Chemistry:Β-Funaltrexamine
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β-Funaltrexamine (β-FNA) is an irreversible (covalently bonding) opioid antagonist that was used to create the first crystal structure of the μ-opioid receptor (MOR).[1] It is selective for antagonism of the MOR over the δ-opioid receptor (DOR) and κ-opioid receptor (KOR).[2] Chemically, it is a naltrexone derivative with a methyl-fumaramide group in the 6-position. In addition to its MOR irreversible antagonism, β-FNA is a reversible agonist of the κ-opioid receptor (KOR) and produces KOR-mediated analgesic effects in animals.[2][3][4] This has limited its usefulness and contributed to the development of methocinnamox as a more selective functionally irreversible antagonist of the MOR with no significant opioid agonistic actions.[3]
See also
- Naltrexamine
- β-Chlornaltrexamine
- β-Fuoxymorphamine
References
- ↑ "Crystal structure of the µ-opioid receptor bound to a morphinan antagonist". Nature 485 (7398): 321–6. March 2012. doi:10.1038/nature10954. PMID 22437502. Bibcode: 2012Natur.485..321M.
- ↑ 2.0 2.1 "Pharmacological profiles of beta-funaltrexamine (beta-FNA) and beta-chlornaltrexamine (beta-CNA) on the mouse vas deferens preparation". Eur J Pharmacol 80 (4): 377–384. June 1982. doi:10.1016/0014-2999(82)90083-8. PMID 6286325.
- ↑ 3.0 3.1 "Methocinnamox is a potent, long-lasting, and selective antagonist of morphine-mediated antinociception in the mouse: comparison with clocinnamox, beta-funaltrexamine, and beta-chlornaltrexamine". J Pharmacol Exp Ther 294 (3): 933–940. September 2000. PMID 10945843.
- ↑ "Mu antagonist and kappa agonist properties of beta-funaltrexamine (beta-FNA) in vivo: long-lasting spinal analgesia in mice". J Pharmacol Exp Ther 252 (3): 1006–1011. March 1990. PMID 2156986.
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