Therapeutics

Besipirdine HCl

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Overview

Name: Besipirdine HCl
Synonyms: HP 749
Therapy Type: Small Molecule
Target Type: Other Neurotransmitters
Condition(s): Alzheimer's Disease
U.S. FDA Status: Alzheimer's Disease (Discontinued)
Company: Aventis Pharmaceuticals, Inc. (was Hoechst)

Background

Besipirdine was designed to address two biochemical deficits commonly observed in the AD brain: cholinergic and adrenergic activity.  This drug has been shown to enhance the activity of both systems (Klein et al., 1996).  Hypoactivity of the cholinergic system is a well-known characteristic of the AD brain. Similarly, AD is associated with loss of locus coeruleus neurons, degeneration of noradrenergic projections, and a decrease in cortical norepinephrine levels (Heneka et al., 2002; Bondareff et al., 1982).

Findings

Besipirdine hydrochloride, an indole-substituted analog of 4-aminopyridine, enhances both cholinergic and adrenergic neurotransmission in the central nervous system. It has been shown to have a high affinity for α2-adrenergic receptors (much lower affinity for α1-adrenergic receptors) and also to modulate cholinergic neurotransmission through unspecified mechanisms (Klein et al., 1996).

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References

Paper Citations

  1. . Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. J Med Chem. 1996 Jan 19;39(2):570-81. PubMed.
  2. . Noradrenergic depletion potentiates beta -amyloid-induced cortical inflammation: implications for Alzheimer's disease. J Neurosci. 2002 Apr 1;22(7):2434-42. PubMed.
  3. . Loss of neurons of origin of the adrenergic projection to cerebral cortex (nucleus locus ceruleus) in senile dementia. Neurology. 1982 Feb;32(2):164-8. PubMed.

Further Reading

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