[THE INFLUENCE OF MELATONIN ON THE PARAMETERS OF CEREBRAL HEMODYNAMICS IN PATIENTS WITH HYPERTENSIVE DISEASE].

The authors discuss the results of application of melatonin in patients with hypertensive disease. Treatment with melatonin facilitated normalization of arterial pressure and cerebral hemodynamics at night time.

[Correction of the influence of clinostatic hypokinesis on encephalitic circulatory dynamics during the sleep in patients with hypertensive disease].

During the sleep person is in the state of antiorthostasis, this state provokes vascular cerebral abnormalities (night cerebral hypervolemia). The nature of encephalon blood supply is changing in this horizontal state, in the result there is lowering of hydrostatic blood pressure, rise of the encephalon blood supply and more difficult venous outflow. 60 patients with essential hypertension (1-2 phases) at the age of 64.

Non-nucleoside inhibitors of HCV polymerase NS5B. Part 3: synthesis and optimization studies of benzothiazine-substituted tetramic acids.

Benzothiazine-substituted tetramic acids were discovered as highly potent non-nucleoside inhibitors of HCV NS5B polymerase. X-ray crystallography studies confirmed the binding mode of these inhibitors with HCV NS5B polymerase. Rational optimization of time dependent inactivation of CYP 3A4 and clearance was accomplished by incorporation of electron-withdrawing groups to the benzothiazine core.

Characterization of the analgesic and anti-inflammatory activities of ketorolac and its enantiomers in the rat.

The marked analgesic efficacy of ketorolac in humans, relative to other nonsteroidal anti-inflammatory drugs (NSAIDs), has lead to speculation as to whether additional non-NSAID mechanism(s) contribute to its analgesic actions. To evaluate this possibility, we characterized (R,S)-ketorolac's pharmacological properties in vivo and in vitro using the nonselective cyclooxygenase (COX) inhibitors [indomethacin (INDO) and diclofenac sodium (DS)] as well as the selective COX-2 inhibitor, celecoxib, as references. The potency of racemic (R,S)-ketorolac was similar in tests of acetic acid-induced writhing, carrageenan-induced paw hyperalgesia, and carrageenan-induced edema formation in rats; ID50 values = 0.