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

@article{Knoll19991Benzofuran2yl2propylaminopentaneA,
  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},
  year={1999},
  volume={128}
}
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… 
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50 Citations
Highly Influential Citations
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50 Citations

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
TLDR
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.
Neuroprotective function of R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane, [R-(-)-BPAP], against apoptosis induced by N-methyl(R)salsolinol, an endogenous dopaminergic neurotoxin, in human dopaminergic neuroblastoma SH-SY5Y cells.
Effects of (R)-(−)-1-(benzofuran-2-yl)-2-propylaminopentane hydrochloride [(−)-BPAP] in animal models of mood disorders
Transporter-mediated actions of R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane.
1-(Benzofuran-2-yl)-2-(3,3,3-trifluoropropyl)aminopentane HCl, 3-F-BPAP, antagonizes the enhancer effect of (-)-BPAP in the shuttle box and leaves the effect of (-)-deprenyl unchanged.
Enhancer substances: selegiline and R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane [(-)-BPAP] enhance the neurotrophic factor synthesis on cultured mouse astrocytes.
Major depression and the synthetic enhancer substances, (−)-deprenyl and R-(−)-1-(benzofuran-2-yl)-2-propylaminopentane
  • P. Gaszner, I. Miklya
  • Biology, Chemistry
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 2006
Longevity study with low doses of selegiline/(-)-deprenyl and (2R)-1-(1-benzofuran-2-yl)-N-propylpentane-2-amine (BPAP).
The L-DOPA-sparing effect of R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane hydrochloride [(-)-BPAP] in reserpine-pretreated rats.
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
TLDR
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.
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References

SHOWING 1-10 OF 41 REFERENCES
(-)Deprenyl and (-)1-phenyl-2-propylaminopentane, [(-)PPAP], act primarily as potent stimulants of action potential-transmitter release coupling in the catecholaminergic neurons.
The pharmacology of 1-phenyl-2-propylamino-pentane (PPAP), a deprenyl-derived new spectrum psychostimulant.
TLDR
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
TLDR
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
TLDR
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.
Phenylethylamine and tyramine are mixed-acting sympathomimetic amines in the brain.
The effect of deprenyl (selegiline) on the natural history of Parkinson's disease.
TLDR
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
TLDR
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.
Enhanced catecholaminergic and serotoninergic activity in rat brain from weaning to sexual maturity: rationale for prophylactic (-)deprenyl (selegiline) medication.
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.
TLDR
In patients with moderately severe impairment from Alzheimer's disease, treatment with selegiline or alpha-tocopherol slows the progression of disease.
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