114926-78-2Relevant articles and documents
Potent, selective tetrahydro-β-carboline antagonists of the serotonin 2B (5HT(2B)) contractile receptor in the rat stomach fundus
Audia, James E.,Evrard, Deborah A.,Murdoch, Gwyn R.,Droste, James J.,Nissen, Jeffrey S.,Schenck, Kathy W.,Fludzinski, Pawel,Lucaites, Virginia L.,Nelson, David L.,Cohen, Marlene L.
, p. 2773 - 2780 (2007/10/03)
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-β- carboline antagonists are able to discriminate among the 5HT2 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-β- carboline antagonists are useful tools for elucidating the role of serotonin acting at the 5HT(2B) receptor in normal and disease physiology.
Chiral and Achiral Formamidines in Synthesis. The First Asymmetric Route to (-)-Yohimbone and an Efficient Total Synthesis of (+/-)-Yohimbone
Meyers, A. I.,Miller, Donald B.,White, Franklin H.
, p. 4778 - 4787 (2007/10/02)
An asymmetric synthesis of (-)-yohimbone from chiral formamidines is presented.The synthetic pathway intercepts a previously reported route to yohimbenone (6) reported by Winterfeldt.An investigation of the -rearrangement involving iminium salts 8 an