The use of the synthetic enhancer substances (-)-deprenyl and (-)-BPAP in major depression
- PMID:15825677
The use of the synthetic enhancer substances (-)-deprenyl and (-)-BPAP in major depression
Abstract
There is still a great need for the development of antidepressants with a new pharmacological spectrum. The finding that phenylethylamine and tryptamine are endogenous enhancers of the impulse propagation mediated release of catecholamines and serotonin in the brain, and the development of synthetic mesencephalic enhancer substances opened the possibility to stimulate catecholaminergic and serotonergic neurons in the mesencephalon via a previously unknown mechanism. (-)-Deprenyl, a prototype of the phenylethylamine-derived synthetic enhancer substances, stimulates the catecholaminergic neurons in the brain but is almost ineffective on the serotonergic neurons. R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane, (-)-BPAP, the recently developed tryptamine-derived selective synthetic mesencephalic enhancer substance, a hundred times more potent compound than (-)-deprenyl, acts also on the serotonergic neurons. 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.
Similar articles
- Major depression and the synthetic enhancer substances, (-)-deprenyl and R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane.Gaszner P, Miklya I.Gaszner P, et al.Prog Neuropsychopharmacol Biol Psychiatry. 2006 Jan;30(1):5-14. doi: 10.1016/j.pnpbp.2005.06.004. Epub 2005 Jul 14.Prog Neuropsychopharmacol Biol Psychiatry. 2006.PMID:16023777Review.
- Pharmacological studies with endogenous enhancer substances: beta-phenylethylamine, tryptamine, and their synthetic derivatives.Shimazu S, Miklya I.Shimazu S, et al.Prog Neuropsychopharmacol Biol Psychiatry. 2004 May;28(3):421-7. doi: 10.1016/j.pnpbp.2003.11.016.Prog Neuropsychopharmacol Biol Psychiatry. 2004.PMID:15093948Review.
- [A comparison of the pharmacology of (-)-deprenyl to N-methylpropargylamine-1-aminoindane (J-508) and rasagiline, the desmethyl-analogue of J-508].Miklya I.Miklya I.Neuropsychopharmacol Hung. 2008 Mar;10(1):15-22.Neuropsychopharmacol Hung. 2008.PMID:18771016Hungarian.
- (-)1-(Benzofuran-2-yl)-2-propylaminopentane, [(-)BPAP], a selective enhancer of the impulse propagation mediated release of catecholamines and serotonin in the brain.Knoll J, Yoneda F, Knoll B, Ohde H, Miklya I.Knoll J, et al.Br J Pharmacol. 1999 Dec;128(8):1723-32. doi: 10.1038/sj.bjp.0702995.Br J Pharmacol. 1999.PMID:10588928Free PMC article.
- Structure-activity studies leading to (-)1-(benzofuran-2-yl)-2-propylaminopentane, ((-)BPAP), a highly potent, selective enhancer of the impulse propagation mediated release of catecholamines and serotonin in the brain.Yoneda F, Moto T, Sakae M, Ohde H, Knoll B, Miklya I, Knoll J.Yoneda F, et al.Bioorg Med Chem. 2001 May;9(5):1197-212. doi: 10.1016/s0968-0896(01)00002-5.Bioorg Med Chem. 2001.PMID:11377178
Cited by
- Enhancer Regulation of Dopaminergic Neurochemical Transmission in the Striatum.Harsing LG, Knoll J, Miklya I.Harsing LG, et al.Int J Mol Sci. 2022 Aug 1;23(15):8543. doi: 10.3390/ijms23158543.Int J Mol Sci. 2022.PMID:35955676Free PMC article.