Amanita And Epilepsy Research

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amanitadreamer
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Amanita And Epilepsy Research

Post by amanitadreamer » Tue Nov 24, 2020 3:55 pm

Amanita Dreamer <amanitadreamer@gmail.com>
Mon, Nov 16, 7:33 AM (8 days ago)
to Adeptus

https://pubmed.ncbi.nlm.nih.gov/19055494/ Rat studies, primates

There was a 14 year clinical trial but I can't find the results of it...but this is the call for patients and set up of the study
https://clinicaltrials.gov/ct2/show/NCT00005925

Anti-convulsant effects of muscimol:
https://pubmed.ncbi.nlm.nih.gov/7189834/

https://www.sciencedirect.com/science/a ... 0879900868


“Ibotenic acid and muscimol are respectively conformationally restricted derivatives of glutamic acid and gamma-aminobutyric acid (GABA).” “Glutamic acid is a major excitatory neurotransmitter in mammalian central nervous systems and its receptors are implicated in neurological disorders such as epilepsy and Huntington’s disease. Inhibitory glutamate receptors (IGluRs) constitute a class of ion channel proteins equivalent to glycine and GABA receptors. Ibotenic acid acts on IGluRs (Cleland 1996).” “AMPA, a synthetic analogue of ibotenic acid, displays the same typical moiety and was found to be more effective and specific glutamate agonist than the parent compound (Watkins, Krogsgaard-Larsen & Honore 1990).” “There is evidence that damaged function of GABA mediated inhibitory synapses is implied in experimental and clinical seizure disorders. Decreased concentration, and then activity of GABA, may have a role in human epilepsy. Muscimol is a potent conformational analogue and biologically active biosostere (Krogsgaard et. el. 2000).” “This toxin tightly binds with the gamma-aminobutyrate receptor (de Feudis 1980). Moreover, it is also an inhibitor of neuronal and glial GABA uptake and a substrate for the GABA- metabolizing enzyme: GABA transaminase. Subsequently, some research teams tried to improve the potency of drugs. Lipophilicity is of considerable interest for the prediction of the transport, adsorption and distribution properties of molecules, and so is an important factor in drug design. More lipophilic bioisosteres of muscimol and GABA have been synthesized, such as Tiagabine. This drug was marketed as a therapeutic agent for the treatment of epilepsy, Gabatril ® (Krogsgaard-Larsen 1977, KrogsgaardLarsen et. el. 1994, Krogsgaard-Larsen, Frolund& Frydenvang 2000).”
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