Current Medicinal Chemistry - Volume 9, Issue 15, 2002

The peripheral benzodiazepine receptors (PBRs) have been identified to bind selectively benzodiazepine ligands and an isoquinoline carboxamide derivative PK 11195 with high affinity. PBRs are present in the central nervous system (CNS), peripheral tissues, and most organs in the human body. PBRs are different from the central benzodiazepine receptors (CBRs) related to the nerve cell membrane GABAA receptor and are Read More

The branched-chain fatty acid valproic acid (VPA) is the most commonly used antiepileptic drug for treating generalized epilepsy. Although originally considered to be of low toxicity, VPA has proved to possess considerable teratogenic potential when applied to the pregnant epileptic women. During the last few years, it has become evident that some of the mechanisms which account for the malformations produced by VPA a Read More

Malaria is the major parasitic infection in many tropical and subtropical regions, leading to more than one million deaths (principally young African children) out of 400 million cases each year (WHO world health report 2000). More than half of the world's population live in areas where they remain at risk of malaria infection. During last years, the situation has worsened in many ways, mainly due to malarial parasites becomi Read More

This review traces the origins of the chemical structure of the cyclooxygenase inhibitors celecoxib and rofecoxib. Early results from the search for non-steroid estrogens led to the triaryl-ethylenes such as chlortrianisene. A congener that incorporated a water-solubilizing basic ether grouping unexpectedly led to an estrogen antagonist and eventually the drug clomiphene. Elaboration of the structure gave the widely used drug Read More

Human serum albumin (HSA) plays a fundamental role in the transport of drugs, metabolites, and endogenous ligands. Binding to HSA controls the free, active concentration of a drug, provides a reservoir for a long duration of action, and ultimately affects drug absorption, metabolism, distribution and excretion. The free concentration of a drug can also be affected by interaction with co-administered drugs or by patholo Read More

The number of herbal formulae considered to be clinically effective and recorded in the Chinese medical literature is huge. The scientific basis for the remedial effects of these herbal formulae is not yet understood, nor has a clear need been given as to how to make use and combine traditional Chinese medicine (TCM) and Western medicine in an effective way. In this context, it is of interest to ascertain what individual Read More