Dimebolin dihydrochlorideCAS: 97657-92-6
MF: C21H25N3•2HCl
MW: 392.4
A histamine, AR, and Ca channel inhibitor.

Dimebolin dihydrochloride (CAS 97657-92-6)

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Synonym: 2,8-Dimethyl-5-[2-(6-methyl-3-pyridinyl)ethyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole dihydrochloride
Application: A histamine, AR, and Ca channel inhibitor
CAS Number: 97657-92-6
Molecular Weight: 392.4
Molecular Formula: C21H25N32HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Dimebolin (hydrochloride), also known as Dimebon™, is an orally-available drug, approved in Russia for use as a non-selective antihistamine, that has shown promise in the treatment of neurodegenerative diseases, including Alzheimer′s disease and Huntington′s disease. In addition to preventing the onset and progression of disease by being neuroprotective, Dimebolin appears to promote clinical improvement by increasing cognitive function. At the cellular level, Dimebolin appears to have diverse effects, inhibiting the neurotoxic action of β-amyloid and acting as a calcium channel protein inhibitor, inhibiting NMDA-type glutamate receptors, and preventing mitochondrial leakage.,6,7 The hydrochloride form of Dimebolin is soluble in both aqueous and organic solvents.


References

1 Lermontova, N.N., Lukoyanov, N.V., Serkova, T.P., et al. Dimebon improves learning in animals with experimental Alzheimer′s disease. Bulletin of Experimental Biology and Medicine 129(6) 640-642 (2000). 2 Doody, R.S., Gavrilova, S.I., 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 372 207-215 (2008). 3 Wu, J., Li, Q., Bezprozvanny, I. Evaluation of dimebon in cellular model of Huntington′s disease. Molecular Neurodegeneration (2008). 4 Bachurin, S., Bukatina, E., Lermontova, N., et al. Antihistamine agent dimebon as a novel neuroprotector and a cognition enhancer. Ann N Y Acad Sci 939 425-435 (2001). 5 Lermontova, N.N., Redkozubov, A.E., Shevtsova, E.F., et al. Dimebon and tacrine inhibit neurotoxic action of β-amyloid in culture and block L-type Ca2+ channels. Bulletin of Experimental Biology and Medicine 132(5) 1079-1083 (2001). 6 Grigor′ev, V.V., Dranyi, O.A., Bachurin, S.O. Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons. Bulletin of Experimental Biology and Medicine 136(5) 474-477 (2003). 7 Bachurin, S.O., Shevtsova, E.P., Kireeva, E.G., et al. Mitochondria as a target for neurotoxins and neuroprotective agents. Ann N Y Acad Sci 993 334-344 (2003).

Physical State :
Solid
Solubility :
Soluble in ethanol (~3 mg/ml), DMSO (~10 mg/ml), DMF (~1 mg/ml), PBS, pH 7.2 (~10 mg/ml), and water (>25 mg/ml).
Storage :
Store at -20° C
Melting Point :
220-222° C
Refractive Index :
n20D 1.63
IC50 :
Histamine H1 receptor: IC50 = 0.16 µM (human); 5-HT6 receptor: IC50 = 0.89 µM (human); Butyrylcholinesterase: IC50 = 7.9 µM (human); Acetylcholinesterase: IC50 = 45 µM (human); L-type calcium channel: IC50 = 57 µM
Ki Data :
5-HT7 receptor: Ki= 8 nM (human); 5-HT6 receptor: Ki= 26 nM (human); 5-HT2c receptor: Ki= 76 nM (human); 5-HT1a receptor: Ki>100 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
UV0625000
PubChem CID :
23729232
Merck Index :
14: 10391
MDL Number :
MFCD01617545
SMILES :
CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)CCC4=CN=C(C=C4)C.Cl.Cl

Download SDS (MSDS)

Certificate of Analysis

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