93835-05-3Relevant articles and documents
Synthesis of aza and carbocyclic β-carbolines for the treatment of alcohol abuse. Regiospecific solution to the problem of 3,6-disubstituted β- And aza-β-carboline specificity
Phani Babu Tiruveedhula,Methuku, Kashi Reddy,Deschamps, Jeffrey R.,Cook, James M.
, p. 10705 - 10715 (2015/11/17)
A novel two step protocol was developed to gain regiospecific access to 3-substituted β- and aza-β-carbolines, 3-PBC (1), 3-ISOPBC (2), βCCt (3), 6-aza-3-PBC (4) and 6-aza-3-ISOPBC (5). These β-carbolines (1-3) are potential clinical agents to reduce alco
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse
Yin, Wenyuan,Majumder, Samarpan,Clayton, Terry,Petrou, Steven,Vanlinn, Michael L.,Namjoshi, Ojas A.,Ma, Chunrong,Cromer, Brett A.,Roth, Bryan L.,Platt, Donna M.,Cook, James M.
experimental part, p. 7548 - 7564 (2011/01/04)
A series of 3,6-disubstituted β-carbolines was synthesized and evaluated for their in vitro affinities at αxβ 3γ2 GABAA/benzodiazepine receptor subtypes by radioligand binding assays in search of α1 s
Bz1 Receptor Subtype Specific Ligands. Synthesis and Biological Properties of BCCt, a Bz1 Receptor Subtype Specific Antagonist
Cox, Eric D.,Hagen, Timothy J.,Mckernan, Ruth M.,Cook, James M.
, p. 710 - 718 (2007/10/03)
Receptor subtype selectivity studies at five major GABAA/BzR subtypes of some selected β-carbolines are reported. In addition, receptor subtype selectivity has been correlated to the in vivo biological profiles of these ligands. The antagonist βCCt 4 is the most Bz1 selective ligand reported to date. In comparison to the agonist zolpidem and the antagonist flumazenil, βCCt is 3.5 and 20 fold more selective, respectively, at Bz1 sites. βCCt has been shown to selectively antagonize the effects of diazepam on punished behavior as well as the anticonvulsant effects, while it failed to antagonize the rate-decreasing muscle-relaxant, ataxic, and sedative effects of this benzodiazepine. The unique biological activity of βCCt combined with its Bz1 subtype selectivity distinguishes it from the antagonist flumazenil (Ro15-1788), Consequently this ligand may be an important tool in identifying Bz1 receptor subtypes in vivo. In addition, an improved synthesis of this 3-substituted β-carboline is described.
