Sumanirole Explained

Sumanirole (PNU-95,666) is a highly selective D₂ receptor full agonist, the first of its kind to be discovered.^{[1] [2] [3]} It was developed for the treatment of Parkinson's disease and restless leg syndrome. While it has never been approved for medical use ^{[4] [5]} it is a highly valuable tool compound for basic research to identify neurobiological mechanisms that are based on a dopamine D₂-linked (vs. D₁-, D₃-, D₄-, and D₅-linked) mechanism of action.^[3]

In 2004, Pfizer announced the end of their clinical development program for sumanirole, citing “recent studies that failed to sufficiently distinguish sumanirole from currently available therapies”.^[6]

See also

• Ropinirole
• PNU-91356A

Notes and References

1. Romero AG, et al. Synthesis of the selective D2 receptor agonist PNU-95666E from D-phenylalanine using a sequential oxidative cyclization strategy. Journal of Organic Chemistry. 1997; 62(19):6582.
2. McCall RB, Lookingland KJ, Bédard PJ, Huff RM . Sumanirole, a highly dopamine D2-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease . The Journal of Pharmacology and Experimental Therapeutics . 314 . 3 . 1248–56 . September 2005 . 15980060 . 10.1124/jpet.105.084202 . 9835081 .
3. Weber M, Chang WL, Breier MR, Yang A, Millan MJ, Swerdlow NR . The effects of the dopamine D2 agonist sumanirole on prepulse inhibition in rats . European Neuropsychopharmacology . 20. 6. 421–425. March 2010 . 20346635 . 10.1016/j.euroneuro.2010.02.011 . 2864324.
4. Barone P, Lamb J, Ellis A, Clarke Z . Sumanirole versus placebo or ropinirole for the adjunctive treatment of patients with advanced Parkinson's disease . Movement Disorders . 22 . 4 . 483–9 . March 2007 . 17115380 . 10.1002/mds.21191 . 20961008 .
5. Garcia-Borreguero D, Winkelman J, Adams A, Ellis A, Morris M, Lamb J, Layton G, Versavel M . Efficacy and tolerability of sumanirole in restless legs syndrome: a phase II, randomized, double-blind, placebo-controlled, dose-response study . Sleep Medicine . 8 . 2 . 119–27 . March 2007 . 17239657 . 10.1016/j.sleep.2006.05.018 .
6. Web site: Pfizer to Discontinue Sumanirole Development Program. Pfizer, Inc.. Parkinson's Disease Foundation.