32560-59-1Relevant articles and documents
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.
Method of treating nausea and vomiting with certain substituted-phenylalkylamino (and aminoacid) derivatives and other serotonin depleting agents
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, (2008/06/13)
A method for the treatment of emesis in a mammal, which method comprises administering to said mammal an emesis inhibiting amount of a compound which depletes serotonin in the brain of mammals; among which are compounds having the formula: STR1 wherein, R is selected from hydrogen, loweralkyl, trifluoromethyl, carboxyl, or loweralkoxycarbonyl; R1 and R2 are hydrogen or loweralkyl; Z is trifluoromethyl or halogen; the optical isomers and pharmaceutically acceptable salts thereof; two of the preferred compounds of the invention are fenfluramine and norfenfluramine.
Optically active amines. XIX. Circular dichroism of ortho, meta, and para substituted β phenylalkylamine hydrochlorides. Further applications of the salicylidenimino chirality rule
Smith,Burrows,Chen
, p. 1562 - 1567 (2007/10/06)
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