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

British journal of pharmacology, 1999-12, Vol.128 (8), p.1723-1732 [Peer Reviewed Journal]

1999 British Pharmacological Society ;2000 INIST-CNRS ;Copyright 1999, Nature Publishing Group 1999 Nature Publishing Group ;ISSN: 0007-1188 ;EISSN: 1476-5381 ;DOI: 10.1038/sj.bjp.0702995 ;PMID: 10588928 ;CODEN: BJPCBM

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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: Knoll, Joseph ; Yoneda, Fumio ; Knoll, Berta ; Ohde, Hironori ; Miklya, Ildikó
Subjects: (−)1‐(benzofuran‐2‐yl)‐2‐propylaminopentane [(−)BPAP], (−)1‐phenyl‐2‐propylaminopentane [(−)PPAP] ; (−)deprenyl (selegiline) ; 1-(Benzofuran-2-yl)-2-propylaminopentane ; Animals ; Benzofurans - chemical synthesis ; Benzofurans - metabolism ; Benzofurans - pharmacology ; Biological and medical sciences ; Brain - drug effects ; Brain - metabolism ; catecholaminergic activity enhancer (CAE) effect ; Cells, Cultured ; Dopamine - metabolism ; Electric Stimulation ; Medical sciences ; Mice ; Neuropharmacology ; Norepinephrine - metabolism ; Pharmacology. Drug treatments ; Phenethylamines - pharmacology ; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) ; Psychology. Psychoanalysis. Psychiatry ; Psychopharmacology ; Psychotropic Drugs - pharmacology ; Rabbits ; Rats ; Receptors, Catecholamine - metabolism ; Receptors, Serotonin - metabolism ; Serotonin - metabolism ; serotoninergic activity enhancer (SAE) effect ; Tryptamines - pharmacology
Is Part Of: British journal of pharmacology, 1999-12, Vol.128 (8), p.1723-1732
Description: 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 potent and selective CAE/SAE substances, structurally unrelated to the amphetamines. Out of 65 newly synthetized compounds, a tryptamine derived structure, (−)1‐(benzofuran‐2‐yl)‐2‐propylaminopentane [(−)BPAP] was selected as a potential follower of (−)deprenyl in the clinic and as a reference compound for further analysis of the CAE/SAE mechanism in the mammalian brain. (−)BPAP significantly enhanced in 0.18 μmol 1−1 concentration the impulse propagation mediated release of [3H]‐noradrenaline and [3H]‐dopamine and in 36 nmol 1−1 concentration the release of [3H]‐serotonin from the isolated brain stem of rats. The amount of catecholamines and serotonin released from isolated discrete rat brain regions (dopamine from the striatum, substantia nigra and tuberculum olfactorium, noradrenaline from the locus coeruleus and serotonin from the raphe) enhanced significantly in the presence of 10−12–10−14 M (−)BPAP. BPAP protected cultured hippocampal neurons from the neurotoxic effect of β‐amyloid in 10−14 M concentration. In rats (−)BPAP significantly enhanced the activity of the catecholaminergic and serotoninergic neurons in the brain 30 min after acute injection of 0.1 μg kg−1 s.c. In the shuttle box, (−)BPAP in rats was about 130 times more potent than (−)deprenyl in antagonizing tetrabenazine induced inhibition of performance. British Journal of Pharmacology (1999) 128, 1723–1732; doi:10.1038/sj.bjp.0702995
Publisher: Oxford, UK: Blackwell Publishing Ltd
Language: English
Identifier: ISSN: 0007-1188
EISSN: 1476-5381
DOI: 10.1038/sj.bjp.0702995
PMID: 10588928
CODEN: BJPCBM
Source: GFMER Free Medical Journals
MEDLINE
PubMed Central
Alma/SFX Local Collection
ProQuest Central

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

1999 British Pharmacological Society ;2000 INIST-CNRS ;Copyright 1999, Nature Publishing Group 1999 Nature Publishing Group ;ISSN: 0007-1188 ;EISSN: 1476-5381 ;DOI: 10.1038/sj.bjp.0702995 ;PMID: 10588928 ;CODEN: BJPCBM

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