Forum — From the August 2013 issue

Gaboxadol

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In 1755 the naturalist Stepan Krasheninnikov observed the Amanita muscaria mushroom’s effects on Russian soldiers in Siberia ingesting it for the first time. Claiming to have been seized by an invisible power, the men submitted to the mushroom’s strange and often violent commands. A servant strangled his master. A soldier found himself ordered to his knees and confessed his sins before God. Krasheninnikov’s interpreter drank some mushroom liquor and “went into such a frenzy that he slashed open his abdomen, on the command . . . of mukhomor, the mushroom.” One soldier who ate this mukhomor found a certain dose reduced his fatigue while marching, but after eating more of the mushroom he “gripped his testicles and died.”

[1] Comparing the behavior of Krasheninnikov’s soldiers with a few recent case reports on the well-known GABA modulator Ambien (zolpidem tartrate) will reveal striking similarities. A 2010 article entitled “Command Hallucinations with Self-Stabbing Associated with Zolpidem Overdose” may be an apposite place to begin.

Krasheninnikov’s report seems to describe the response drug-naïve users can have to GABAergic deliriants, which act on a neurotransmitter that reduces the transmission of excitatory impulses in about half the brain’s neurons.[1] Subsequent centuries of eager reporting on the outré customs he had described culminated in an extermination campaign begun under Stalin and continued by the KGB that is said to have completely eradicated traditional A. muscaria use by 1980. While operatives were systematically destroying the ostensibly anticommunist Siberian mushroom traditions via a series of assassinations in which shamans were reportedly thrown from helicopters, plunged into frozen lakes, or simply shot, with their drums kept as trophies, biochemists internationally were recognizing the enormous value of muscimol, a psychoactive alkaloid produced by A. muscaria, which, instead of changing the activity of endogenous GABA, actually replaces it in the brain.

A team of Danish researchers led by the medicinal chemist and GABA expert Povl Krogsgaard-Larsen began synthesizing and publishing on dozens of muscimol derivatives. One molecule created in 1977 stood out: a derivative that, like muscimol itself, behaved as a direct agonist of the GABAA receptor and could be ingested orally. Furthermore, it was less toxic than muscimol. This compound would come to be known as gaboxadol.

Until relatively recently, self-experimentation was a vital component of drug discovery, and so when Krogsgaard-Larsen recognized the uniqueness of gaboxadol he ingested the drug in increasing doses to characterize its qualitative effects. “We had blood samples taken continuously,” he told me. “Normally I’m scared of blood and I don’t like the pain of needles, but this time I was not scared and there was no pain whatsoever. At 10mg the general feeling I had when I was walking around was just as if I had taken two or three beers — it was a very comfortable feeling.” Krogsgaard-Larsen filed for a patent for gaboxadol and transferred it to the pharmaceutical company Lundbeck. Then came a surge of human testing.

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’s last article for Harper’s Magazine, “Blood Spore,” appeared in the July issue. He is writing a book on clandestine chemistry.

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