Chemistry:U-69,593
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Short description: Chemical compound
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| Formula | C22H32N2O2 |
| Molar mass | 356.510 g·mol−1 |
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U-69,593 is a drug which acts as a potent and selective κ1-opioid receptor agonist.[1][2][3] In animal studies it has been shown to produce antinociception,[1][4][5] anti-inflammation,[6] anxiolysis (at low doses),[7][8][9] respiratory depression,[5] and diuresis,[10] while having little effect on gastrointestinal motility.[1] It also inhibits the peripheral, though not central secretion of oxytocin and vasopressin in rats.[11][12]
See also
- U-50,488
- The dichloro analog is called spiradoline.
References
- ↑ 1.0 1.1 1.2 "Interaction of U-69,593 with mu-, alpha- and kappa-opioid binding sites and its analgesic and intestinal effects in rats". Life Sciences 42 (3): 293–301. 1988. doi:10.1016/0024-3205(88)90638-8. PMID 2826959.
- ↑ Frey HH (March 1988). "Effect of mu- and kappa-opioid agonists on the electroconvulsive seizure threshold in mice and antagonism by naloxone and MR 2266". Pharmacology & Toxicology 62 (3): 150–4. doi:10.1111/j.1600-0773.1988.tb01863.x. PMID 2836842.
- ↑ "Characterization and visualization of rat and guinea pig brain kappa opioid receptors: evidence for kappa 1 and kappa 2 opioid receptors". Proceedings of the National Academy of Sciences of the United States of America 85 (11): 4061–5. June 1988. doi:10.1073/pnas.85.11.4061. PMID 2836869. Bibcode: 1988PNAS...85.4061Z.
- ↑ "Kappa-opioid receptor-mediated antinociception in the rat. II. Supraspinal in addition to spinal sites of action". The Journal of Pharmacology and Experimental Therapeutics 251 (1): 342–50. October 1989. PMID 2571723. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=2571723.
- ↑ 5.0 5.1 "Comparison of kappa opioids in rhesus monkeys: behavioral effects and receptor binding affinities". The Journal of Pharmacology and Experimental Therapeutics 268 (1): 47–58. January 1994. PMID 8301589. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8301589.
- ↑ "Analgesic and antiinflammatory effects of two novel kappa-opioid peptides". Anesthesiology 94 (6): 1034–44. June 2001. doi:10.1097/00000542-200106000-00018. PMID 11465595. https://dx.doi.org/10.1097/00000542-200106000-00018.
- ↑ "Kappa opioid agonists produce anxiolytic-like behavior on the elevated plus-maze". Psychopharmacology 118 (4): 444–50. April 1995. doi:10.1007/BF02245945. PMID 7568631.
- ↑ "U-69,593 microinjection in the infralimbic cortex reduces anxiety and enhances spontaneous alternation memory in mice". Brain Research 856 (1–2): 259–80. February 2000. doi:10.1016/S0006-8993(99)01990-3. PMID 10677636.
- ↑ "Concurrent modulation of anxiety and memory". Behavioural Brain Research 109 (2): 229–41. May 2000. doi:10.1016/S0166-4328(99)00177-1. PMID 10762693.
- ↑ "Differential effects of fedotozine compared to other kappa agonists on diuresis in rats". The Journal of Pharmacology and Experimental Therapeutics 279 (3): 1379–85. December 1996. PMID 8968362. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8968362.
- ↑ "The opioid receptor subtypes mu and kappa, but not delta, are involved in the control of the vasopressin and oxytocin release in the rat". European Journal of Pharmacology 209 (3): 199–206. December 1991. doi:10.1016/0014-2999(91)90170-U. PMID 1665795.
- ↑ "Prevention by morphine of apomorphine- and oxytocin-induced penile erection and yawning: site of action in the brain". Neuropsychopharmacology 6 (1): 17–21. January 1992. PMID 1315136.
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