'Analgesic from mushrooms begins clinical trials' (1981)

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'Analgesic from mushrooms begins clinical trials' (1981)

Post by Amanita Research » Sun Oct 25, 2020 11:23 pm

Title: Analgesic from mushrooms begins clinical trials (1981)

Abstract : Gaboxydol (THIP)
"A potent analgesic that is as strong a pain-killer as morphine, but that works by a completely different mechanism and that has shown no signs of being addictive, is now undergoing clinical trials in Europe, its inventor, Poul Krogsgaard-Larsen of the Royal Danish School of Pharmacy reported at the ACS meeting. The compound is a structural analog of muscimol, one of the two active constituents of the toxic mushroom, Amanita muscaria. Muscimol itself is structurally related to the brain neurotransmitter GABA (y-aminobutyric acid), but is too toxic for use in humans. The new agent, tetrahydroisooxazolo-[5,4-c]-pyridine3-ol or THIP, is a variant of muscimol in which part of the molecule is held in a more rigid conformation; it shows very little toxicity in clinical studies. The mechanism of action of THIP is not known, but its analgesic effect is not inhibited by the narcotic antagonist naloxone, which indicates that the mechanism is different from that of morphine. The agent is very unusual, Krogsgaard-Larsen says, in that it can cross the blood-brain barrier even though it carries a charge; it can also be taken orally, and a dose of about 10 to 15 milligrams appears to be as effective as an injection of morphine. The clinical trials are being conducted by Lundbech and Company of Copenhagen and Sandoz Ltd. of Switzerland."
Maugh, T. H. (1981). Analgesic from mushrooms begins clinical trials. Science, 212(4493), 431-431.
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