dimebolin
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
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
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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- dimebolin
- 2,8-Dimethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole
- 2,5-Dimethylindole
- 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indole
- (1-Methyl-1H-indol-3-yl)-methylamine
- 1-METHYL-4,5,6,7-TETRAHYDRO-1H-PYRROLO[3,2-C]PYRIDINE
- 2-METHYL-3-N,N-DIMETHYLAMINOMETHYLINDOLE
- 2,3,4,5-TETRAHYDRO-8-METHYL-1H-PYRIDO[4,3-B]INDOLE
- 1H-PYRROLE-3-METHANAMINE, 1-METHYL-
- RARECHEM AN KA 0161
- METHYL-(5-METHYL-1H-INDOL-3-YLMETHYL)-AMINE
- 2-(6-METHYLPYRIDIN-3-YL)ETHANAMINE