A phase I study was performed of CGS 20267, an oral nonsteroidai, highly potent, and selective aromatase inhibitor, in 21 postmenopausal patients with advanced breast cancer. The patients were recruited in 3 successive groups of 7, receiving 0.1, 0.5, and 2.5 mg p.oJday, respectively. All patients had received at least one prior endocrine treatment (range, 1-4), and six patients had received pr...

Sexual behaviors in green anoles are regulated by steroid hormones. Androgens activate the display of masculine courtship and copulatory behaviors, and estradiol activates feminine receptivity. Testosterone can also facilitate receptivity in females. The present study was conducted to test the role of converting testosterone to estradiol (aromatization) in the regulation of sexual and aggressiv...

Upregulation of aromatase (estrogen synthase) in glia around the site of neural injury may limit neural degeneration. Systemic administration of estrogen limits neural damage, but the specific role of local estrogen provision in this effect is unclear. In male zebra finches, we tested the effect of local aromatase inhibition and estrogen replacement on type of cellular degeneration and the dist...

a rapid, specific and accurate proton quantitative nuclear magnetic resonance spectroscopic (1h qnmr) and also a reversed phase derivatization hplc method have been developed to quantify a toxic, uv-visible inactive and non-volatile impurity n,n-dimethylamine hydrochloride (dma∙hcl) in metformin hydrochloride (mf∙hcl), an active pharmaceutical ingradient. the method is based on proton quantitat...

Chronic allograft injury (CAI) is a major cause of late graft failure with a multifactorial pathogenesis; however, in different experiments an inhibition of the renin-angiotensin system by angiotensin-converting enzyme inhibitors and angiotensin II type 1 receptor blockers ameliorated the progression of chronic renal disease. Different concepts supposed that aldosterone is involved in developme...

Recent evidence has implicated steroid hormones, specifically estrogens, in the rapid modulation of cognitive processes. Songbirds have been a useful model system in the study of complex cognitive processes including birdsong, a naturally learned vocal behavior regulated by a discrete steroid-sensitive telencephalic circuitry. Singing behavior is known to be regulated by long-term actions of es...

Estradiol is converted to catechol estrogens via 2- and 4-hydroxylation by cytochrome P450 enzymes. 4-Hydroxyestradiol elicits biological activities distinct from estradiol, most notably an oxidant stress response induced by free radicals generated by metabolic redox cycling reactions. In this study, we have examined 2- and 4-hydroxylation of estradiol by microsomes of human uterine myometrium ...

A mixture of acetaminophen, diphenhydramine hydrochloride and pseudoephedrine hydrochloride is used for the symptomatic treatment of common cold. In this study, a derivative spectrophotometric method based on zero-crossing technique was proposed for simultaneous determination of acetaminophen, diphenhydramine hydrochloride and pseudoephedrine hydrochloride. Determination of these drugs was perf...

Buprenorphine is a partial mu agonist and kappa antagonist which is used for the treatment of pain and opioid addiction. A mixture of buprenorphine hydrochloride and naloxone hydrochloride has been approved for the treatment of opioid dependence.In this study a third order derivative spectrophotometric method based on zero-crossing technique has been used for the simultaneous determination of b...

Reducing aldosterone action is beneficial in various major diseases such as heart failure. Currently, this is achieved with mineralocorticoid receptor antagonists, however, aldosterone synthase (CYP11B2) inhibitors may offer a promising alternative. In this study, we used three-dimensional modeling of CYP11B2 to model the binding modes of the natural substrate 18-hydroxycorticosterone and the r...