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Titolo:
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
Autore:
Yoneda, F; Moto, T; Sakae, M; Ohde, H; Knoll, B; Miklya, I; Knoll, J;
Indirizzi:
Fujisawa Pharmaceut Co Ltd, Res Inst, Matsubara, Osaka 5808503, Japan Fujisawa Pharmaceut Co Ltd Matsubara Osaka Japan 5808503 a 5808503, Japan Semmelweis Univ Med, Dept Pharmacol, H-1445 Budapest, Hungary Semmelweis Univ Med Budapest Hungary H-1445 ol, H-1445 Budapest, Hungary
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 5, volume: 9, anno: 2001,
pagine: 1197 - 1212
SICI:
0968-0896(200105)9:5<1197:SSLT(>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
(-)DEPRENYL SELEGILINE MEDICATION; DEPRENYL PROLONGS LIFE; PARKINSONS-DISEASE; MALE-RATS; STRIATAL DOPAMINE; MAO-B; NEURONS; NEUROTOXICITY; INHIBITION; LONGEVITY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
37
Recensione:
Indirizzi per estratti:
Indirizzo: Yoneda, F Fujisawa Pharmaceut Co Ltd, Res Inst, Matsubara, Osaka 5808503, Japan Fujisawa Pharmaceut Co Ltd Matsubara Osaka Japan 5808503 Japan
Citazione:
F. Yoneda et al., "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", BIO MED CH, 9(5), 2001, pp. 1197-1212

Abstract

The catecholaminergic and serotoninergic neurons in the brain change theirperformance according to the physiological need via a catecholaminergic/serotoninergic activity enhancer (CAE/SAE) mechanism. Phenylethylamine (PEA),tyramine and tryptamine are the presently known endogenous CAE/SAE substances which enhance the impulse propagation mediated release of catecholamines and serotonin in the brain. A PEA derivative, (-)deprenyl (selegiline), known as a selective inhibitor of MAO-B, is for the time being the only CAE/SAE substance in clinical use. Aiming to develop a selective CAE/SAE substance much more potent than (-)deprenyl, a series of new 1-aryl-2-alkylaminoalkanes, structurally unrelated to PEA and the amphetamines, was designed and prepared. Among them, (-)1-(benzofuran-2-yl)-2-propylaminopentane ((-)BPAP) was selected as a promising candidate substance for further studies. (-)BPAP significantly enhanced in rats the impulse propagation mediated release of catecholamines and serotonin in the brain 30 min after acute injectionof 0.36 nmol/kg sc. In the shuttle box, (-)BPAP was in rats about 130 times more potent than (-)deprenyl in antagonizing tetrabenazine induced inhibition of performance. (-)BPAP protected cultured hippocampal neurons from the neurotoxic effect of P-amyloid in 10(-14)-10(-15) concentration. (C) 2001Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 15:35:35