Name: Besipirdine HCl
Synonyms: HP 749
Therapy Type: Small Molecule
Target Type: Other Neurotransmitter Systems
Condition(s): Alzheimer's Disease
U.S. FDA Status: Alzheimer's Disease (Discontinued)
Company: Aventis Pharmaceuticals, Inc. (was Hoechst)
Besipirdine was designed to address two biochemical deficits commonly observed in 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 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).
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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