| 词条 | Sumanirole |
| 释义 |
| IUPAC_name = (R)-5,6-Dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one | image = Sumanirole.svg | width = 150 | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | metabolism = | elimination_half-life = | excretion = | IUPHAR_ligand = 3949 | CAS_number = 179386-43-7 | CAS_supplemental = 179386-44-8 (maleate) | ATC_prefix = none | ATC_suffix = | PubChem = 9818479 | ChemSpiderID = 7994229 | ChEMBL = 419792 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 3E93IV1U45 | C=11 | H=13 | N=3 | O=1 | molecular_weight = 203.240 g/mol | smiles = CN[C@@H]1Cc2cccc3[nH]c(=O)n(C1)c23 }}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
References1. ^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. {{Antiparkinsonian}}{{Dopaminergics}}2. ^{{cite journal |vauthors=McCall RB, Lookingland KJ, Bédard PJ, Huff RM |title=Sumanirole, a highly dopamine D2-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=314 |issue=3 |pages=1248–56 |date=September 2005 |pmid=15980060 |doi=10.1124/jpet.105.084202 |url=}} 3. ^1 {{cite journal |vauthors=Weber M, Chang WL, Breier MR, Yang A, Millan MJ, Swerdlow NR |title=The effects of the dopamine D2 agonist sumanirole on prepulse inhibition in rats |journal=European Neuropsychopharmacology |volume= 20|issue= 6|pages= 421–425|date=March 2010 |pmid=20346635 |doi=10.1016/j.euroneuro.2010.02.011 |url= |pmc=2864324}} 4. ^{{cite journal |vauthors=Barone P, Lamb J, Ellis A, Clarke Z |title=Sumanirole versus placebo or ropinirole for the adjunctive treatment of patients with advanced Parkinson's disease |journal=Movement Disorders |volume=22 |issue=4 |pages=483–9 |date=March 2007 |pmid=17115380 |doi=10.1002/mds.21191 |url=}} 5. ^{{cite journal |vauthors=Garcia-Borreguero D, Winkelman J, Adams A, Ellis A, Morris M, Lamb J, Layton G, Versavel M |title=Efficacy and tolerability of sumanirole in restless legs syndrome: a phase II, randomized, double-blind, placebo-controlled, dose-response study |journal=Sleep Medicine |volume=8 |issue=2 |pages=119–27 |date=March 2007 |pmid=17239657 |doi=10.1016/j.sleep.2006.05.018 |url=}} 6. ^{{ cite web|title=Pfizer to Discontinue Sumanirole Development Program|author=Pfizer, Inc.|url=http://www.pdf.org/en/science_news/release/pr_1216748386|publisher=Parkinson's Disease Foundation}} 4 : Amines|Dopamine agonists|Imidazoquinolines|Ureas |
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