Dexanabinol (HU-211 or ETS2101
) is a
synthetic cannabinoid
Synthetic cannabinoids are a class of designer drug molecules that bind to the same receptors to which cannabinoids (THC, CBD and many others) in cannabis plants attach. These novel psychoactive substances should not be confused with synthetic ...
derivative in development by e-Therapeutics plc. It is the "unnatural"
enantiomer
In chemistry, an enantiomer ( /ɪˈnænti.əmər, ɛ-, -oʊ-/ ''ih-NAN-tee-ə-mər''; from Ancient Greek ἐνάντιος ''(enántios)'' 'opposite', and μέρος ''(méros)'' 'part') – also called optical isomer, antipode, or optical ant ...
of the potent cannabinoid agonist
HU-210
HU-210 is a synthetic cannabinoid that was first chemical synthesis, 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 Tetrahydrocannabinol, ...
.
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 recepto ...
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
Anticonvulsants (also known as antiepileptic drugs or recently as antiseizure drugs) are a diverse group of pharmacological agents used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of b ...
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
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietar ...
and is currently undergoing
Phase I trials for the treatment of
brain cancer
A brain tumor occurs when abnormal cells form within the brain. There are two main types of tumors: malignant tumors and benign (non-cancerous) tumors. These can be further classified as primary tumors, which start within the brain, and secondar ...
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 international security, security, develop friendly relations among nations, achieve international cooperation, and be ...
'
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 syst ...
from 1961 nor their
Convention on Psychotropic Substances
The Convention on Psychotropic Substances of 1971 is a United Nations treaty designed to control psychoactive drugs such as #Amphetamine-type stimulants, amphetamine-type stimulants, barbiturates, benzodiazepines, and Psychedelic drug, psychede ...
from 1971,
[UN International Drug Control Conventions](_blank)
/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
Federal or foederal (archaic) may refer to:
Politics
General
*Federal monarchy, a federation of monarchies
*Federation, or ''Federal state'' (federal system), a type of government characterized by both a central (federal) government and states or ...
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 territorie ...
, 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
Possession may refer to:
Law
* Dependent territory, an area of land over which another country exercises sovereignty, but which does not have the full right of participation in that country's governance
* Drug possession, a crime
* Ownership
* ...
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 (state song), Alabama"
, image_map = Alabama in United States.svg
, seat = Montgomery, Alabama, Montgomery
, LargestCity = Huntsville, Alabama, Huntsville
, LargestCounty = Baldwin County, Al ...
.
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 C ...
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](_blank)
/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
Norbinaltorphimine (nor-BNI or nBNI) is an opioid antagonist used in scientific research. It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- ...
References
{{Ionotropic glutamate receptor modulators
Cannabinoids
NMDA receptor antagonists
Phenols
Benzochromenes
Primary alcohols
HU cannabinoids