Published in Cellular and Molecular Life Sciences
Retinoid X receptors (RXRs) form a unique subclass within the nuclear receptor (NR) superfamily of ligand-dependent transcription factors. RXRs are obligatory partners for a number of other NRs, placing RXRs in a coordinating role at the crossroads of multiple signaling pathways. In addition, RXRs can function as self-sufficient homodimers. Recent ...
Published in Molecular nutrition & food research
Methylxanthines (MTXs) are consumed by almost everybody in almost every area of the world. Caffeine, theophylline and theobromine are the most well-known members of this family of compounds; they are present, inter alia, in coffee, tea, cacao, yerba mate and cola drinks. MTXs are readily absorbed in the gastrointestinal tract and are able to penetr...
Published in Neurotoxicology
The biogenic amine histamine (HA) is not only the neurotransmitter of photoreceptors but also has important roles in mechanosensory reception, temperature preference, sleep and olfactory processing in insects. Two cDNAs (MdhclA and MdhclB) that encode HA-gated chloride channel subunits (MdHCLA and MdHCLB) were cloned from the housefly Musca domesti...
Published in EJNMMI Radiopharmacy and Chemistry
BackgroundThe somatostatin receptor subtype 2 (sstr2) is expressed on a majority of luminal breast cancers, however SPECT and scintigraphy imaging with agonistic sstr2 probes has been sub-optimal. High affinity antagonists can access more binding sites on the cell surface, resulting in higher tumor uptake and improved sensitivity. We compared the t...
Published in Medicinal Chemistry Research
A series of triaryl-substituted hydrazones as structural acyclic prototypes were synthesized and screened for anti-proliferative activity against breast (Michigan cancer foundation-7 and MD Anderson metastatic breast-231) and uterine cancer (Ishikawa) cell lines. Two compounds were found to be the most active, 5e showed the maximum inhibition of bo...
Published in Bioorganic & medicinal chemistry letters
A series of octahydropyrrolo[3,4-c]pyrroles were synthesized and evaluated by orexin 1 and 2 receptor (OX1 & 2 R) antagonists assays. Compound 14l with potent OXR antagonist activity and suitable pharmacokinetic behavior was chosen to be investigated in an EEG study, which demonstrated effects of sleep promotion comparable to Suvorexant. Furthermor...
Abstract Background The N-methyl-D-aspartate (NMDA) receptors are glutamate receptors that play vital roles in central nervous system development and are involved in synaptic plasticity, which is an essential process for learning and memory. The subunit N-methyl D-aspartate receptor subtype 2B (NR2B) is the chief excitatory neurotransmitter recepto...
Published in Archivos de la Sociedad Espanola de Oftalmologia
After treatment with spironolactone, both patients showed a visual acuity improvement and structural changes (reduced neurosensory retinal detachment and cystoid degeneration). Aldosterone receptor agonists (ARA) used for persistent forms of chronic central serous chorioretinopathy show encouraging results and could represent a therapeutic alternat...
Published in Psychopharmacology
Steven R. Goldberg was a pioneering behavioral pharmacologist whose intravenous drug self-administration studies advanced the understanding of conditioned stimuli and schedules of reinforcement as determinants of pattern and persistence of drug-seeking behavior, and in particular, the importance of nicotine in tobacco use. His passing in 2014 led t...
Published in Archivos de la Sociedad Espanola de Oftalmologia
After treatment with spironolactone, both patients showed a visual acuity improvement and structural changes (reduced neurosensory retinal detachment and cystoid degeneration). Aldosterone receptor agonists (ARA) used for persistent forms of chronic central serous chorioretinopathy show encouraging results and could represent a therapeutic alternat...
