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A set of 36 arylpiperazine derivatives with two novel complex terminal imide fragments, 8,11-dimethyl-3,5-dioxo-4-azatricyclo[5.2.2.0(2,6)]undec-8-en-1-yl acetate and 1,11-dimethyl-4-azatricyclo[5.2.2.0(2,6)]undecane-3,5,8-trione, were synthesized and tested for their affinity for 5-HT(1A) and 5-HT(2A) receptors. The Fujita-Ban analysis showed that the influence of structural modifications on the affinity for both receptor subtypes is additive and that the activity of similar compounds could be predicted with high accuracy. Compounds 46, 48 and 18 out of 14 screened in a functional model of anxiety and depression demonstrated antidepressant activity in the forced swimming tests in mice, and were devoid of neurotoxic effects (chimney test in mice).

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The preparation of a number of derivatives of dibenzo[e.h]bicyclo[2.2.2]octane -2.3-dicarboximide with an expected anxiolytic activity.

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The preparation of a number of derivatives of 1-ethoxybicyclo[2.2.2]-oct-5-one-2,3-dicarboximide with potential anxiolytic activity has been described. The aim of our study was to obtain new analogs of tandospirone.

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The preparation of a number of derivatives of 1,2,3,4,7-pentamethylbicyclo[2.2.1]hept-2-ene-5,6-dicarboximide with potential anxiolytic activity has been described. The aim of our study was to obtain new analogues of tandospirone, that is derivatives of cyclic imides [1].

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The preparation of a number of derivatives of dibenzo[e.h]bicyclo[2.2.2]octane-2.3-dicarboximide with an expected anxiolytic activity.

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The preparation of a number of derivatives of dibenzo[e.h]bicyclo[2.2.2]octane-2.3-dicarboximide with an expected anxiolytic activity.

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The preparation of a number of derivatives of 1-methoxybicyclo[2.2.2]-oct-5-ene-2,3-dicarboximide possessing an expected anxiolytic activity has been described.

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The preparation of a number of derivatives of N-hydroxy-1,4-dimethyl-dibenzo[e.h]bicyclo[2.2.2]octane-2,3dicarboximide with a potential activity on central nervous system has been described.

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The preparation of a number of new N-substituted derivatives of 7-diphenylmethylenebicyclo[2.2.1]hept-2-ene-5,6-dicarboximide with an expected anxiolytic activity.

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Preparation of a number of derivatives of 1-methyl-5-oxobicyclo[2.2.1]heptane-2,3-dicarboximide with a potential anxiolytic activity has been described. New analogs of Tandospirone i.e. derivatives of bicyclo[2.2.1]heptane (10), were aimed at.

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Continuing our studies connected with the design of new anxiolytics we have now synthesized a series of new compounds, derivatives of 7,8-benzo-1,3-diazaspiro[4,5]decane-2,4-dione bearing a 4-aryl-1-piperazinylbutyl group attached to the imide nitrogen. One single compound was submitted to the 5-HT1A receptor binding assay and found to display the expected--though rather weak--receptorial affinity.

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In continuation of the development of antipsychotic and anxiolytic agents with a reduced propensity toward extrapyramidal side-effects, a series of N-aminoalkyl derivatives of (s)-(+)-2,3-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11-(10H, 11aH)-dione was prepared. Evaluation of these compounds in revealed a very low affinity for 5-HT1A receptor.

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The preparation of N-substituted cyclic imides N-[4-[(4-aryl)-1-piperazinyl]alkyl]-5,7-dioxabicyclo[2.2.2]octane- 2, 3-dicarboximides by condensation of N-(3-chloropropyl)- or N-(4-chlorobutyl)imides with appropriate amine has been described. One of compounds was tested in the Vogel's test and displayed an expected activity on CNS.

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Intrauterine insemination with husband's sperm (IUI) is offered to couples with infertility due to various causes although there is no general agreement on which of these causes should be so treated. In this report 77 couples were diagnosed as having either cervical factor, male factor, immunological factor or unexplained infertility. Insemination was performed 24-32 hours after a rapid rise in the serum LH level. Two of 16 pregnancies which resulted miscarried, 1 was ectopic and the remainder were full term. Eleven occurred in the cervical factor group, 3 in the immunological factor and only 1 in each of the male factor and unexplained infertility groups. The differences in the number of pregnancies between the cervical factor and male and unexplained infertility groups are significant but not between the groups with cervical and immunological factors. The majority of pregnancies (81%) were achieved in the first 4 cycles. Patients with the cervical factor as the cause of their subfertility are likely to benefit from the IUI with their husband's sperm. The small number of patients with the immunological factor in this study does not allow for a conclusion. In our experience the male factor and unexplained infertility patients are unlikely to benefit from intrauterine insemination with husband's sperm.

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Synthesis of 8-hydroxy-7-methoxy-2H-1-benzopyran-2-one and syntheses of several 8-(3-amino-2-hydroxypropoxy)-7-methoxy-2H-1-benzopyran-2-one derivatives with antiarrhythmic activity is described.

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The report is based on a material of 45 patients with 54 ureteral damages after obstetric-gynaecological operations. In 30 cases nephrostomy was done and the operation on the ureter was delayed, while 24 ureters were operated on immediately after establishing of the diagnosis. The authors are proponents of early operations. The results of these operations are better, the patients recover earlier regaining fitness, and additional procedure, nephrostomy, is avoided.

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