Synonym
Brasofensine sulfate; BMS 204756; BMS-204756; NS 2214; NS2214; NS-2214
IUPAC/Chemical Name
(E)-3-(3,4-dichlorophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2-carbaldehyde O-methyl oxime sulfate
InChi Key
MOYPZNPGNIZILM-NPJZCEOMSA-N
InChi Code
InChI=1S/C16H20Cl2N2O.H2O4S/c1-20-11-4-6-16(20)13(9-19-21-2)12(8-11)10-3-5-14(17)15(18)7-10;1-5(2,3)4/h3,5,7,9,11-13,16H,4,6,8H2,1-2H3;(H2,1,2,3,4)/b19-9+;/t11-,12+,13+,16+;/m0./s1
SMILES Code
O=S(O)(O)=O.CO/N=C/[C@@H]1[C@@H](C2=CC=C(Cl)C(Cl)=C2)C[C@]3([H])CC[C@@]1([H])N3C
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
425.33
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 |
1: Zhu M, Whigan DB, Chang SY, Dockens RC. Disposition and metabolism of [14C]brasofensine in rats, monkeys, and humans. Drug Metab Dispos. 2008 Jan;36(1):24-35. doi: 10.1124/dmd.107.016139. Epub 2007 Oct 1. PMID: 17908924.
2: Minuzzi L, Olsen AK, Bender D, Arnfred S, Grant R, Danielsen EH, Cumming P. Quantitative autoradiography of ligands for dopamine receptors and transporters in brain of Göttingen minipig: comparison with results in vivo. Synapse. 2006 Mar 15;59(4):211-9. doi: 10.1002/syn.20234. PMID: 16385509.
3: Doudet DJ, Ruth TJ, Holden JE. Sequential versus nonsequential measurement of density and affinity of dopamine D2 receptors with [11C]raclopride: 2: effects of DAT inhibitors. J Cereb Blood Flow Metab. 2006 Jan;26(1):28-37. doi: 10.1038/sj.jcbfm.9600161. PMID: 15973354.
4: Johnston TH, Brotchie JM. Drugs in development for Parkinson's disease. Curr Opin Investig Drugs. 2004 Jul;5(7):720-6. PMID: 15298067.
5: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 May;25(4):317-40. PMID: 12808477.
6: Pearce RK, Smith LA, Jackson MJ, Banerji T, Scheel-Krüger J, Jenner P. The monoamine reuptake blocker brasofensine reverses akinesia without dyskinesia in MPTP-treated and levodopa-primed common marmosets. Mov Disord. 2002 Sep;17(5):877-86. doi: 10.1002/mds.10238. PMID: 12360536.
7: Frackiewicz EJ, Jhee SS, Shiovitz TM, Webster J, Topham C, Dockens RC, Whigan D, Salazar DE, Cutler NR. Brasofensine treatment for Parkinson's disease in combination with levodopa/carbidopa. Ann Pharmacother. 2002 Feb;36(2):225-30. doi: 10.1345/aph.1A152. PMID: 11847938.
8: Yu P. Brasofensine NeuroSearch. Curr Opin Investig Drugs. 2000 Dec;1(4):504-7. PMID: 11249705.
9: Fischman AJ, Bonab AA, Rubin RH. Regional pharmacokinetics of orally administered PET tracers. Curr Pharm Des. 2000 Nov;6(16):1625-9. doi: 10.2174/1381612003398771. PMID: 10974157.
