Don’t Block Psychedelic Research
Don’t Block Psychedelic Research
DOI and DOC are essential compounds used by scientists to understand serotonin receptors and their role in disorders like anxiety, depression, pain, substance use disorder, and even cancer.
DOI and DOC on trial
Putting DOI and DOC in Schedule I will halt vital research that could improve the health of people suffering from various disorders. We are working to preserve access to these compounds to ensure these important research avenues are not jeopardized.”
Dr. Alaina Jaster, PhD.
Defining research harm
It’s time to let science lead the way and tear down the barriers that hold back progress. Only by removing these obstacles can we make way for groundbreaking advancements in science and medicine. Together, my colleagues and I are here to champion a future where science is not hindered by unnecessary barriers but empowered to explore and innovate.
Dr. Raul Ramos, PhD.
Miller Research Fellow
HHMI Hanna Gray Fellow
Bautista/Lumpkin Labs
University of California, Berkeley
The Origins of DOI and DOC
*Sasha in his home lab. Photo courtesy of the Shulgin Foundation.
It is essential that our present negative propaganda regarding psychedelic drugs be replaced with honesty and truthfulness about their effects, both good and bad.
In the late 1960s and early 1970s, chemist Alexander “Sasha” Shulgin pioneered a new era of psychedelic research through the systematic modification of chemical compounds related to the naturally occurring psychedelic mescaline. Through these compounds, known as substituted phenethylamines, Shulgin and his peers explored how subtle chemical substitutions at specific positions on the aromatic ring dramatically altered psychoactive properties.
Of the 179 compounds detailed in his opus Phenethylamines I Have Known and Loved (PiHKAL), one such chemical, 2,5-dimethoxy-4-methylamphetamine (DOM) (which Shulgin called his “hair shirt” and, à la Albert Hofmann, his “problem child”), became the starting material for a pair of Canadian chemists in 1973, which culminated in the synthesis of two important chemicals: 2,5-dimethoxy-4-iodoamphetamine (DOI) and 2,5-dimethoxy-4-chloroamphetamine (DOC).
In the fifty years since Coutts and Malicky first synthesized DOI and DOC, DOI in particular has been pivotal in understanding serotonin receptor pharmacology and function. Due to its high selectivity for the 5-HT2A receptor subtype, DOI is distinguished from earlier psychedelics like LSD, which, although potent, interact promiscuously with multiple serotonin, dopamine, and adrenergic receptors. For this reason DOI became one of the most widely used synthetic psychedelics in neuroscience research for studying 5-HT2A receptor function.
Unraveling the Mysteries of the Serotonin Receptor
1979 represented a groundbreaking year in serotonin research, when the 5-HT1 and 5-HT2 were isolated in the mammalian brain by Snyder and Peroutka. Soon after, it was found that most serotonin antagonists (molecules that bind to a receptor and block the activity of an agonist) at that time would bind with higher affinity to the 5-HT2 receptor than the 5-HT1 receptor. For this reason, researchers speculated that antagonists exerted their effects by binding to the 5-HT2 while 5-HT1 was the site of action of agonists.
Radioligands are molecules with a radioactive isotope contained in their structure that can be used to visualize and detect specific receptors or proteins in the body.
*simplified view of a [125I}-DOI radioligand bound to a receptor.
We do this work because the war on drugs is a war on us.