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Carfentanil or carfentanyl is an analog of the synthetic opioid analgesic fentanyl. It is more effective at reducing pain response in rats than any other opioid.
Carfentanil was first synthesized in 1974 by a team of chemists at Janssen Pharmaceutica which included Paul Janssen.
Carfentanil has been sold since 1986 under the brand name “Wildnil” for use in tranquilizer darts in combination with an α2-adrenoreceptor agonist for large mammals including elk and elephants. It is chosen for its high safety margin as the fatal dose of carfentanil is approximately the same as that of fentanyl despite much higher opioid activity.
Radiolabelled [11C]carfentanil is widely used as a selective radiotracer in animal and human positron emission tomography (PET) imaging studies of the μ-opioid system due to its high affinity for receptors.
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The effects of carfentanil, including overdose, can be reversed by naloxone.
Carfentanil (also known as Carfentanyl; 4-carbomethoxyfentanyl; R33799) is an analog of the synthetic opioid analgesic Fentanyl. Carfentanil was first synthesized in 1974 by a team of chemists at Janssen Pharmaceutica which included Paul Janssen.
The effect of Carfentanil exceeds Fentanyl and Morphine in 100 and 10000 times, respectively. Median analgesic activity of ED50 for Carfentanil with intravenous administration to rats is 0.41 μg / kg, the effect on the human body begins already with 1 μg.
A November 2016 article in Time, “Heroin Is Being Laced With a Terrifying New Substance: What to Know About Carfentanil”, reports over 300 cases of overdose related to fentanyl and fentanyl analogues and several deaths connected to the drug since August 2016 in several of the United States, including Ohio, West Virginia, Indiana, Kentucky and Florida. In 2017, a Milwaukee, Wisconsin man died from a carfentanil overdose, likely taken unknowingly with another illegal drug such as heroin or cocaine. Carfentanil is most often taken with heroin or by users who believe they are taking heroin. Carfentanil is added to or sold as heroin because it is less expensive, easier to obtain (until China added it to its list of controlled substances on 1 March 2017, it was legal for Chinese firms to advertise and sell carfentanil over the Internet, offering advice to customers in other countries on how to import it illegally) and easier to make than heroin.
