Remarks on the Synthesis of Quaternary Cocaine Compounds

Strycker, Stanley J.; Long, J. P.

doi:10.1002/jps.2600571051

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2009

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“…Many chemical analogs of cocaine have previously been synthesized [8], [9]. Cocaine methiodide (CM) is a chemical analog of cocaine with a stable positive charge at physiological pH.…”

Section: Introductionmentioning

confidence: 99%

Potencies of Cocaine Methiodide on Major Cocaine Targets in Mice

et al. 2009

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Cocaine methiodide (CM), a charged cocaine analog, cannot pass the blood brain barrier. It has been assumed the effects of systemic CM represent cocaine actions in peripheral tissues. However, the IC50 values of CM have not been clearly determined for the major cocaine targets: dopamine, norepinephrine, and serotonin transporters, and sodium channels. Using cells transfected with individual transporters from mice and synaptosomes from mouse striatum tissues, we observed that the inhibition IC50 values for monoamine uptake by CM were 31-fold to 184-fold higher compared to cocaine at each of the transporters. In dorsal root ganglion neurons, cocaine inhibited sodium channels with an apparent IC50 of 75 µM, while CM showed no observable effect at concentrations up to 3 mM. These results indicate that an equal dose of CM will not produce an equivalent peripheral effect of cocaine.

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“…Many chemical analogs of cocaine have previously been synthesized [8], [9]. Cocaine methiodide (CM) is a chemical analog of cocaine with a stable positive charge at physiological pH.…”

Section: Introductionmentioning

confidence: 99%