| Identification | Back Directory | [Name]
9-AMINO-1,2,3,4-TETRAHYDRO-ACRIDIN-1-OL, MALEATE | [CAS]
118909-22-1 | [Synonyms]
HP-029
Mentane
P 83-6029A
Velnacrine maleate
HYDROXYTACRINE MALEATE
Velnacrine maleate [usan]
1-hydroxy tacrine Maleate
Velnacrine Maleate(HP-029)
HYDROXYTACRINE MALEATE SALT
Velnacrine Hydrogen Maleate
9-AMINO-1,2,3,4-TETRAHYDRO-ACRIDIN-1-OL, MALEATE
(±)-9-Amino-1,2,3,4-tetrahydroacridin-1-ol, HP-029
9-Amino-1-hydroxy-1,2,3,4-tetrahydroacridine maleate
9-AMINO-1,2,3,4-TETRAHYDRO-ACRIDINE-1-(2H)-OL MALEATE
9-AMino-1,2,3,4-tetrahydro-1-acridinol (2Z)-2-Butenedioate
9-Amino-1,2,3,4-tetrahydroacridin-1-ol maleate, 9-Amino-1,2,3,4-tetrahydroacridin-1-ol (2Z)-but-2-enedioate | [Molecular Formula]
C17H18N2O5 | [MDL Number]
MFCD00069287 | [MOL File]
118909-22-1.mol | [Molecular Weight]
330.34 |
| Chemical Properties | Back Directory | [Melting point ]
171-173 | [storage temp. ]
-20°C Freezer | [solubility ]
Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly) | [form ]
White solid. | [color ]
Pale Beige to Beige | [Stability:]
Store in freezer at -20°C |
| Safety Data | Back Directory | [Hazard Codes ]
T | [Hazard Note ]
Toxic | [HS Code ]
2933998090 | [Toxicity]
LD50 in mice (mg/kg): 136 orally; 162 i.p. (Shutske 1988, 1989) |
| Hazard Information | Back Directory | [Originator]
Velnacrine maleate SM 10.888,Hoechst-Roussel (Aventis) Sumitimo JPN | [Uses]
A potential Alzheimer Disease therapeutic of low toxicity. Exhibits biochemical and pharmacological profile similar to THA except that it is far less toxic and without measurable liver toxicity in humans | [Uses]
A potential Alzheimer's Disease therapeutic of low toxicity. Exhibits biochemical and pharmacological profile similar to THA except that it is far less toxic and without measurable liver toxicity in humans. | [Manufacturing Process]
In 100 ml of tetrahydrofuran was added 5.00 g of 9-amino-3,4-dihydroacridin-
1(2)-one. The mechanically stirred suspension was cooled to -5°C and 21.4 ml
(1 eq.) of 1.1 M LiAlH 4 solution in ether was added dropwise. After completion
of the addition, the reaction mixture was stirred further for 2 hours,
whereupon the reaction complete based on thin chromatography analysis. The
LiAlH 4 was neutralized with 2 ml of saturated NH 4 Cl and the salts were
dissolved with 30% potassium hydroxide. The insoluble product was filtered
off and rinsed with water. The precipitate was then dissolved in 3 N
hydrochloric acid and the residual insoluble salts filtered off. The acid solution
washed with ethyl acetate and made basic (pH 9) with 10% sodium
hydroxide. The precipitated product was filtered and washed with water. After
drying at 80°C under vacuum overnight, 4.15 g (82%) of (+/-)-9-amino-
1,2,3,4-tetrahydro-1-acridinol was obtained, melting point 245°C. (+/-)-9-
Amino-1,2,3,4-tetrahydro-1-acridinol maleate has melting point 171-173°C. | [Brand name]
Mentane (Hoechst-Roussel). | [Therapeutic Function]
Cholinesterase inhibitor, Cognition activator | [Biological Activity]
Cholinesterase inhibitor. Potential Alzheimer's disease therapeutic. | [References]
[1]. d. muoz-torrero. acetylcholinesterase inhibitors as disease-modifying therapies for alzheimer’s disease. curr. med. chem. 15, 2433-2455 (2008).
[2]. e. giacobini. cholinesterase inhibitors for alzheimer’s disease therapy: from tacrine to future applications. neurochemistry international 32, 413-419(1998).
[3]. birks j s. cholinesterase inhibitors for alzheimer's disease[j]. the cochrane library, 2006.
[4]. peng j z, remmel r p, sawchuk r j. inhibition of murine cytochrome p4501a by tacrine: in vitro studies[j]. drug metabolism and disposition, 2004, 32(8): 805-812.
[5]. acetylcholine and choline effects on erythrocyte nitrite and nitrate levels. |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|