Sumanirol
Sumanirol (PNU-95,666) je visoko selektivni pun agonist D2 receptora. On je prvi otkriveni agonist iz te grupe.[4][5][6]
(IUPAC) ime | |||
---|---|---|---|
(R)-5,6-dihidro-5-(metilamino)-4H-imidazo[4,5,1-ij]hinolin-2(1H)-on | |||
Klinički podaci | |||
Identifikatori | |||
CAS broj | 179386-43-7 179386-44-8 (maleat) | ||
ATC kod | nije dodeljen | ||
PubChem[1][2] | 9818479 | ||
ChemSpider[3] | 7994229 | ||
UNII | 3E93IV1U45 | ||
Hemijski podaci | |||
Formula | C11H13N3O | ||
Mol. masa | 203,240 g/mol | ||
SMILES | eMolekuli & PubHem | ||
| |||
Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status |
Sumanirol je razvijen za lečenje Parkinsonove bolesti i sindroma nemirnih nogu. Mada on nije odobren za kliničku upotrebu,[7][8] 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).[6]
Reference uredi
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.
- ↑ 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.
- ↑ 6,0 6,1 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.