| Identification | Back Directory | [Name]
dimebolin | [CAS]
3613-73-8 | [Synonyms]
dimebon
Dimebone
dimebolin
Dimeboline
Brn 0622478
Latrepirdine
Preparation-84
DiMebon (latrepirdine)
Dimebon dihydrochloride
Dimebolin-Dihydrochloride
DiMebon dihydrochloride hydrate
2,8-dimethyl-5-[2-(6-methylpyridin-3-yl)ethyl]-3,4-dihydro-1H-pyrido[4,3-b]indole
2,3,4,5-Tetrahydro-2,8-dimethyl-5-(2-(6-methyl-3-pyridyl)-ethyl)-1H-pyrid(4,3B)indole
2,3,4,5-Tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridyl)ethyl]-1H-pyrido[4,3-b]indole
2,3,4,5-Tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridinyl)ethyl]-1H-pyrido[4,3-b]indole
2,3,4,5-Tetrahydro-2,8-dimethyl-5-[2-(6-methylpyridin-3-yl)ethyl]-1H-pyrido[4,3-b]indole
1H-Pyrido(4,3-B)indole, 2,3,4,5-tetrahydro-2,8-dimethyl-5-(2-(6-methyl-3-pyridyl)ethyl)-
2,8-DiMethyl-5-[2-(6-Methyl-3-pyridinyl)ethyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole
2,8-Dimethyl-5-[2-(6-methyl-pyridin-3-yl)-ethyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole
2,8-Dimethyl-5-[2-(6-methyl-pyridin-3-yl)-ethyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Dimebolin | [EINECS(EC#)]
1312995-182-4 | [Molecular Formula]
C21H25N3 | [MDL Number]
MFCD00387540 | [MOL File]
3613-73-8.mol | [Molecular Weight]
319.44 |
| Chemical Properties | Back Directory | [Melting point ]
115-116 °C | [Boiling point ]
448.46°C (rough estimate) | [density ]
1.13 | [refractive index ]
1.6380 (estimate) | [storage temp. ]
Store at -20°C | [solubility ]
≤30mg/ml in ethanol;1mg/ml in DMSO;3mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
9.05±0.20(Predicted) | [CAS DataBase Reference]
3613-73-8 |
| Hazard Information | Back Directory | [Uses]
Non-steroidal anti-inflammatory with analgesic and antipyretic effects | [Definition]
ChEBI: Latrepirdine is a member of methylpyridines and a pyridoindole. It has a role as a geroprotector. | [Biological Activity]
dimebolin is an orally-available antihistamine drug with a long history of clinical use in russia [1][2][3][4].dimebolin has been proposed to be useful for treating neurodegenerative disorders, including alzheimer's disease (ad) and huntington's disease (hd). dimebon might exhibit efficacy by blocking nmda receptors or voltage-gated ca2+ channels and by preventing mitochondrial permeability pore transition [3].dimebolin is an orally-available antihistamine drug. dimebon improved survival of cerebellar granule cells during long-term incubation with aβ25-35. dimebolin also blocked potential-dependent ca(2+) entry into neurons by about 20% by blocking l-type ca(2+) channels [4]. in the cerebellum cell culture, dimebolin protected neurons against the neurotoxic action of aβ25-35 with ec50 value of 25 μm. on isolated rat ileum intestine, dimebolin displayed ca2+-blocking properties with ic50 value of 57 μm. dimebon also exhibited anticholinesterase activity with ic50 values of 7.9 μm and 42 μm for butyryl-choline esterase and acetylcholine esterase, respectively [5].in rats treated with the neurotoxin af64a, dimebolin exhibited cognition and memory-enhancing properties. in mice, dimebolin prevented nmda-induced seizures with ec50 value of 42 ± 6 mg/kg [5]. | [in vivo]
Latrepirdine treatment of TgCRND8 transgenic mice is associated with improved learning behavior and with a reduction in accumulation of Aβ42 and α-synuclein. Male, 90-day-old TgCRND8 mice or their wild-type littermates (nTg) receive 31 consecutive once daily i.p. injections of either 3.5 mg/kg Latrepirdine or 0.9% saline (vehicle). At the culmination of treatment, mice are tested for cued and contextual fear conditioning using a paradigm that has been widely accepted for evaluating learning and memory deficits in APP transgenic mice. A significant increase in cued memory only among Latrepirdine-versus vehicle-treated TgCRND8 mice (p=0.01) is observed. A weak, non-significant trend toward an improvement in contextual memory among Latrepirdine-versus vehicle-treated mice (p=0.099) is also observed[1]. | [storage]
Store at -20°C | [References]
[1]. lermontova nn, lukoyanov nv, serkova tp, et al. dimebon improves learning in animals with experimental alzheimer's disease. bull exp biol med. 2000 jun;129(6):544-6.
[2]. doody rs, gavrilova si, sano m, et al. effect of dimebon on cognition, activities of daily living, behaviour, and global function in patients with mild-to-moderate alzheimer's disease: a randomised, double-blind, placebo-controlled study. lancet. 2008 jul 19;372(9634):207-15.
[3]. wu j, li q, bezprozvanny i. evaluation of dimebon in cellular model of huntington's disease. mol neurodegener. 2008 oct 21;3:15.
[4]. lermontova nn, redkozubov ae, shevtsova ef, et al. dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block l-type ca(2+) channels. bull exp biol med. 2001 nov;132(5):1079-83.
[5]. bachurin s, bukatina e, lermontova n, et al. antihistamine agent dimebon as a novel neuroprotector and a cognition enhancer. ann n y acad sci. 2001 jun;939:425-35. |
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Jia Xing Isenchem Co.,Ltd
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SPIRO PHARMA
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www.spiropharma.com.cn |
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