticonvulsant or neurotoxic action. The activity of compound 5d resembles this of buspirone.

Ten cyclic animals (1-10), including a form of decahydro-5H-pyrido [1',2';5,1] imidazo [3,4-a]-beta-carboline, were obtained by treating erythro 1-(2'-piperidyl)-1,2,3,4-tetrahydro-beta-carboline with aldehydes. The anticonvulsant action of those compounds (1-10) was investigated in mice using a behavioral test. Only 5-(3-chlorophenyl) (2) and 5-(3-pyridyl) (9) derivatives showed an anticonvulsant activity in the electric seizure test, but their therapeutic index was inferior to that of phenytoin.