quantitative structure-activity relationship (qsar) models were employed for prediction the activity of p2x7 receptor antagonists. a data set consisted of 50 purine derivatives was utilized in the model construction where 40 and 10 of these compounds were in the training and test sets respectively. a suitable group of calculated molecular descriptors was selected by employing stepwise multiple ...

cardiovascular effects of opioid withdrawal have long been studied. it was reported that patients with underlying ischemic heart disease and atherosclerotic vessels may be complicated by a sudden physical and emotional stress due to withdrawal syndrome. but some other believes sudden increase in catecholamine level as a sympathetic overflow might effect on heart with and without underlying isch...

abstract fixed drug eruption (fde) is a unique type of cutaneous drug reaction that typically recurs in the identical locations on re-exposure to the attributed drug. fde is characterized by the appearance of a single or multiple sharply demarcated violaceous erythematous plaques which heal with residual hyperpigmentation. a 27-year-old woman presented with multiple dark patches over her eyelid...

in the present study, the effect of gaba (γ-aminobutyric acid) receptor agonists and antagonists on morphine-induced antinociception was investigated in formalin test in rats. intraperitoneal (i.p.) injection of different doses of morphine (1, 3, 6 and 9 mg/kg) and intracerebroventricular (i.c.v.) injection of different doses of muscimol (0.5, 1 and 2 g/rat) or baclofen (0.25, 0.5 and 1 g/rat) ...

Tachykinin NK2 receptor antagonists could reduce motility and symptoms during gastrointestinal diseases characterized by local inflammation such as diarrhea or colitis; however, how these conditions change pharmacodynamic and pharmacokinetic characteristics of NK2 receptor antagonists is unknown. We investigated the effect of the peptide NK2 receptor antagonist nepadutant on spontaneous intesti...

The susceptibility of E. coli and Salmonella to penicillin is highest in a basal medium devoid of amino acids. Blood serum in certain concentrations, meat infusion broth, yeast extract, and casein hydrolysate interfere with the penicillin activity. The effect is apparently due to the antagonism of certain amino acids in the materials. Dicarboxyl-monoamino acids (i.e. aspartic, glutamic, and hyd...

Dihydrofolate reductase (DHFR; tetrahydrofolate; NADP' oxidoreductase, EC 1.5.1.3) catalyses the NADPH-dependent reduction of 7,8-dihydrofolate (FAH,) to 5,6,7,8-tetrahydrofolate (FAH,). The coenzyme FAH, serves as a carrier of one-carbon fragments in a number of biosynthetic transfer reactions (Rader & Huennekens, 1973). It is apparent that DHFR is the intracellular target for the anti-cancer ...

Adrenocorticotropin (ACTH) acts via a highly selective receptor that is a member of the melanocortin receptor subfamily of type 1 G protein-coupled receptors. The ACTH receptor, also known as the melanocortin 2 receptor (MC2R), is unusual in that it is absolutely dependent on a small accessory protein, melanocortin receptor accessory protein (MRAP) for cell surface expression and function. ACTH...