Sumanirole
 | |
| Clinical data | |
|---|---|
| ATC code | none |
| Identifiers | |
| |
| CAS Number |
179386-43-7 179386-44-8 (maleate) |
| PubChem (CID) | 9818479 |
| IUPHAR/BPS | 3949 |
| ChemSpider | 7994229 |
| UNII |
3E93IV1U45  |
| ChEMBL | CHEMBL419792 |
| Chemical and physical data | |
| Formula | C11H13N3O |
| Molar mass | 203.240 g/mol |
| 3D model (Jmol) | Interactive image |
| |
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
References
- ↑ 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.
- ↑ McCall RB, Lookingland KJ, Bédard PJ, Huff RM (September 2005). "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. doi:10.1124/jpet.105.084202. PMID 15980060.
- 1 2 Weber M, Chang WL, Breier MR, Yang A, Millan MJ, Swerdlow NR (March 2010). "The effects of the dopamine D2 agonist sumanirole on prepulse inhibition in rats". European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology. 20 (6): 421–425. doi:10.1016/j.euroneuro.2010.02.011. PMC 2864324
. PMID 20346635. - ↑ Barone P, Lamb J, Ellis A, Clarke Z (March 2007). "Sumanirole versus placebo or ropinirole for the adjunctive treatment of patients with advanced Parkinson's disease". Movement Disorders : Official Journal of the Movement Disorder Society. 22 (4): 483–9. doi:10.1002/mds.21191. PMID 17115380.
- ↑ Garcia-Borreguero D, Winkelman J, Adams A, Ellis A, Morris M, Lamb J, Layton G, Versavel M (March 2007). "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. doi:10.1016/j.sleep.2006.05.018. PMID 17239657.
- ↑ Pfizer, Inc. "Pfizer to Discontinue Sumanirole Development Program" (PDF). Parkinson's Disease Foundation.
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