XLR-11 (5"-fluoro-UR-144 or 5F-UR-144) is a drug that acts as a potent

agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ag ...

for the

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 ...

s CB₁ and CB₂ with EC₅₀ values of 98 nM and 83 nM, respectively. It is a 3-(tetramethylcyclopropylmethanoyl)indole derivative related to compounds such as UR-144,

A-796,260 A-796,260 is a drug developed by Abbott Laboratories that acts as a potent and selective cannabinoid CB2 receptor agonist. Replacing the aromatic 3-benzoyl or 3- naphthoyl group found in most indole derived cannabinoids with the 3- tetramethylcy ...

and

A-834,735 A-834,735 is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors, with a ''K''i of 12 nM at CB1 and 0.21 nM at CB2. Replacing the aromatic 3-benzoyl or 3- ...

, but it is not specifically listed in the patent or scientific literature alongside these other similar compounds, and appears to have not previously been made by

Abbott Laboratories Abbott Laboratories is an American multinational medical devices and health care company with headquarters in Abbott Park, Illinois, United States. The company was founded by Chicago physician Wallace Calvin Abbott in 1888 to formulate known dr ...

, despite falling within the claims of patent WO 2006/069196. XLR-11 was found to produce rapid, short-lived hypothermic effects in rats at doses of 3 mg/kg and 10 mg/kg, suggesting that it is of comparable potency to APICA and

STS-135 STS-135 ( ISS assembly flight ULF7) was the 135th and final mission of the American Space Shuttle program. It used the orbiter ''Atlantis'' and hardware originally processed for the STS-335 contingency mission, which was not flown. STS-135 la ...

Detection

A forensic standard for this compound is available, and a representative mass spectrum has been posted on Forendex.

Recreational use

XLR-11 was instead first identified by laboratories in 2012 as an ingredient in synthetic cannabis smoking blends, and appears to be a novel compound invented specifically for grey-market recreational use.

Legal Status

XLR-11 was banned in New Zealand by being added to the temporary class drug schedule, effective from 13 July 2012. The U.S. Drug Enforcement Administration (DEA) made the synthetic cannabinoids UR-144, XLR11, and AKB48 Schedule I, illegal drugs under the Controlled Substances Act (CSA) for the next two years as of 16 May 2013. It has also been banned in Florida as of 11 December 2012. Arizona banned XLR-11 on 3 April 2013. As of October 2015 XLR-11 is a controlled substance in China. XLR-11 is banned in the Czech Republic.

Side effects

XLR-11 has been linked to hospitalizations due to its use.

Toxicity

XLR-11 has been linked to

acute kidney injury Acute kidney injury (AKI), previously called acute renal failure (ARF), is a sudden decrease in kidney function that develops within 7 days, as shown by an increase in serum creatinine or a decrease in urine output, or both. Causes of AKI are c ...

in some users, along with

AM-2201 AM-2201 (1-(5-fluoropentyl)-3-(1-naphthoyl)indole) is a recreational designer drug that acts as a potent but nonselective full agonist for the cannabinoid receptor. It is part of the AM series of cannabinoids discovered by Alexandros Makriyanni ...

References