174339-89-0Relevant academic research and scientific papers
NOVEL RHO KINASE INHIBITORS AND METHODS OF USE
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Page/Page column 80, (2012/10/18)
The subject invention concerns materials and methods for treating diseases and disorders associated with expression of Rho associated kinases (ROCKs). Examples of diseases and disorders contemplated within the scope of the invention include, but are not limited to, oncological disorders, cardiovascular diseases, CNS disorders, and inflammatory disorders. In one embodiment, a method of the invention comprises administering a therapeutically effective amount of one or more compounds of the present invention, or a composition comprising the compounds, to a person or animal in need of treatment. The subject invention also concerns compounds that inhibit ROCKs, and compositions that comprise the inhibitor compounds of the invention. Compounds contemplated within the scope of the invention include, but are not limited to, those compounds shown in Table (5).
5-HT-1D receptor ligands
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, (2008/06/13)
Described herein are tryptamine analogs that display high binding affinity and selectivity for the 5-HT1Dβ receptor, of the formula: STR1 wherein R 1 is a group selected from aryl-C 1-7 alkyl; aryl-C 2-7 alkoxy; aryl-C 2-7 alkanoyl and aryl-C 1-7 alkanoyloxy, wherein said alkyl, alkoxy, alkanoyl and alkanoyloxy groups are optionally substituted by a C 1-4 alkyl substituent and wherein said aryl group is optionally substituted by one or more substituent selected from hydroxyl, halogen, mercapto, linear or branched C 1-4 alkyl, linear or branched C 1-4 alkoxy, linear or branched C 1-4 alkylthio, thiol substituted C 1-4 alkyl and nitro substituted C 1-4 alkyl;R 2 and R 3 are selected independently from H and C 1-4 alkyl; andR 4 is selected from H, C 1-4 alkyl, aryl and arylC 1-4 alkyl. The compounds are useful as reagents for receptor identification and in receptor-based drug screening programs, and can also be used therapeutically to treat conditions for which administration of a 5-HT1D ligand is indicated, for example in the treatment of migraine.
Binding of 5-Arylalkyloxytryptamines at Human 5-HT1Dβ Serotonin Receptors
Hong, Seoung-Soo,Dukat, Malgorzata,Teitler, Milt,Herrick-Davis, Kathy,McCallum, Kirk,et al.
, p. 690 - 699 (2007/10/03)
Several 5-substituted tryptamine derivatives were prepared and examined for their binding at 5-HT1D serotonin receptors. Initially, a region of bulk tolerance was probed. Subsequently, a series of 5-(arylalkyloxy)tryptamines was prepared. Within a homolog
