Inhibition of monoamine oxidase-B by 5H-indeno[1,2-c]pyridazines: biological activities, quantitative structure-activity relationships (QSARs) and 3D-QSARs.

A large series (66 compounds) of indeno[1,2-c]pyridazin-5-ones (IPs) were synthesized and tested on their monoamine oxidase-A (MAO-A) and MAO-B inhibitory activity. All of the tested compounds acted preferentially on MAO-B displaying weak (nonmeasurable IC50 values) to high (submicromolar IC50 values) activities. The most active compound was p-CF3-3-phenyl-IP (IC50 = 90 nM).

Inhibition of monoamine oxidase by isoquinoline derivatives. Qualitative and 3D-quantitative structure-activity relationships.

A series of isoquinolines, N-methyl-1,2-dihydroisoquinolines, N-methyl-1,2,3,4-tetrahydroisoquinolines, 1,2,3,4-tetrahydroisoquinolines, and N-methylisoquinolinium ions were tested as inhibitors of monoamine oxidases A and B. All compounds were found to act as reversible and time-independent MAO inhibitors, often with a distinct selectivity towards MAO-A. As a class, the N-methylisoquinolinium ions were found to be the most active MAO-A inhibitors, with N-methyl-6-methoxyisoquinolinium ion emerging as a potent (IC50 = 0.

[Psychotic women and their children].

With desinstitutionalization, the social life of psychiatric patients and particularly that of psychotics has arisen in new terms over the past twenty years. In particular, relationships and sexuality of these patients are manifest realities to which few studies are devoted. 61 schizophrenic and 21 bipolar women (18-45 years of age, mean 34 in-or outpatients) were interviewed with a battery of instruments (PANSS, Carpenter's criteria of schizophrenia with deficit syndrome, axis V of DSM-III-R) and with a semi-structured questionnaire related to clinical data, sexuality, relationships, children and motherhood.

Sexual victimization in women with schizophrenia and bipolar disorder.

Exposure of populations with psychosis to traumatic events (among them sexual trauma) has seldom been studied. In addition, the clinical features developed by victims with psychosis after a traumatic event are rarely taken into account. Sixty-four women with schizophrenia and 26 women with bipolar disorder (DSM-III-R diagnosed, 18-45 years, inpatients and outpatients) were interviewed using a clinician-rated battery of instruments, including a semi-structured questionnaire concerning sexual victimization and its impact.

[Role of psychiatry in the preoperative phase of facial reconstructive surgery].

Nowadays, the place of psychiatrist is currently admitted in facial plastic surgery, but is still discussed in reconstructive surgery. This page will stress the importance of a cooperation between surgeon and psychiatrist, preoperatively in orthognathic surgery. After a brief review of literature, we will try to precise when psychiatrist's advice would help, preoperatively, maxillofacial surgeon.

X-ray crystal structure, partitioning behavior, and molecular modeling study of piracetam-type nootropics: insights into the pharmacophore.

To detect possible molecular determinants of amnesia-reverting activity, the conformational properties of a number of rigid and flexible piracetam-type cognition enhancers have been assessed by X-ray diffraction, NMR spectroscopy, and ab initio and high-temperature-quenched molecular dynamics (QMD) calculations. The structures of the preferred conformers in solution derived from 1H-NMR spectral analysis were in good agreement with those found by QMD calculations. Interestingly, the calculation of the average molecular lipophilicity potential on the water-accessible surface of the selected conformers was helpful in interpreting the partitioning behavior observed by measuring octanol-water partition coefficients and capacity factors in reversed-phase high-performance liquid chromatography.

[Psychological trauma and mental disorders].

Fifty-eight female impatients consecutively hospitalized in the University Hospital Department of Psychiatry in Tours were interviewed with a clinician battery of instruments (among them, the SI-PTSD by Davidson). The diagnoses leading to hospitalization were: severe disorders of psychotic type (schizophrenic, schizophreniform, schizo-affective, schizoid and paranoid delusional disorders as well as bipolar disorder), borderline and narcissistic personalities for 7%, and other disorders for 53%. Among the results, we observed that 59% of these patients had experienced at least one major stressful event (rape 26%, other sexual assault 29%, physical assault 31%, seeing somebody dying in a violent way 8%, war scene 2%, injured in an accident 2%).

ECG activity in the sleep of insomniac patients under the influence of lormetazepam and zopiclone.

The influence of the benzodiazepine hypnotic lormetazepam (1 mg) and the cyclopyrrolone hypnotic zopiclone (7.5 mg) on heart rate activity was studied in 16 elderly insomniacs in a placebo-controlled, randomised, 3-fold crossover trial. After digital preprocessing of the ECG, QRS complexes were automatically recognised by a detection technique based on adaptative thresholds.

[Treating psychic traumas: a psychiatric emergency].

Interest for the psychopathological field of trauma has experienced a revival over the last fifteen years. Early and active treatment of victims is necessary to attenuate the psychopathological consequences of trauma. However, emergency psychiatry still rarely places a high value on it.

Molecular lipophilicity potential, a tool in 3D QSAR: method and applications.

A new method is presented to calculate the Molecular Lipophilicity Potential (MLP). The method is validated by showing that the MLP thus generated on the solvent-accessible surface can be used to back-calculate log P. Because the MLP is shown to be sensitive to conformational effects, the MLP/log P relation is best sought by taking all conformers into account.

Topographical characterization of normal visual evoked responses.

A study of visual evoked responses in a normal population was carried out using a high-precision programmable stimulator and an innovative brain mapping system which presents the overall activity on a three dimensional surface representing the human head. The interpolation method used gives a more precise computation of the potential value between electrodes. Two normal distributions of visual responses are presented which were identified while trying to topographically characterize visual evoked responses in order to construct a comparative data base.

Automatic analysis of sleep using two parameters based on principal component analysis of electroencephalography spectral data.

A computer program for the analysis of a sleep electroencephalogram (EEG) is presented. The method relies on two steps. First, a spectral analysis is performed for signals recorded from one or more electrode locations.

Three dimensional representation of brain electrical activity.

Brain topography mapping is a useful technique for the representation of electrical activity recorded on the scalp. It clarifies spatial and temporal relationships between different cortical areas. In this work we propose a system which includes several enhancements over those previously proposed, such as an optimised interpolation method and a three dimensional reconstruction of maps.

The submental island flap: a new donor site. Anatomy and clinical applications as a free or pedicled flap.

This paper describes the use of a new island flap based on the submental artery. Previously described cervical flaps have inherent problems ranging from limited mobility to unacceptable donor-site scars, to unpredictable outcomes. The flap design and technique were studied on 20 fresh cadavers and 8 patients who underwent radical neck dissections.

Effects of solvation on the ionization and conformation of raclopride and other antidopaminergic 6-methoxysalicylamides: insight into the pharmacophore.

Previous work has shown that raclopride in water at neutral pH exists in a zwitterionic form, suggesting a stereoelectronic structure largely different from that of other benzamides. In the present study, the acid-base behavior of other 6-methoxysalicylamides is shown to be comparable to that of raclopride. An extensive investigation by high-temperature molecular dynamics gave insight into the conformational behavior of neutral and zwitterionic raclopride in vacuum and in water.

Quantitative structure-metabolism relationship analyses of MAO-mediated toxication of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine and analogues.

The 1-octanol/water partition coefficients of a number of toxic and nontoxic analogues of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) were determined using centrifugal partition chromatography (CPC), a novel and effective technique for measuring lipophilicity, and found to be highly correlated with values calculated by a fragmental method. Some conformational properties of these compounds were also assessed by molecular mechanics calculations and 1H-NMR spectroscopy. A quantitative structure-metabolism relationship (QSMR) study of MPTP and analogues based on literature data was undertaken in order to determine the key features eliciting MAO-A and MAO-B reactivity and selectivity and influencing toxication.