Diphenpipenol Explained

Diphenpipenol is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co.^[1] It is chemically a 1-substituted-4-(1,2-diphenylethyl)piperazine derivative related to compounds such as MT-45 and AD-1211, but diphenpipenol is the most potent compound in the series, with the more active (S) enantiomer being around 105 times the potency of morphine in animal studies.^[2] This makes it a similar strength to fentanyl and its analogues, and consequently diphenpipenol can be expected to pose a significant risk of producing life-threatening respiratory depression, as well as other typical opioid side effects such as sedation, itching, nausea and vomiting.

Diphenpipenol has been offered for sale online as a designer drug, though analysis of a sample of supposed diphenpipenol found it to instead contain a structural isomer with much weaker opioid activity, and it is unclear if genuine diphenpipenol has actually been sold.^[3]

See also

• 3C-PEP
• Azaprocin
• Bucinnazine
• Diphenidine
• Lefetamine

Notes and References

1. US . 4080453 . 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives and compositions containing the same. . 21 March 1978 . Nishimura H, Uno H, Natsuka, Shimokawa N, Shimizu M, Nakamura H . Dainippon Pharmaceutical Co Ltd .
2. Natsuka K, Nakamura H, Nishikawa Y, Negoro T, Uno H, Nishimura H . Synthesis and structure-activity relationships of 1-substituted 4-(1,2-diphenylethyl)piperazine derivatives having narcotic agonist and antagonist activity . Journal of Medicinal Chemistry . 30 . 10 . 1779–87 . October 1987 . 3656354 . 10.1021/jm00393a017 .
3. Cannaert A, Hulpia F, Risseeuw M, Van Uytfanghe K, Deconinck E, Van Calenbergh S, Blanckaert P, Stove C . 6 . Report on a new opioid NPS: chemical and in vitro functional characterization of a structural isomer of the MT-45 derivative diphenpipenol . Journal of Analytical Toxicology . June 2020 . 45 . 2 . 134–140 . 32514558 . 10.1093/jat/bkaa066 . 1854/LU-8664239 . free .