Sumanirol
Агонист D2
Sumanirol (PNU-95,666) je visoko selektivni pun agonist D2 receptora. On je prvi otkriveni agonist iz te grupe.[1][2][3]
IUPAC ime | |
---|---|
(R)-5,6-dihidro-5-(metilamino)-4H-imidazo[4,5,1-ij]hinolin-2(1H)-on | |
Identifikatori | |
CAS broj | 179386-43-7 179386-44-8 (maleat) |
ATC kod | none |
PubChem | CID 9818479 |
ChemSpider | 7994229 |
UNII | 3E93IV1U45 |
Hemijski podaci | |
Formula | C11H13N3O |
Molarna masa | 203,240 g/mol |
|
Sumanirol je razvijen za lečenje Parkinsonove bolesti i sindroma nemirnih nogu. Mada on nije odobren za kliničku upotrebu,[4][5] on je korisno oruđe za bazna istraživanja neurobioloških mehanizama koji su bazirani na modu dejstva dopaminskog D2 receptora (vs. D1, D3, D4, i D5 receptora).[3]
Reference
уреди- ^ 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 (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. PMID 15980060. doi:10.1124/jpet.105.084202.
- ^ а б Weber M, Chang WL, Breier MR, Yang A, Millan MJ, Swerdlow NR (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. PMC 2864324 . PMID 20346635. doi:10.1016/j.euroneuro.2010.02.011.
- ^ Barone P, Lamb J, Ellis A, Clarke Z (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. PMID 17115380. doi:10.1002/mds.21191.
- ^ Garcia-Borreguero D, Winkelman J, Adams A, Ellis A, Morris M, Lamb J, Layton G, Versavel M (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. PMID 17239657. doi:10.1016/j.sleep.2006.05.018.