U-50488 Explained

U-50488 is a drug which acts as a highly selective κ-opioid agonist, but without any μ-opioid antagonist effects.^[1] It has analgesic, diuretic and antitussive effects,^[2] and reverses the memory impairment produced by anticholinergic drugs.^[3] U-50488 was one of the first selective kappa agonists invented and research on its derivatives has led to the development of a large family of related compounds.^{[4] [5]} This compound has never received FDA approval and there are no reported human cases in the literature involving an U-50488 overdose.^[6]

See also

• LPK-26
• U-47700
• U-69,593

Notes and References

1. Von Voigtlander PF, Lewis RA . U-50,488, a selective kappa opioid agonist: comparison to other reputed kappa agonists . Progress in Neuro-Psychopharmacology & Biological Psychiatry . 6 . 4–6 . 467–70 . 1982 . 6298890 . 10.1016/S0278-5846(82)80130-9 . 37011292 .
2. Kamei J . Role of opioidergic and serotonergic mechanisms in cough and antitussives . Pulmonary Pharmacology . 9 . 5–6 . 349–56 . 1996 . 9232674 . 10.1006/pulp.1996.0046 .
3. Hiramatsu M, Kameyama T . Roles of kappa-opioid receptor agonists in learning and memory impairment in animal models . Methods and Findings in Experimental and Clinical Pharmacology . 20 . 7 . 595–9 . September 1998 . 9819804 . 10.1358/mf.1998.20.7.485724 .
4. Szmuszkovicz J . U-50,488 and the kappa receptor: a personalized account covering the period 1973 to 1990 . Progress in Drug Research. Fortschritte der Arzneimittelforschung. Progrès des Recherches Pharmaceutiques . 52 . 167–95 . 1999 . 10.1007/978-3-0348-8730-4_4 . 10396128 .
5. Szmuszkovicz J . U-50,488 and the kappa receptor. Part II: 1991-1998 . Progress in Drug Research. Fortschritte der Arzneimittelforschung. Progrès des Recherches Pharmaceutiques . 53 . 1–51 . 1999 . 10616295 .
6. Amin ZM, Rambaran KA, Fleming SW, Cho K, Chacko L, Alzghari SK . Addressing Hazards from Unscheduled Novel Psychoactive Substances as Research Chemicals: The Case of U-50488 . Cureus . 9 . 12 . e1914 . December 2017 . 29441248 . 5800751 . 10.7759/cureus.1914 . free .