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Encyclopedia > Dimebon
Dimebon
Systematic (IUPAC) name
2,3,4,5-Tetrahydro-2,8-dimethyl-5-(2-(6-methyl-3-pyridyl)ethyl)-

1H-pyrido(4,3-b)indole IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ...

Identifiers
CAS number 3613-73-8
ATC code  ?
PubChem 197033
Chemical data
Formula C21H25N3 
Mol. mass 319.443 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

? CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... PubChem is a database of chemical molecules. ... This article or section does not cite any references or sources. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Standard atomic weight 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... It has been suggested that Effective half-life be merged into this article or section. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ...

Legal status
Routes  ?

Dimebon (Dimebolin) is an antihistamine drug which has been used clinically in Russia since 1983.[1] The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... An antihistamine is a drug which serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions, through action at the histamine receptor. ...


Recently Dimebolin has attracted renewed interest after being shown to have positive effects on persons suffering from Alzheimer’s disease. Animal studies showing potential beneficial effects on Alzheimer's disease models were shown in Russian research in 2000.[2] Preliminary results from human trials have also been promising. In an initial six-month phase II trial, results have shown that at 12 months there was significant improvement over placebo. [3] Alzheimer redirects here. ...



Dimebolin is an orally active small molecule that has been shown to inhibit brain cell death in preclinical studies of Alzheimer's disease and Huntington's disease, making it a potential treatment for these and other neurodegenerative diseases. Research suggests that Dimebon may also have cognition-enhancing effects in healthy individuals, in the absence of neurodegenerative disease pathology.[4] Huntingtons disease or Huntingtons chorea (HD) is an inherited disorder characterized by abnormal body movements called chorea, and loss of memory. ...



Dimebon appears to operate through multiple mechanisms of action, both blocking the action of neurotoxic beta-amyloid proteins and inhibiting L-type calcium channels,[5] modulating the action of AMPA and NMDA glutamate receptors,[6] and may exert a neuroprotective effect by blocking a novel target that involves mitochondrial pores,[7] which are believed to play a role in the cell death that is associated with neurodegenerative diseases and the aging process. [8] Research is continuing in both Russia and western nations into the potential applications of Dimebon as a neuroprotective and potential nootropic. [9] Amyloid beta (Aβ or Abeta) is a protein fragment of 39-42 amino acids that is the main constituent of amyloid plaques in various neurological disorders, most prominently Alzheimers disease. ... Another, unrelated ion channeling process is part of ion implantation. ... The α-amino-3-hydroxy-5-methylisoxazole-4- propionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor) is a non-NMDA-type ionotropic transmembrane receptor for glutamate that mediates fast synaptic transmission in the central nervous system (CNS). ... The NMDA receptor (NMDAR) is an ionotropic receptor for glutamate (NMDA (N-methyl d-aspartate) is a name of its selective specific agonist). ... Nootropics, popularly referred to as smart drugs and smart nutrients, are substances which boost human cognitive abilities (the functions and capacities of the brain). ...


References

  1. ^ Matveeva IA. Action of dimebon on histamine receptors. Farmakologiia i Toksikologiia. 1983 Jul-Aug;46(4):27-9. (Russian)
  2. ^ Lermontova NN, Lukoyanov NV, Serkova TP, Lukoyanova EA, Bachurin SO. Dimebon improves learning in animals with experimental Alzheimer's disease. Bulletin of Experimental Biology and Medicine. 2000 Jun;129(6):544-6.
  3. ^ Antihistamine Shows Promise in Treating Alzheimer’s, NYTimes.com, [[1]]
  4. ^ Bachurin S, Bukatina E, Lermontova N, Tkachenko S, Afanasiev A, Grigoriev V, Grigorieva I, Ivanov Y, Sablin S, Zefirov N. Antihistamine agent Dimebon as a novel neuroprotector and a cognition enhancer. Annals of the New York Academy of Sciences. 2001 Jun;939:425-35.
  5. ^ Lermontova NN, Redkozubov AE, Shevtsova EF, Serkova TP, Kireeva EG, Bachurin SO. Dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block L-type Ca(2+) channels. Bulletin of Experimental Biology and Medicine. 2001 Nov;132(5):1079-83.
  6. ^ Grigorev VV, Dranyi OA, Bachurin SO. Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons. Bull Exp Biol Med. 2003 Nov;136(5):474-7.
  7. ^ Bachurin SO, Shevtsova EP, Kireeva EG, Oxenkrug GF, Sablin SO. Mitochondria as a target for neurotoxins and neuroprotective agents. Annals of the New York Academy of Sciences. 2003 May;993:334-44
  8. ^ http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=104&STORY=/www/story/06-11-2007/0004605280&EDATE=
  9. ^ Shevtsova EF, Kireeva EG, Bachurin SO. Mitochondria as the target for neuroprotectors. Vestnik Rossiiskoi Akademii Meditsinskikh Nauk. 2005;(9):13-7. (Russian)

 
 

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