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dimebolin

Basic information Safety Supplier Related

dimebolin Basic information

Product Name:
dimebolin
Synonyms:
  • dimebolin
  • 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-methyl-3-pyridyl)ethyl]-1H-pyrido[4,3-b]indole
  • Dimeboline
  • Dimebone
  • Preparation-84
  • dimebon
  • 2,3,4,5-Tetrahydro-2,8-dimethyl-5-[2-(6-methylpyridin-3-yl)ethyl]-1H-pyrido[4,3-b]indole
CAS:
3613-73-8
MF:
C21H25N3
MW:
319.44
EINECS:
638-815-4
Mol File:
3613-73-8.mol
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dimebolin Chemical Properties

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
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dimebolin Usage And Synthesis

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].

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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