Drug Target Sites Research Articles

Analgesic effects of cyclazocine and morphine microinjected into the rat dorsomedial hypothalamus demonstrated by the bradykinin-induced flexor reflex test

The analgesic effect of cyclazocine microinjected into the diencephalon of rats was studied by using the bradykinin-induced flexor reflex test. The dorsal portion of the medial hypothalamic area was sensitive to cyclazocine with respect to the production of analgesia (ED 50 2.6 μg/rat). Microinjections of morphine into the same portion also produced a dose-dependent analgesic effect (ED 50 2.5 μg/rat). As naloxone (0.9 mg/kg s.c.) antagonized both these analgesic effects, the findings suggest that the dorsal portion of the medial hypothalamic area of the rat is one of the primary target sites of analgesix drugs.

General Mechanisms of Antimicrobial Resistance

Bacteria can become resistant to antimicrobial agents by two routes, either by mutation or by the inheritance of new genetic information in the form of resistance plasmids. The mechanisms by which bacteria express resistance are manyfold, and five different biochemical mechanisms have been demonstrated in clinical isolates. The most important mechanisms are alteration of the drug target site, interference with the transport of the antimicrobial agent into the cell, and detoxification (inactivation) of the drug in the immediate environment of the cell.

Biopolymers in drug technology: the use of DNA in purifying phleomycin.

AbstractIt is sometimes easier and cheaper to extract a drug's target sites from cells than it is to purify, concentrate or manufacture the drug itself. This is especially true in the case of DNA and some of the exotic antibiotics that react with it. Phleomycin, an inhibitor of replication, was considered as a specific case in point. Biologically active components of this antibiotic mixture bind nondestructively to DNA, in vitro and in vivo, and thereafter may be processed by simple, economical methods usually reserved to macromolecules of much greater size.