The stable conformations of GABA(A)-benzodiazepine receptor bivalent ligands were determined by low temperature NMR spectroscopy and confirmed by single crystal X-ray analysis. The stable conformations in solution correlated well with those in the solid state. The linear conformation was important for these dimers to access the binding site and exhibit potent in vitro affinity and was illustrated for alpha5 subtype selective ligands. Bivalent ligands with an oxygen-containing linker folded back upon themselves both in solution and the solid state. Dimers which are folded do not bind to Bz receptors.
The stable conformations of GABA(A)-benzodiazepine receptor bivalent ligands were determined by low temperature n class="Chemical">NMR spectroscopy and confirmed by single crystal X-ray analysis. The stable conformations in solution correlated well with those in the solid state. The linear conformation was important for these dimers to access the binding site and exhibit potent in vitro affinity and was illustrated for alpha5 subtype selective ligands. Bivalent ligands with an oxygen-containing linker folded back upon themselves both in solution and the solid state. Dimers which are folded do not bind to Bz receptors.
Authors: Donna M Platt; James K Rowlett; Roger D Spealman; James Cook; Chunrong Ma Journal: Psychopharmacology (Berl) Date: 2002-09-04 Impact factor: 4.530
Authors: U Rudolph; F Crestani; D Benke; I Brünig; J A Benson; J M Fritschy; J R Martin; H Bluethmann; H Möhler Journal: Nature Date: 1999-10-21 Impact factor: 49.962
Authors: Terry Clayton; Michael M Poe; Sundari Rallapalli; Poonam Biawat; Miroslav M Savić; James K Rowlett; George Gallos; Charles W Emala; Catherine C Kaczorowski; Douglas C Stafford; Leggy A Arnold; James M Cook Journal: Int J Med Chem Date: 2015-11-10