Dexanabinol
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Dexanabinol (HU-211 or ETS2101) is a synthetic cannabinoid derivative in development by e-Therapeutics plc. It is the "unnatural" enantiomer of the potent cannabinoid agonist
HU-210 HU-210 is a synthetic cannabinoid that was first synthesized in 1988 from (1R,5S)-myrtenol by a group led by Raphael Mechoulam at the Hebrew University. HU-210 is 100 to 800 times more potent than natural THC from cannabis and has an extended d ...
. Unlike other
cannabinoid Cannabinoids () are several structural classes of compounds found in the cannabis plant primarily and most animal organisms (although insects lack such receptors) or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tet ...
derivatives, HU-211 does not act as a
cannabinoid receptor Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid recep ...
agonist, but instead has
NMDA antagonist NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the ''N''-Methyl-D-aspartate receptor ( NMDAR). They are commonly used as anesthetics for animals and humans; the state of anesthesia they induce ...
effects. It therefore does not produce cannabis-like effects, but is anticonvulsant and
neuroprotective Neuroprotection refers to the relative preservation of neuronal structure and/or function. In the case of an ongoing insult (a neurodegenerative insult) the relative preservation of neuronal integrity implies a reduction in the rate of neuronal los ...
, and is widely used in scientific research as well as currently being studied for applications such as treating head injury, stroke, or cancer. It was shown to be safe in clinical trials and is currently undergoing Phase I trials for the treatment of brain cancer and advanced solid tumors.


Clinical trials

Dexanabinol has been studied in IV administration and oral dosing. e-Therapeutics is evaluating the compound in clinical trials for brain and solid cancers. Phase II studies are planned based on the results of the current trials. A phase 1b study for hepatocellular carcinoma and pancreatic cancer was started in 2015.


Legal status

HU-211 is not listed in the schedules set out by the
United Nations The United Nations (UN) is an intergovernmental organization whose stated purposes are to maintain international peace and security, develop friendly relations among nations, achieve international cooperation, and be a centre for harmoniz ...
'
Single Convention on Narcotic Drugs The Single Convention on Narcotic Drugs, 1961 (Single Convention, 1961 Convention, or C61) is an international treaty that controls activities (cultivation, production, supply, trade, transport) of specific narcotic drugs and lays down a syste ...
from 1961 nor their Convention on Psychotropic Substances from 1971,UN International Drug Control Conventions
/ref> so the signatory countries to these international drug control treaties are not required by said treaties to control HU-211.


United States

HU-211 is not listed in the list of scheduled controlled substances in the USA. It is therefore not scheduled at the federal level in the
United States The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territori ...
, but it is possible that HU-211 could legally be considered an
analog Analog or analogue may refer to: Computing and electronics * Analog signal, in which information is encoded in a continuous variable ** Analog device, an apparatus that operates on analog signals *** Analog electronics, circuits which use analog ...
of Delta-8-THC (one of the THC isomers which is in Schedule I under the designation of "Tetrahydrocannabinols"), and therefore sales or possession could potentially be prosecuted under the
Federal Analogue Act The Federal Analogue Act, , is a section of the United States Controlled Substances Act passed in 1986 which allows any chemical "substantially similar" to a controlled substance listed in Schedule I or II to be treated as if it were listed in ...
. HU-211 is a Schedule I controlled substance in
Alabama (We dare defend our rights) , anthem = "Alabama" , image_map = Alabama in United States.svg , seat = Montgomery , LargestCity = Huntsville , LargestCounty = Baldwin County , LargestMetro = Greater Birmingham , area_total_km2 = 135,765 ...
. HU-211 is a Schedule I
controlled substance A controlled substance is generally a drug or chemical whose manufacture, possession and use is regulated by a government, such as illicitly used drugs or prescription medications that are designated by law. Some treaties, notably the Single ...
in the state of
Florida Florida is a state located in the Southeastern region of the United States. Florida is bordered to the west by the Gulf of Mexico, to the northwest by Alabama, to the north by Georgia, to the east by the Bahamas and Atlantic Ocean, and to ...
making it illegal to buy, sell, or possess in Florida.Florida Statutes - Chapter 893 - DRUG ABUSE PREVENTION AND CONTROL
/ref> Effective January 1, 2016, HU-211 is a regulated drug in Vermont designated as a "Hallucinogenic Drug."Vermont DOH - Regulated Drug Rule 2016 .PDF
/ref>


See also

*
Etonitazene Etonitazene is an analgesic drug, first reported in 1957, that has been shown to have approximately 1,000 to 1,500 times the potency of morphine in animals. Because it is characterized by a strong dependency potential and a tendency to produce pr ...
* Norbinaltorphimine


References

{{Ionotropic glutamate receptor modulators Cannabinoids NMDA receptor antagonists Phenols Benzochromenes Primary alcohols HU cannabinoids