Abbott Laboratories

  The frantic effort of drug companies to develop completely new painkillers turned up many hopefuls from examining epibatidine derivatives. The most successful and promising of these was found by Abbott Laboratories in 1998. Each chemical devised by the laboratory was numbered and those from Abbot Labs given the prefix ABT.

  When the journal Science published the structure of epibatidine on it's characterisation by Daly's lab, Abbott laboratories noticed the structural similarites between this and the compounds they had been testing for Alzheimer's Disease. Because these also operated by binding to acetylcholine receptors, Abbott labs began to test their compounds for signs of analgesic activity.


  It was in 1998 that after testing over 500 epibatidine derivatives, ABT-594 was discovered to be 50 times more potent than morphine, yet on animal tests, no paralysis or depression of muscle action was observed.


  ABT-594 was synthesised from epibatidine, and initial testing was extremely promising, with the compound binding many hundreds of times more strongly to nicotinic receptors of the pain pathways in the central nervous system than those of the neuromuscular junction.

Epibatidine bound only 57 times more strongly to receptors on the CNS.

The tests also indicated that ABT-594 was not addictive, even though nicotine itself is. Epibatidine is effective in combating both inflammatory pain and neuropathic pain. (Inflammatory is caused by direct cell damage and receptors detecting, whereas neuropathic is caused by a range of syndromes and pain persists without direct stimuli from tissues), and ABT-594 showed promise in both areas in the Phase I safety trials.

These involve a small number of healthy volunteers, (20-100), usually under constant observation, e.g. in a hospital, where the side effects are noted.

ABT-594 had moved onto Phase II testing in Europe a few years ago, after the safety tests had demonstrated low toxicity levels. These involve patients who actually require drug relief. Half the patients are given a placebo in this phase.

ABT-594 has completed this phase, yet Abbott labs have not released results.


3D model of ABT-594

Molecule needs at least Java 1.2

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