BROMADOLINE (U-47931E)

Description
WHAT IS BROMADOLINE (U-47931E)?
Bromadoline (U-47931E) is an opioid analgesic selective for the μ-opioid receptor developed by the Upjohn company in the 1970s.[3]The drug has a potency lying between that of codeine and morphine, being...
Description
WHAT IS BROMADOLINE (U-47931E)?
Bromadoline (U-47931E) is an opioid analgesic selective for the μ-opioid receptor developed by the Upjohn company in the 1970s.[3]The drug has a potency lying between that of codeine and morphine, being slightly stronger than pentazocine.Bromadoline (U-47931E) is an opioid that is speculated to be around 70% as potent as Morphine.Bromadoline U-47931E 4-bromo-N-[2 (dimethylamino)cyclohexyl]benzamide) U-47931E (Bromadoline) is classified as a novel opioid. Novel opioids have been reported to cause effects similar to heroin and fentanyl. Novel opioids in the trans-N-[2- (methylamino)cyclohexyl]-benzamide class, such as U-47700, and similar classes, such as U49900, have caused adverse events, including deaths, as described in the literature. Structurally similar compounds include U-47700, U-49900, U-48800, isopropyl-U-47700, and 3,4- methylenedioxy-U-47700. U-47700 is a Schedule I substance in the United States.

LEGAL STATUS
Following its sale as a designer drug, U-47700 was made illegal in Sweden on January 26, 2016.[45]

U-47700 was emergency scheduled in Ohio on May 3, 2016 by executive order of Governor John Kasich.[46]

U-47700 was emergency scheduled in Florida on September 27, 2016 by an emergency rule of Florida Attorney General Pam Bondi.[47]

Responding to a perceived threat to public health and safety, the U.S. Drug Enforcement Administration has placed U-47700 into Schedule 1 of the Controlled Substances Act, effective November 14, 2016.[48]

U-47700 was placed into Schedule 1 of South Dakota’s Controlled Substance Schedule. It was signed by Governor Daugaard on February 9, 2017.[49].

SIDE EFFECTS OF BROMADOLINE (U-47931E)
U-47931E has never been studied on humans, but would be expected to produce effects similar to those of other potent opioid agonists, including strong analgesia, sedation, euphoria, constipation, itching and respiratory depression which could be harmful or fatal. Tachycardia was another side effect encountered with U-47931E use. Tolerance and dependence would be expected to develop.

U-47931E is a structural isomer of the earlier opioid AH-7921 and the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold. Upjohn looked for the key moieties which gave the greatest activity and posted over a dozen patents on related compounds, each optimizing one moiety until they discovered that U-47931E was the most active.



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18 říjen 2022
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