PARASYMPATHOMIMETICS AND ANTICHOLINESTERASES

The Design of Anticholinesterases

The significance of new findings in two areas will be discussed with respect to the design of inhibitors of acetylcholinesterase. One area is that of enzyme structure, including the oligomeric form and the existence of allosteric binding sites, of isozymes and of a mutant enzyme. The other area is that of the forces which bind inhibitors to the enzyme prior to reacting with it, including ionic,...

The chemotherapy of poisoning by organophosphate anticholinesterases.

Oximes (with or without atropine as an adjunct) have recently been used successfully in the treatment of humans poisoned by organophosphate anticholinesterases. The discovery of the nature of the biochemical lesion in organophosphate poisoning has permitted the design of drugs to repair specifically this particular lesion. This paper reviews historically the researches which led to the developm...

Comparison of Adrenerglc Activation by Anticholinesterases and by Hypoxia

• Several anticholinesterases have been found to produce a blood pressure rise in the rat." This effect has been attributed to the central adrenergic activation.' On the other hand, anticholinesterases are known to cause bronchoconstriction and to produce, by this action, a long-lasting hypoxia (or anoxia) which is also known to produce general sympathetic activation. Asphyxiation of normal cat...

Comparison of adrenergic activation by anticholinesterases and by hypoxia.

• Several anticholinesterases have been found to produce a blood pressure rise in the rat." This effect has been attributed to the central adrenergic activation.' On the other hand, anticholinesterases are known to cause bronchoconstriction and to produce, by this action, a long-lasting hypoxia (or anoxia) which is also known to produce general sympathetic activation. Asphyxiation of normal cat...

The action of diisopropyl phosphorofluoridate and other anticholinesterases on amino acids.