132664-85-8Relevant articles and documents
He pyrrole testsamine synonym, preparation method and its application
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Paragraph 0044; 0052-0054, (2017/03/08)
The invention relates to the field of medicinal chemistry and particularly relates to picotamide analogues (I), a preparation method and a pharmaceutical composition containing the picotamide analogues, wherein R represents hydrogen, 3, 5, 6- trimethyl, 5-methyl or 6-methyl. The picotamide analogues provided by the invention can be used for treating or preventing thromboembolic diseases.
INDOLE, INDAZOLE AND BENZIMIDAZOLE ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
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Page/Page column 20, (2010/12/31)
Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, Z, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
High-efficacy 5-HT1A agonists for antidepressant treatment: A renewed opportunity
Maurel, Jean Louis,Autin, Jean-Marie,Funes, Philippe,Newman-Tancredi, Adrian,Colpaert, Francis,Vacher, Bernard
, p. 5024 - 5033 (2008/03/13)
We report the discovery of novel 5-HT1A receptor agonists and describe the process that led to the antidepressant candidate 9 (F 15599). 9 has nanomolar affinity for 5-HT1A binding sites and is over 1000-fold selective with respect to the other 5-HT1 receptor subtypes, 5-HT2-7 receptor families, and also numerous GPCRs, transporters, ion channels, and enzymes. In a cellular model of signal transduction, 9 activates h5-HT1A receptors with an efficacy superior to that of the prototypical 5-HT1A agonist (±)-8-OH-DPAT and comparators undergoing clinical trials. After acute oral administration in rats, 9 totally reverses immobility in the forced swimming test and produces behaviors characteristic of 5-HT1A receptor activation. However, these effects occurred at widely separated doses, suggesting that 9 discriminates between distinct populations of 5-HT1A receptors. While the clinical relevance of these observations is still unknown, this opens new perspectives for the treatment of depressive disorders.