N-Skatyltryptamines-Dual 5-HT6R/D2R Ligands with Antipsychotic and Procognitive Potential.

A series of N-skatyltryptamines was synthesized and their affinities for serotonin and dopamine receptors were determined. Compounds exhibited activity toward 5-HT1A, 5-HT2A, 5-HT6, and D2 receptors. Substitution patterns resulting in affinity/activity switches were identified and studied using homology modeling. Chosen hits were screened to determine their metabolism, permeability, hepatotoxicity, and CYP inhibition. Several D2 receptor antagonists with additional 5-HT6R antagonist and agonist properties were identified. The former combination resembled known antipsychotic agents, while the latter was particularly interesting due to the fact that it has not been studied before. Selective 5-HT6R antagonists have been shown previously to produce procognitive and promnesic effects in several rodent models. Administration of 5-HT6R agonists was more ambiguous-in naive animals, it did not alter memory or produce slight amnesic effects, while in rodent models of memory impairment, they ameliorated the condition just like antagonists. Using the identified hit compounds 15 and 18, we tried to sort out the difference between ligands exhibiting the D2R antagonist function combined with 5-HT6R agonism, and mixed D2/5-HT6R antagonists in murine models of psychosis.

[Qualification and methods of laser capsulotomy in pseudophakic eye]. / Kwalifikacja do wykonania kapsulotomii laserowej w rzekomosoczewkowosci i technika zabiegu.

Posterior capsule opacification (PCO) called secondary cataract is one of the most common late complication after the cataract surgery. This drawback might happened in 25 to 50 per cent in adult group and 51 to 100 per cent in children and adolescent group during 2 to 5 years after surgery. Currently Nd: YAG capsulotomy is the best method of secondary cataract treatment. Decision making about PCO should be based on thorough analysis of potential risk factors and advantages which follows that procedure. Advantages are: improvement of visual acuity, improvement of contrast sensivity, reducing glare and better appearance of eye fundus. However after capsulotomy some complications may happen: cystoid macular edema (CME), retinal detachment (RD), intraocular pressure increase (IOP), intraocular lens (IOL) dislocation. Nowadays it is growing awareness of prevention PCO. Counteracting arise PCO include treatment before, during and after surgery and it is strictly connected with reduction of inflammatory reaction, proper of surgical technique. In our publication we would like to stress some important issue about qualification process and techniques of Nd: YAG capsulotomy.