Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT2B) Contractile Receptor in the Rat Stomach Fundus
摘要:
A series of potent, selective 5HT(2B) receptor antagonists has been identified based upon yohimbine, with SAR studies resulting in a 1000-fold increase in 5HT(2B) receptor affinity relative to the starting structure (-log K(B)s > 10.0 have been obtained). These high-affinity tetrahydro-beta-carboline antagonists are able to discriminate among the 5HT(2) family of serotonin receptors, with members of the series showing selectivities of more than 100-fold versus both the 5HT(2A) and 5HT(2C) receptors based upon radioligand binding and functional assays. As the first compounds reported with such selectivity and enhanced receptor affinity, these tetrahydro-beta-carboline antagonists are useful tools for elucidating the role of serotonin acting at the 5HT(2B) receptor in normal and disease physiology.
The present invention provides a new Pictet-Spengler process useful for preparing tetrahydro-beta-carboline compounds.
本发明提供了一种新的皮克特-斯宾格勒过程,用于制备四氢-β-咔啉化合物。
Intermediates to tetrahydro-beta-carbolines
申请人:Eli Lilly and Company
公开号:US05635528A1
公开(公告)日:1997-06-03
3-Ethanamine and 3-ethanamine related compounds are provided that are useful intermediates and have beneficial central nervous system activity.
3-乙胺和3-乙胺相关化合物被提供,它们是有用的中间体,并且具有有益的中枢神经系统活性。
Method for treating 5HT.sub.2B receptor related conditions
申请人:Eli Lilly and Company
公开号:US05688807A1
公开(公告)日:1997-11-18
The present invention provides methods for binding a 5-HT.sub.2B receptor in mammals using a both known and novel compounds. Further, the invention provides a method for treating or preventing 5-HT.sub.2B related conditions. Finally, the invention provides an article of manufacture.
The present invention provides tetrahydro-betacarboline compounds having useful central nervous system activity.
本发明提供了具有有用的中枢神经系统活性的四氢-β-咔啉化合物。
[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.