WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H326794
CAS#: 179386-44-8 (maleate)
Description: Sumanirole, also known as PNU-95666, is a highly selective D2 receptor full agonist, the first of its kind to be discovered. It was developed for the treatment of Parkinson's disease and restless leg syndrome. While it has never been approved for medical use, 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.
Hodoodo Cat#: H326794
Name: Sumanirole maleate
CAS#: 179386-44-8 (maleate)
Chemical Formula: C15H17N3O5
Exact Mass: 0.00
Molecular Weight: 319.320
Elemental Analysis: C, 56.42; H, 5.37; N, 13.16; O, 25.05
Related CAS #: 179386-43-7 (free base) 179386-44-8 (maleate)
Synonym: PNU-95666; PNU 95666; PNU95666; U 95666E; U-95666E; U95666E; Sumanirole maleate
IUPAC/Chemical Name: (R)-5-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one maleate
InChi Key: VOJRMYBBPKNLLI-ORHWHDKWSA-N
InChi Code: InChI=1S/C11H13N3O.C4H4O4/c1-12-8-5-7-3-2-4-9-10(7)14(6-8)11(15)13-9;5-3(6)1-2-4(7)8/h2-4,8,12H,5-6H2,1H3,(H,13,15);1-2H,(H,5,6)(H,7,8)/b;2-1-/t8-;/m1./s1
SMILES Code: O=C1NC2=C3N1C[C@H](NC)CC3=CC=C2.O=C(O)/C=C\C(O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Related CAS# 179386-43-7 (Sumanirole free base). 179386-44-8 (Sumanirole maleate)
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The following data is based on the product molecular weight 319.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
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1: Zou MF, Keck TM, Kumar V, Donthamsetti P, Michino M, Burzynski C, Schweppe C, Bonifazi A, Free RB, Sibley DR, Janowsky A, Shi L, Javitch JA, Newman AH. Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity. J Med Chem. 2016 Apr 14;59(7):2973-88. doi: 10.1021/acs.jmedchem.5b01612. Epub 2016 Apr 1. PubMed PMID: 27035329; PubMed Central PMCID: PMC4915350.
2: Weber M, Chang WL, Breier MR, Yang A, Millan MJ, Swerdlow NR. The effects of the dopamine D2 agonist sumanirole on prepulse inhibition in rats. Eur Neuropsychopharmacol. 2010 Jun;20(6):421-5. doi: 10.1016/j.euroneuro.2010.02.011. Epub 2010 Mar 25. PubMed PMID: 20346635; PubMed Central PMCID: PMC2864324.
3: Singer C, Lamb J, Ellis A, Layton G; Sumanirole for Early Parkinson's Disease Study Group. A comparison of sumanirole versus placebo or ropinirole for the treatment of patients with early Parkinson's disease. Mov Disord. 2007 Mar 15;22(4):476-82. PubMed PMID: 17318839.
4: Garcia-Borreguero D, Winkelman J, Adams A, Ellis A, Morris M, Lamb J, Layton G, Versavel M; Sumanirole in RLS Study Group. Efficacy and tolerability of sumanirole in restless legs syndrome: a phase II, randomized, double-blind, placebo-controlled, dose-response study. Sleep Med. 2007 Mar;8(2):119-27. Epub 2007 Jan 18. PubMed PMID: 17239657.
5: Barone P, Lamb J, Ellis A, Clarke Z. Sumanirole versus placebo or ropinirole for the adjunctive treatment of patients with advanced Parkinson's disease. Mov Disord. 2007 Mar 15;22(4):483-9. PubMed PMID: 17115380.
6: McCall RB, Lookingland KJ, Bédard PJ, Huff RM. Sumanirole, a highly dopamine D2-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease. J Pharmacol Exp Ther. 2005 Sep;314(3):1248-56. Epub 2005 Jun 24. PubMed PMID: 15980060.
7: de Paulis T. Sumanirole Pharmacia. Curr Opin Investig Drugs. 2003 Jan;4(1):77-82. Review. PubMed PMID: 12625034.
