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BenzylfentanylBenzylfentanyl is a fentanyl analogue that was once a schedule I substance, but since 2010 it has been removed from this list. It is considered to be an “essentially inactive” opioid that is useless as a painkiller, sedative, anaesthetic or even recreational drug.

It has a binding affinity Ki of 213 nM at the μ-opioid receptor meaning it binds 200x less strongly than fentanyl to this receptor. Binding to the opioid receptors is essential for these drugs to be effective.

The emergency scheduling of Benzylfentanyl as a Schedule I compound was done during a period of abuse of fentanyl analogues in the USA. From 1978 to the mid 1980s there was widespread abuse of fentanyl analogues mostly in the state of California. This lead to the passing of the Federal Analogues Act which banned a whole family of fentanyl analogues based on their structural similarity.

Later when benzylfentanyl was analysed it was found to have no potency or potential for abuse as an opioid drug. Hence it was removed from the controlled substances list in 2010.

Benzylfentanyl cannot then be included among the list of abused fentanyl analogues. In the 1980s it was detected in drug seizures, although this is most likely as it was a by product of creating other, more active fentanyl analogues.

Other fentanyl analogues such as acetylfentanyl and 3 methyl fentanyl however have proven to be very powerful drugs unlike benzylfentanyl.

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Benzylfentanyl is an exception to the rule. Most of the fentanyl analogues tend to be very powerful drugs, many times stronger than heroin or morphine.

The side effects of fentanyl analogues are similar to those of fentanyl itself and tend to include nausea, vomiting, itching and strong respiratory depression which can be life threatening.

Many of these compounds have been associated with a high mortality rate. This is due to a combination of two dangerous factors. They have an extreme potency in combination with producing higher levels of respiratory depression relative to the euphoria or “high” produced. They are known to cause respiratory arrest.

In the early 2000s fentanyl and fentanyl analogues were widely abused in Estonia. This was due to a number of factors. Most notably the regular supply of heroin to Europe had been cut off due to the American war in Afghanistan against the heroin producing Taliban tribes. Fentanyl and its analogues tend to surface as drugs of abuse when heroin is in low supply or of poor quality. The quality of the “high” is considered to be lesser than that of heroin, oxycodon or morphine. They are also often shorter acting and so provide a less satisfactory high for these users.  The danger of fentanyl analogues is such that the average life expectancy of opioid drug users in this country was only 29 compared to the European average of 38 years for heroin users.

More recently fentanyl analogues have surfaced once again in the USA. They are thought to be manufactured by clandestine labs in China, and smuggled in to the country by Mexican drug cartels.