Preferential Synaptic Type of GABA-A Receptor Ligands Enhancing Neuronal Survival and Facilitating Functional Recovery After Ischemic Stroke.

Selective enhancement of synaptic GABA signaling mediated by GABA-A receptors has been previously reported to promote functional recovery after ischemic stroke, while tonic GABA signaling has been detrimental. To identify agents that enhance synaptic signaling, we synthesized GABA-A ligands based on three chemotypes with affinity values p= 6.44-8.

Core-size and geometry toxicity in small amino terminated PAMAM dendrimers.

A series of 6 small PAMAM dendrimers (G0-dendrimers) differing in the size, polarity and flexibility has been synthesized. The toxicity has been investigated in three different human cancer cell lines (HeLa, MCF-7, THP-1) and the endothelial skin cell line HMEC-1 in order to evaluate their potential as vehicles for drug delivery.

Cape Gooseberry ( L.) Volatile Compounds Determination by Vacuum-Assisted Sorbent Extraction (VASE)-Selected Aspects.

Vacuum-Assisted Sorbent Extraction (VASE) is a novel extraction technique that uses vacuum to facilitate the transfer of volatile compounds from the matrix to the sorbent. This technique was explored for extraction of volatiles from cape gooseberry fruit, for both qualitative and quantitative analyses. Selected extraction parameters were tested: sample size, extraction temperature and time, influence of tissue disintegration on release of volatiles, and also addition of Ag ions in the form of AgNO to stop enzymatic formation of volatile compounds.

Dual 5-HT/SERT ligands for mitigating neuropsychiatric symptoms of dementia exerting neuroprotection against amyloid-β toxicity, memory preservation, and antidepressant-like properties.

In light of the biological targets alterations in dementia patients suffering from neuropsychiatric symptoms, particularly in the 5-HT receptor and SERT transporters, this study aimed to develop dual-acting molecules targeting both these targets. By combining a 5-substituted indole with piperazine scaffolds, we synthesized molecules with nanomolar affinities for these sites, avoiding interaction with off-targets detrimental to dementia patients. Preliminary pharmacodynamic and ADMET assays let the identification of compound 15 as a lead molecule.