Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT<sub>2B</sub>) Contractile Receptor in the Rat Stomach Fundus
作者:James E. Audia、Deborah A. Evrard、Gwyn R. Murdoch、James J. Droste、Jeffrey S. Nissen、Kathy W. Schenck、Pawel Fludzinski、Virginia L. Lucaites、David L. Nelson、Marlene L. Cohen
DOI:10.1021/jm960062t
日期:1996.1.1
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.
Onda; Kawanishi, Yakugaku Zasshi/Journal of the Pharmaceutical Society of Japan, 1956, vol. 76, p. 966
作者:Onda、Kawanishi
DOI:——
日期:——
Hahn et al., Justus Liebigs Annalen der Chemie, 1935, vol. 520, p. 107,115
作者:Hahn et al.
DOI:——
日期:——
Synthesis of 8-Oxoberbines and Related Benzolactams by Pd(OAc)<sub>2</sub>-Catalyzed Direct Aromatic Carbonylation
prepared from 1-benzyl-1,2,3,4-tetrahydroisoquinolines or 1-benzyl-1,2,3,4-tetrahydro-β-carbolines by a phosphine-free Pd(II)-catalyzed directaromaticcarbonylation in a Pd(OAc)2-Cu(OAc)2 catalytic system. The site selectivity was compared with that of the carbonylation with Pd(OAc)2 or Pd(OAc)2·2 PPh3, respectively.