| 18053729 |
Maksay G, Nemes P, Vincze Z, Biro T: Synthesis of (nor) tropeine (di) esters and allosteric modulation of glycine receptor binding. J Neurochem. 1999 Nov;73(5):2158-66.
(Hetero) aromatic mono- and diesters of tropine and nortropine were prepared. Modulation of [3H] strychnine binding to glycine receptors of rat spinal cord was examined with a ternary allosteric model. The esters displaced [3H] strychnine binding with nano- or micromolar potencies and strong negative cooperativity. Coplanarity and distance of the ester moieties of diesters affected the binding affinity being nanomolar for isophthaloyl-bistropane and nortropeines. Nortropisetron had the highest affinity (K (A) approximately 10 nM). Two esters displayed negative cooperativity with glycine in displacement, while three esters of low-affinity and nortropisetron exerted positive cooperativity with glycine. |
82(1,1,1,2) |