Mid-term outcomes following primary semi-constrained total knee arthroplasty in patients less than 60 years old, a retrospective review.

Introduction: Total knee arthroplasty (TKA) is a successful operation for osteoarthrosis. Typically, the knee can be balanced using posterior stabilized or cruciate retaining implants. However, in patients with severe deformity or ligamentous laxity, this cannot be obtained, and more constrained devices are needed.

Delayed-Onset Seizure in a Mild Quetiapine Overdose: Report of a Case and Review of the Literature.

Among atypical antipsychotics, quetiapine is commonly prescribed and considered to have a favorable side effect and safety profile. Here, we report the case of a patient who developed a generalized tonic-clonic seizure 28 hours following ingestion of 1,400 mg of quetiapine. Review of the literature identifies delayed-onset seizure as a potential complication of quetiapine overdose.

Synthesis and molecular docking of novel non-competitive antagonists of GluK2 receptor.

Here we present the synthesis, pharmacological activity, and molecular docking of novel non-competitive antagonists of GluK2 receptor. The compounds concerned are derivatives of indole and carbazole and are the second reported series of non-competitive antagonists of the GluK2 receptor (the first one was also published by our group). The activity of the indole derivatives is in the micromolar range, as in the case of the first series of non-competitive GluK2 receptor antagonists.

Structural studies, homology modeling and molecular docking of novel non-competitive antagonists of GluK1/GluK2 receptors.

Non-competitive ligands of kainate receptors have focused significant attention as medicinal compounds because they seem to be better tolerated than competitive antagonists and uncompetitive blocker of these receptors. Here we present structural studies (X-ray structure determination, NMR and MS spectra) of novel indole-derived non-competitive antagonists of GluK1/GluK2 receptors, homology models of GluK1 and GluK2 receptors based on novel AMPA receptor template as well as molecular docking of ligands to their molecular targets. We find that the allosteric site is in the receptor transduction domain, in one receptor subunit, not between the two subunits as it was indicated by our earlier studies.

5-(4-Hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-2,3,6,7-tetrahydro-1,4-thiazepines as compounds with high affinity at the benzodiazepine binding site on GABA(A) receptors.

A series of thiazepines has been studied as new ligands for the benzodiazepine binding site of the GABAA receptor. Compounds with high affinity and weak selectivity regarding alpha beta3gamma2, alpha2beta3gamma2, alpha3beta3gamma2, and alpha5beta3gamma2 subtypes were found. The pharmacophore is discussed based on experimental and theoretical results.