A series of 6- and 7-substituted-2-arylpyrazolo[4,3-c]quinolin-3-ones was synthesized and tested in vitro for binding with the benzodiazepine receptor in competition with [3H]flunitrazepam. Electronic parameters (molecular electrostatic potential (MEP), charge distribution on the nitrogen atoms, dipole moment mu, and ionization potential (IP)) were calculated for the compounds by semi-empirical quantum chemistry methods. Lipophilicity of the compounds, expressed as logarithm of the octanol-water partition coefficient (log P), was calculated by the program Pallas. A quantitative correlation of the biological data with molecular parameters revealed a significant dependence (r = 0.95) of the activity on hydrophobic constants of the substituents, log P, and magnitude of the MEP minimum associated with the carbonyl oxygen atom.

Binding, Competitive↗

PubMedDate not supplied

[Characteristics of a target population for preventing house-dust mite allergy in toddlers].

AIM: To evaluate a recruitment strategy to identify high risk toddlers for a programme of prevention of allergy. For screening, parents were asked to participate in our study by information form and screening questionnaire on the occasion of routine check-up visits of toddlers scheduled between 20 and 48 months of age in four paediatric practices. As a next step, readiness of parents for implementation of preventive measures was confirmed. METHOD: Inclusion criteria were age between 20 and 48 months and a positive atopic family history (evaluated by 5 questions regarding asthma, allergic rhino-conjunctivitis and atopic dermatitis) of parents or siblings. This was confirmed by sensitization to an environmental allergen (skin prick test (SPT)) in at least one parent. If these inclusion criteria were fulfilled, the toddlers were randomly allocated to the intervention and control group of the prevention programme. RESULTS: 111 of 175 screening questionnaires (63.4 %) were returned. In 76.6 % (n = 85) of these 111 questionnaires a positive atopic family history (mother, father, sibling) was noted. All inclusion criteria were fulfilled by only 43 toddlers (age: median 33.6 months, 5-95 % quantile: 21.6-48 months). Based on the positive screening questionnaire, history of atopy was confirmed by positive SPT in 70.0 % of fathers and 77.8 % of mothers. Despite a negative screening questionnaire, history of atopy was detected by a positive SPT in 11.1 % of mothers and 47.4 % of fathers. Detection of specific IgE against house-dust mite in 9 of 18 serum samples revealed the risk for allergy of the toddlers. A re-evaluation after three months showed that all the elements of the prevention programme as well as the recommendations for the control group had been almost completely accepted by all the families concerned practically without any reservations. CONCLUSION: The recruitment of toddlers with high risk for developing allergy turned out well and could be validated. The prevention programme was readily accepted by the families and thus can be used for a larger study.

Antigens, Dermatophagoides↗

PubMedDate not supplied

[COX-2-expression in extragenital endometriosis lesions as a novel therapeutical approach?].

OBJECTIVE: Extragenital endometriosis is a rare form of endometriosis. Due to its invasive and metastatic properties it resembles some features of malignant tumours. Cyclooxygenase (COX)-2 is a rate-limiting enzyme in the biosynthesis of prostaglandins and is mainly expressed in inflammatory and malignant processes. In this study we investigated the COX-2 expression in extragenital endometriosis. MATERIAL AND METHODS: Tissue was obtained of 13 women with rectal and vaginal endometriosis, scar endometriosis and endometriosis of the omentum majus. The COX-2 expression was investigated by immunohistochemistry. RESULTS: In the glandular epithelium a COX-2 overexpression was found in all cases and in the stroma a weak to moderate COX-2 expression was found in half of the cases. A hormonal therapy at the time of surgery had no influence on the COX-2 expression in extragenital endometriosis. CONCLUSION: The high COX-2 expression in extragenital endometriosis is believed to be strongly correlated with the pathological abnormalities this of disease.

Cyclooxygenase 2↗