R-30490 (also known as 4-methoxymethylfentanyl) is an
opioid
Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...
analgesic
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
related to the highly potent animal tranquilizer
carfentanil
Carfentanil or carfentanyl, formerly sold under the brand name Wildnil, is an extremely potent opioid analgesic used in veterinary medicine to anesthetize large animals such as elephants and rhinoceroses. It is a structural analogue of the ...
, and with only slightly lower potency. It was first synthesised by a team of chemists at
Janssen Pharmaceutica
Johnson & Johnson Innovative Medicine (formerly Janssen Pharmaceuticals) is a Belgian pharmaceutical company headquartered in Beerse, Belgium, and wholly owned by Johnson & Johnson. It was founded in 1953 by Paul Janssen.
In 1961, Janssen Ph ...
led by
Paul Janssen
Paul Adriaan Jan, Baron Janssen (12 September 1926 – 11 November 2003) was a Belgian physician. He was the founder of Janssen Pharmaceutica, a pharmaceutical company with over 20,000 employeesPaul Lewi, Obituary of Dr Paul Janssen (1926–20 ...
, who were investigating the
structure-activity relationships of the
fentanyl
Fentanyl is a highly potent synthetic piperidine opioid primarily used as an analgesic (pain medication). It is 30 to 50 times more Potency (pharmacology), potent than heroin and 50 to 100 times more potent than morphine. Its primary Medici ...
family of drugs. R-30490 was found to be the most selective agonist for the
μ-opioid receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical ...
out of all the fentanyl analogues tested, but it has never been introduced for medical use in humans, although the closely related drug
sufentanil
Sufentanil, sold under the brand names Sufenta among others, is a synthetic opioid analgesic drug approximately 5 to 10 times as potent as its parent drug, fentanyl, and 500 to 1,000 times as potent as morphine. Structurally, sufentanil diff ...
is widely used for analgesia and anesthesia during major surgery.
Side effects of
fentanyl
Fentanyl is a highly potent synthetic piperidine opioid primarily used as an analgesic (pain medication). It is 30 to 50 times more Potency (pharmacology), potent than heroin and 50 to 100 times more potent than morphine. Its primary Medici ...
analogs are similar to those of fentanyl itself, which include
itching
An itch (also known as pruritus) is a sensation that causes a strong desire or reflex to scratch. Itches have resisted many attempts to be classified as any one type of sensory experience. Itches have many similarities to pain, and while both ...
,
nausea
Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. It can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the throat.
Over 30 d ...
and potentially serious
respiratory depression
Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide (hypercapni ...
, 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.
See also
*
Carfentanil
Carfentanil or carfentanyl, formerly sold under the brand name Wildnil, is an extremely potent opioid analgesic used in veterinary medicine to anesthetize large animals such as elephants and rhinoceroses. It is a structural analogue of the ...
*
List of fentanyl analogues
The following is a list of fentanyl Structural analog, analogues (sometimes referred to as fentalogs), and includes both compounds developed by pharmaceutical companies for legitimate medical use, and those which have been sold as designer drugs. ...
*
Opioid potency comparison
References
{{Opioid receptor modulators
Synthetic opioids
Piperidines
Propionamides
Anilides
Mu-opioid receptor agonists
Fentanyl
Ethers