Brasofensine

Cas：171655-91-7

Product Information：

Brasofensine is a monoamine reuptake blocker is a phenyltropane that had been under development for the treatment of Parkinson's and Alzheimer's disease. In animal models of Parkinson's disease, brasofensine was effective in stimulating LMA and reversing akinesia. The (Z)-isomer has been consigned the name BMS-205912.

Synonym:

(E)-1R,2R,3S-3-(3,4-dichlorophenyl)-8-methyl-8-azabicyclo(3.2.1)octane-2-carbaldehyde O-methyloxime

BMS 204756

brasofensine

NS2214

Chemical Name: 

3beta-(3,4-Dichlorophenyl)-1alphaH,5alphaH-tropane-2alpha-carboxaldehyde (E)-(O-methyloxime)

InChi Key: 

NRLIFEGHTNUYFL-MTKJPOGLSA-N

InChi Code: 

InChI=1S/C16H20Cl2N2O/c1-20-11-4-6-16(20)13(9-19-21-2)12(8-11)10-3-5-14(17)15(18)7-10/h3,5,7,9,11-13,16H,4,6,8H2,1-2H3/b19-9+/t11?,12-,13-,16?/m1/s1

Smiles Code:

CN1C2CCC1[C@@H]([C@H](C2)c3ccc(c(c3)Cl)Cl)/C=N/OC

Technical Data：

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, not in water

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

References：

1. 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. PubMed PMID: 11847938.

2. 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. PubMed PMID: 12360536.

3. Johnston TH, Brotchie JM. Drugs in development for Parkinson's disease. Curr Opin Investig Drugs. 2004 Jul;5(7):720-6. Review. PubMed PMID: 15298067.

4. 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. PubMed PMID: 15973354.

5. 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. Epub 2007 Oct 1. PubMed PMID: 17908924.