1205-53-4Relevant academic research and scientific papers
Hybrid dopamine uptake blocker-serotonin releaser ligands: A new twist on transporter-focused therapeutics
Blough, Bruce E.,Landavazo, Antonio,Partilla, John S.,Baumann, Michael H.,Decker, Ann M.,Page, Kevin M.,Rothman, Richard B.
supporting information, p. 623 - 627 (2014/07/07)
As part of our program to study neurotransmitter releasers, we report herein a class of hybrid dopamine reuptake inhibitors that display serotonin releasing activity. Hybrid compounds are interesting since they increase the design potential of transporter related compounds and hence represent a novel and unexplored strategy for therapeutic drug discovery. A series of N-alkylpropiophenones was synthesized and assessed for uptake inhibition and release activity using rat brain synaptosomes. Substitution on the aromatic ring yielded compounds that maintained hybrid activity, with the two disubstituted analogues (PAL-787 and PAL-820) having the most potent hybrid activity.
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, Fumio,Moto, Toshiaki,Sakae, Masatoshi,Ohde, Hironori,Knoll, Berta,Miklya, Ildiko,Knoll, Joseph
, p. 1197 - 1212 (2007/10/03)
The catecholaminergic and serotoninergic neurons in the brain change their performance according to the physiological need via a catecholaminergic/serotoninergic activity enhancer (CAE/SAE) mechanism. Phenylethylamine (PEA), tyramine and tryptamine are th
