[EN] METHOD FOR TREATING 5HT2B RECEPTOR RELATED CONDITIONS<br/>[FR] METHODE DE TRAITEMENT D'ETATS ASSOCIES AU RECEPTEUR 5HT2B
申请人:ELI LILLY AND COMPANY
公开号:WO1995024200A1
公开(公告)日:1995-09-14
(EN) The present invention provides methods for binding a 5-HT2B receptor in mammals using both known and novel compounds. Further, the invention provides a method for treating or preventing 5-HT2B related conditions. Finally, the invention provides an article of manufacture.(FR) L'invention concerne des méthodes de fixation du récepteur 5-HT2B chez les mammifères au moyen de composés connus et nouveaux, ainsi qu'une méthode de traitement ou de prévention d'états associés à 5-HT2B. Un article manufacturé est également décrit.
(EN) 本发明提供了一种使用已知和新颖化合物来结合哺乳动物中的5-HT2B受体的方法。此外,本发明还提供了一种用于治疗或预防5-HT2B相关疾病的方法。最后,本发明提供了一种制品。
(FR) La présente invention concerne des méthodes de fixation du récepteur 5-HT2B chez les mammifères au moyen de composés connus et nouveaux, ainsi qu'une méthode de traitement ou de prévention d'états associés à 5-HT2B. Un article manufacturé est également décrit.
2,3-Dialkyl(dimethylamino)indoles: interaction with 5HT1, 5HT2, and rat stomach fundal serotonin receptors
作者:Pawel Fludzinski、Laura A. Wittenauer、Kathryn W. Schenck、Marlene L. Cohen
DOI:10.1021/jm00161a048
日期:1986.11
2,3-Dialkyl(dimethylamino)indoles, synthesized via the Fisher indole synthesis, were found to weakly bind to 5HT1 and 5HT2 sites in brain cortical membranes (IC50 greater than 1 microM at both sites for all compounds). These (dimethylamino)indoles were relatively potent antagonists of the serotonin receptor in the rat stomach fundus. At higher concentrations, several of the compounds were weak agonists at this receptor. For direct comparison with data obtained in the isolated rat fundus, antagonism of serotonin-induced contractions at 5HT2 receptors in the rat jugular vein was also examined. Several of the compounds showed good selectivity for the fundus receptor relative to the 5HT2 receptor; together with minimal affinity for 5HT1 and 5HT2 binding sites in brain cortical membranes, these results support the idea that the serotonin receptor in the stomach fundus is distinct from 5HT1 and 5HT2 binding sites.
METHOD FOR TREATING 5HT 2B RECEPTOR RELATED CONDITIONS