Name:	Besipirdine HCl
Other Names:	HP 749
Development Status:	investigational in U.S.
FDA Phase:	Discontinued
Pharmacological Role:	Besipirdine hydrochloride, an indole-substituted analog of 4-aminopyridine, enhances both cholinergic and adrenergic neurotransmission in the central nervous system, and may have greater efficacy than purely cholinergic agents in treating dementia due to Alzheimer's disease.
Companies:	Aventis Pharmaceuticals, Inc. (was Hoechst)

References

Huff FJ, Antuono PG, Delagandara JE, McDonald MA, Cutler NR, Cohen SR, Green RC, Zemlan FP, Crismon ML, Alter M, Shipley JE, Reichman WE. A treatment and withdrawal trial of besipirdine in Alzheimer disease. Alzheimer Dis Assoc Disord. 1996 Summer;10(2):93-102. Abstract

Klein JT, Davis L, Olsen GE, Wong GS, Huger FP, Smith CP, Petko WW, Cornfeldt M, Wilker JC, Blitzer RD, Landau E, Haroutunian V, Martin LL, Effland RC. 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. Abstract

Huff FJ. Preliminary evaluation of besipirdine for the treatment of Alzheimer's disease. Besipirdine Study Group. Ann N Y Acad Sci. 1996 Jan 17;777:410-4. Abstract

Sramek JJ, Viereck C, Huff FJ, Wardle T, Hourani J, Stewart JA, Cutler NR. A 'bridging' (safety/tolerance) study of besipirdine hydrochloride in patients with Alzheimer's disease. Life Sci. 1995;57(12):1241-8. Abstract

Smith CP, Huger FP, Petko W, Kongsamut S. HP 749 enhances calcium-independent release of [3H]norepinephrine from rat cortical slices and synaptosomes. Neurochem Res. 1994 Oct;19(10):1265-70. Abstract

Hsu RS, DiLeo EM, Chesson SM, Klein JT, Effland RC. Determination of HP 749, a potential therapeutic agent for Alzheimer's disease, in plasma by high-performance liquid chromatography. J Chromatogr. 1991 Dec 6;572(1-2):352-9. Abstract