Sumanirole

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]

Sumanirole

Clinical data
Other names	PNU-95,666
ATC code	none
Identifiers
IUPAC name (R)-5,6-Dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one
CAS Number	179386-43-7 179386-44-8 (maleate)
PubChem CID	9818479
IUPHAR/BPS	3949
ChemSpider	7994229
UNII	3E93IV1U45
ChEMBL	ChEMBL419792
CompTox Dashboard (EPA)	DTXSID00870144
Chemical and physical data
Formula	C11H13N3O
Molar mass	203.245 g·mol−1
3D model (JSmol)	Interactive image
SMILES CN[C@@H]1Cc2cccc3[nH]c(=O)n(C1)c23

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

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 (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. S2CID 9835081.
3. 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. 20 (6): 421–425. doi:10.1016/j.euroneuro.2010.02.011. PMC 2864324. PMID 20346635.
4. 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. 22 (4): 483–9. doi:10.1002/mds.21191. PMID 17115380. S2CID 20961008.
5. 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.
6. Pfizer, Inc. "Pfizer to Discontinue Sumanirole Development Program". Parkinson's Disease Foundation.