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Structural pharmacology and therapeutic potential of 5-methoxytryptamines

Nature. 2024-05; 
Audrey L Warren, David Lankri, Michael J Cunningham, Inis C Serrano, Lyonna F Parise, Andrew C Kruegel, Priscilla Duggan, Gregory Zilberg, Michael J Capper, Vaclav Havel, Scott J Russo, Dalibor Sames, Daniel Wacker
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Proteins, Expression, Isolation and Analysis … Eluted protein was further processed through the addition of PreScission Protease (Genscript) to remove the N-terminal His tag from the Gβ 1 subunit. Purified G protein and PreScission … Get A Quote

摘要

Psychedelic substances such as lysergic acid diethylamide (LSD) and psilocybin show potential for the treatment of various neuropsychiatric disorders. These compounds are thought to mediate their hallucinogenic and therapeutic effects through the serotonin (5-hydroxytryptamine (5-HT)) receptor 5-HT (ref. ). However, 5-HT also plays a part in the behavioural effects of tryptamine hallucinogens, particularly 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT), a psychedelic found in the toxin of Colorado River toads. Although 5-HT is a validated therapeutic target, little is known about how psychedelics engage 5-HT and which effects are mediated by this receptor. Here we map the molecular underpinnings of 5-MeO-DMT phar... More

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