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Sumanirole

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Sumanirole
Clinical data
Other namesPNU-95,666
ATC code
  • none
Identifiers
  • (R)-5,6-Dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC11H13N3O
Molar mass203.245 g·mol−1
3D model (JSmol)
  • CN[C@@H]1Cc2cccc3[nH]c(=O)n(C1)c23

Sumanirole (PNU-95,666) is a highlyselectiveD2 receptorfull agonist, the first of its kind to be discovered.[1][2][3] It was developed for the treatment ofParkinson's disease andrestless 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

[edit]

References

[edit]
  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. ^abWeber 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.


Dopaminergics
DAprecursors
DA receptoragonists
MAO-Binhibitors
COMTinhibitors
AAADinhibitors
Anticholinergics
Others
D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists
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