(−)1‐(Benzofuran‐2‐yl)‐2‐propylaminopentane, [(−)BPAP], a selective enhancer of the impulse propagation mediated release of catecholamines and serotonin in the brain

  title={(−)1‐(Benzofuran‐2‐yl)‐2‐propylaminopentane, [(−)BPAP], a selective enhancer of the impulse propagation mediated release of catecholamines and serotonin in the brain},
  author={Joseph Knoll and Fumio. Yoneda and Bertha Knoll and Hironori Ohde and Ildikó Miklya},
  journal={British Journal of Pharmacology},
The brain constituents β‐phenylethylamine (PEA) and tryptamine enhance the impulse propagation mediated transmitter release (exocytosis) from the catecholaminergic and serotoninergic neurons in the brain (‘catecholaminergic/serotoninergic activity enhancer, CAE/SAE, effect’). (−)Deprenyl (Selegiline) and (−)1‐phenyl‐2‐propylaminopentane [(−)PPAP] are amphetamine derived CAE substances devoid of the catecholamine releasing property. By changing the aromatic ring in PPAP we developed highly… 
The fate of (−)1-(benzofuran-2-yl)-2-propylaminopentane · HCl, (−)-BPAP, in rats, a potent enhancer of the impulse-evoked release of catecholamines and serotonin in the brain
Radioactivity was well absorbed and penetrated the brain, its elimination was fast and enterohepatic circulation was observed in rats, and more than 90% of the substance was recovered in the excreta during 72 hours.
The use of the synthetic enhancer substances (-)-deprenyl and (-)-BPAP in major depression.
  • P. Gaszner, I. Miklya
  • Biology, Chemistry
    Neuropsychopharmacologia Hungarica : a Magyar Pszichofarmakologiai Egyesulet lapja = official journal of the Hungarian Association of Psychopharmacology
  • 2004
The evaluation of the special pharmacological profile of the synthetic mesencephalic enhancer substance, especially the high potency and the unusual safety and tolerability of (-)-BPAP provide hope that this compound may in the future significantly improve the effectiveness of drug therapy in major depression and its combination with uptake inhibitors may substantially diminish the number of therapy resistant cases.


The pharmacology of 1-phenyl-2-propylamino-pentane (PPAP), a deprenyl-derived new spectrum psychostimulant.
1-phenyl-2-propylaminopentane facilitates learning and retention, is highly potent in antagonizing the tetrabenazine-induced depression in behavioral tests and is very effective in the forced swimming test.
(-)Deprenyl (selegiline), a catecholaminergic activity enhancer (CAE) substance acting in the brain.
  • J. Knoll
  • Biology, Psychology
    Pharmacology & toxicology
  • 1998
It may be supposed that a prophylactic low dose administration of a safe catecholaminergic activity enhancer substance during the postdevelopmental phase of life will slow the age-related decline of behavioral performances, delay natural death and decrease susceptibility to Parkinson's disease and Alzheimer's disease.
Multiple, small dose administration of (-)deprenyl enhances catecholaminergic activity and diminishes serotoninergic activity in the brain and these effects are unrelated to MAO-B inhibition.
  • J. Knoll, I. Miklya
  • Biology, Chemistry
    Archives internationales de pharmacodynamie et de therapie
  • 1994
The results prove that the described effects of deprenyl are unrelated to MAO-B inhibition and indicate the existence of hitherto unknown catecholaminergic and serotoninergic activity enhancer mechanisms in the brain, of which the former is stimulated and the latter inhibited by multiple, small dose administrations ofdeprenyl and related substances.
The effect of deprenyl (selegiline) on the natural history of Parkinson's disease.
Early deprenyl therapy delays the requirement for antiparkinsonian medication, possibly by slowing progression of the disease.
Rescue of dying neurons: A new action for deprenyl in MPTP parkinsonism
Research shows that deprenyl can increase SNc neuronal survival by a mechanism that is independent of the blockade of MPTP's conversion to MPP+ and may be responsible for slowing the progressioon of PD.
Is there a "non-MAO" macromolecular target for L-deprenyl?: Studies on MAOB mutant mice.
A controlled trial of selegiline, alpha-tocopherol, or both as treatment for Alzheimer's disease. The Alzheimer's Disease Cooperative Study.
In patients with moderately severe impairment from Alzheimer's disease, treatment with selegiline or alpha-tocopherol slows the progression of disease.