16148-48-4Relevant academic research and scientific papers
1H-indole derivatives as a highly selective cyclooxygenase-2 inhibitor
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, (2008/06/13)
The present invention relates to a novel 1H-indole derivative having a structure of formula 1 and its pharmaceutically acceptable salts as a highly selective cyclooxygenase-2 inhibitor. Wherein, X, Y, and Q are defined in this specification respectively.
5-SUBSTITUTED-3-(1,2,3,6-TETRAHYDROPYRIDIN-4-YL)-AND 3-(PIPERIDIN-4-YL)-1H-INDOLES: NEW 5-HT1F AGONISTS
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, (2008/06/13)
This invention provides novel 5-HT 1F agonists of Formula I STR1 where A--B, R, R 1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.
Use of serotonin 5-HT1F agonists for the prevention of migraine
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, (2008/06/13)
This invention provides methods for the prevention of migraine which comprises administering to a mammal in need thereof a serotonin 5-HT1F agonist.
The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists.
Buchheit,Gamse,Giger,Hoyer,Klein,Kloeppner,Pfannkuche,Mattes
, p. 2331 - 2338 (2007/10/02)
A number of substituted indole carbazimidamides were prepared and evaluated as 5-HT4 receptor agonists by using the isolated field-stimulated guinea pig ileum preparation. Their selectivity for the 5-HT4 receptor was established by examining their affinity for other 5-HT receptors using radioligand-binding techniques. Several selective and highly potent full as well as partial agonists emerged from this study. For example, 1b,d were found to be the most potent, full 5-HT4 receptor agonist described so far (EC50 = 0.5 and 0.8 nM, respectively), being 6 and 4 times more potent than serotonin itself. On the other hand, 5b and 1h appeared as partial 5-HT4 receptor agonists in the nonstimulated guinea pig ileum preparation with potencies, evaluated against serotonin action, respectively similar (5b, Ki = 12 nM) to and 300-fold higher (1h, Ki = 0.04 nM) than serotonin.
