7-PET is an opioid analgesic drug that has 300 times the potency of morphine by weight.[1] It was discovered by K.W. Bentley[2] and is related to the more well known oripavine derivative etorphine, which is used as a veterinary painkiller and anesthetic medication for the sedation of large animals such as elephants, giraffes, and rhinos. 7-PET itself has a 3-O-methyl ether which reduces potency, but the 3-OH derivative is around 2200 times more potent than morphine, almost the same potency as etorphine as a μ agonist,[3][4] and unexpectedly the 3-hydrogen compound is also around the same potency of 2000 times morphine.[5]
Unlike etorphine, 7-PET is not controlled under the UN drug conventions, but it might still be considered to be a controlled substance analogue of etorphine on the grounds of its related chemical structure in some jurisdictions such as the United States, Canada, Australia, and New Zealand.
See also
- 14-Cinnamoyloxycodeinone
- 14-Phenylpropoxymetopon
- BU72
- N-Phenethylnormorphine
- N-Phenethyl-14-ethoxymetopon
- Phenomorphan
- RAM-378
- Ro4-1539
References
- ^ Lewis JW, Bentley KW, Cowan A (1971). "Narcotic analgesics and antagonists". Annual Review of Pharmacology. 11: 241–270. doi:10.1146/annurev.pa.11.040171.001325. PMID 4948499.
- ^ Bentley KW, Hardy DG, Meek B (June 1967). "Novel analgesics and molecular rearrangements in the morphine-thebaine group. II. Alcohols derived from 6,14-endo-etheno- and 6,14-endo-ethanotetrahydrothebaine". Journal of the American Chemical Society. 89 (13): 3273–3280. doi:10.1021/ja00989a031. PMID 6042763.
- ^ Feinberg AP, Creese I, Snyder SH (November 1976). "The opiate receptor: a model explaining structure-activity relationships of opiate agonists and antagonists". Proceedings of the National Academy of Sciences of the United States of America. 73 (11): 4215–4219. Bibcode:1976PNAS...73.4215F. doi:10.1073/pnas.73.11.4215. PMC 431391. PMID 186791.
- ^ Bentley KW, Lewis JW (1973). Kosterlitz HW, Collier HO, Villarreal JE (eds.). Agonist and Antagonist Actions of Narcotic Analgesic Drugs. Baltimore: University Park Press. pp. 7–16. ISBN 978-0839107255. LCCN 72012612.
- ^ Lewis JW, Readhead MJ (May 1970). "Novel analgetics and molecular rearrangements in the morphine-thebaine group. 18. 3-deoxy-6,14-endo-etheno-6,7,8,14-tetrahydrooripavines". Journal of Medicinal Chemistry. 13 (3): 525–527. doi:10.1021/jm00297a041. PMID 5441135.