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R-30490 (also known as 4-Methoxymethylfentanyl) is an opioid analgesic related to the highly potent animal tranquilizer carfentanil and with only slightly lower potency. It was first synthesized by a team of chemists at Janssen Pharmaceutica led by Paul Janssen, who were investigating the structure-activity relationships of the fentanyl family of drugs. R-30490 was found to be the most selective agonist for the μ-opioid receptor out of all the fentanyl analogs tested, but it has never been introduced for medical use in humans, although the closely related drug sufentanil is widely used for analgesia and anesthesia during major surgery.

4-Methoxymethylfentanyl, also known as R-30490, is a synthetic opioid analgesic structurally related to fentanyl and its analogs. It was first synthesized by a team of chemists at Janssen Pharmaceutica, led by Paul Janssen, during investigations into the structure-activity relationships of the fentanyl family of drugs.

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Chemical Structure and Properties

The chemical formula of 4-methoxymethylfentanyl is C₂₄H₃₂N₂O₂, with a molecular weight of approximately 380.53 g/mol. Its structure consists of a piperidine ring, an anilide group, and a methoxymethyl group attached to the aromatic ring.

Pharmacological Profile

4-Methoxymethylfentanyl is a potent μ-opioid receptor agonist, with analgesic properties similar to fentanyl. However, due to limited research, its exact potency and safety profile are not well-established. It is important to note that fentanyl analogs, including 4-methoxymethylfentanyl, can pose significant risks, including respiratory depression and potential for abuse.

Usage and Administration

There is no approved medical use for 4-methoxymethylfentanyl in humans. Researchers and forensic specialists primarily use it for their applications. Due to its high potency and potential for severe adverse effects, experts strongly advise against its recreational use.

Legal Status

The legal status of 4-methoxymethylfentanyl varies by jurisdiction. In some regions, it may be classified as a controlled substance due to its structural similarity to fentanyl and potential for abuse. It is essential to consult local regulations to determine its legality in a specific area.

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Safety Considerations

Handling 4-methoxymethylfentanyl requires strict safety precautions, including the use of appropriate personal protective equipment (PPE) and adherence to protocols for handling potent opioids. Accidental exposure can lead to serious health risks, including respiratory depression and overdose.

Conclusion

4-Methoxymethylfentanyl is a synthetic opioid analog with a chemical structure related to fentanyl. While it shares similarities with fentanyl in terms of receptor activity, its pharmacological properties, safety profile, and potential for abuse are not well-understood. Given its potency and associated risks, it is crucial to approach this compound with caution and awareness of legal and safety considerations.

R-30490 (also known as 4-methoxymethylfentanyl) is an opioid analgesic related to the highly potent animal tranquilizer carfentanil, and with only slightly lower potency. It was first synthesised by a team of chemists at Janssen Pharmaceutica led by Paul Janssen, who were investigating the structure-activity relationships of the fentanyl family of drugs. R-30490 was found to be the most selective agonist for the μ-opioid receptor out of all the fentanyl analogues tested, but it has never been introduced for medical use in humans, although the closely related drug sufentanil is widely used for analgesia and anesthesia during major surgery.

Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.