Current Medicinal Chemistry - Volume 9, Issue 1, 2002

Neuronal acetylcholine ion channel receptors (nAChRs), that exist in several subtypes resulting from a different organisation of various subunits around the central ion channel, are involved in a variety of functions and disorders of the central nervous system. There is evidence to implicate a deficit of nAChRs in the symptomatology of severe neurologic pathologies, such as Alzheimer's and Parkinson's diseases. Reliable three- Read More

The clinical effectiveness of morphine is limited by several side effects, including the development of tolerance and dependence. Most of these side effects are believed to be mediated by central opioid receptors therefore, hydrophilic opioids, which don't cross the blood-brain barrier, may have advantages over morphine in some clinical applications. We recently synthesized several analogues of DALDA (Tyr-D-Arg-Phe-Lys-NH2), Read More

The cellular electrophysiologic effect of GYKI 16638, a new antiarrhythmic compound was studied and compared with that of sotalol and mexiletine in undiseased human right ventricular muscle preparation by applying the conventional microelectrode technique.GYKI 16638 (5 μM), at stimulation cycle length of 1000 ms, lengthened action potential duration (APD90) from 338.9 ± 28.6 ms to 385.4 ± 24 ms (n = 9, p< 0.05). This AP Read More

(-)-Deprenyl (selegiline), a propargylamine derivative of methylamphetamine, is a potent, irreversible inhibitor of monoamine-oxidase type B (MAO-B). The MAO-B inhibitory effects of various doses (0.1-0.25-0.5 mg / kg) of (-)-deprenyl in rat brain and liver were compared, using either oral or subcutaneous drug administration. The intensity of the first pass metabolism of (-)-deprenyl was also estimated. The effect of pre-treat Read More

A large number of oral antidiabetic agents are available today. This article provides a short review of the pharmacology and some clinical aspects of various oral antidiabetic drugs. It focuses mainly on the newest developing drugs (therapy of the near future) and on the most commonly used older groups for the common approach of every- day practice (sulphonylureas). The primary goal of this review is to compare the electr Read More

Liver metastases cause the majority of deaths from colorectal cancer, and response to chemotherapy and external radiotherapy is poor. An alternative is internal radionuclide therapy using 90Y labeled microspheres. These microspheres are very stable and have a proven efficacy in the field of treatment of primary or metastatic hepatic cancer. Whilst these glass spheres showed encouraging results in patients, their high Read More

In the human brain several cell types are capable of initiating and amplifying a brain specific inflammatory response involving the synthesis of cytokines, prostaglandins and oxygen free radicals. In Alzheimer's disease (AD), signs of an inflammatory activation of microglia and astroglia are present inside and outside amyloid deposits. Cell culture and animal models suggest an interactive relationship between inflammatory a Read More

Non steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used for inflammation therapy. The major drawback in using the NSAIDs is in their tendency to cause gastrointestinal toxicity. Since the roles of arachidonic acid (A.A) metabolites, as leukotrienes (Lts), prostaglandins (PGs) and thromboxanes (TXA2) as mediators of the inflammatory reaction were clarified, much effort has been made to Read More

Recent contributions applying Computational Chemistry to serotonin-3 and nicotinic acetylcholine ionotropic receptors are reviewed. These two receptors constitute a good example for the examination of the computational protocols that have been used to understand how they work. On the one hand, (5-HT3R) receptor mapping techniques have been mostly employed in its study and very few examples of receptor fitting hav Read More

A combination of the economic importance of blood as a resource and the advent of the AIDS epidemic has led to a requirement for improved pathogen screening techniques for donated blood. However, due to “window” periods where infective agents cannot be detected, the ability to disinfect of blood and its derivatives - plasma, platelets and red blood cell concentrates - has assumed great importance.Whereas conve Read More