Both substance P and neurokinin A are known as neurotransmitters of the submandibular ganglion cell. In this study, the effects of neurokinin (NK) receptor-subtype agonists on hamster submandibular ganglion cells were investigated using the whole-cell patch-clamp technique. Membrane currents evo...

In the mammalian brain the neurokinin NK2 receptors are predominantly located in the hippocampus, thalamus, septum and frontal cortex. It has been shown that administration of the NK2 receptor agonist, neurokinin A (NKA), into the medial septum of rats increases extracellular levels of acetylcho...

The bone marrow (BM) is home to at least two stem cells, hematopoietic (HSC) and mesenchymal. Hematopoiesis is partly regulated through neurokinin-1 (NK-1) and NK-2 belonging to the family of G-protein/7-transmembrane receptors. NK-1 and NK-2 show preference for the neurotransmitters, substance ...

A structure-activity study on neurokinin A and its C-terminal fragment NKA (4–10) has been performed in order to find selective agonists for the NK-2 receptor and identify chemical modifications suitable for protecting the peptides from degradation, while maintaining activity. Five series of co...

Several neurokinins, namely substance P, neurokinin A, neurokinin B, [β-Ala8]neurokinin A-(4–10) and senktide, were tested on noradrenaline-precontracted rabbit aortic rings to characterize the receptor mediating their endothelium-dependent relaxant effect in this preparation. CP-96,345, the n...

Mice lacking the NK1 receptor (NK1R−/− mice) and selective, high-affinity, non-peptide, NK1, NK2 and NK3 receptor antagonists were used to identify the tachykinin receptor subtype(s) mediating the central responses induced by neurokinin A (NKA). The peptides, substance P (SP), NKA and senktide a...

This paper describes a pharmacokinetic study performed in Sprague–Dawley rats after i.v. administration of a single 6-mg/kg dose of 2β-carbomethoxy-3β-(4-fluorophenyl)-N-(3-iodo-E-allyl)nortropane (Altropane). Plasma samples were collected from the retro-orbital sinus at times up to 3 h after...

Quantum chemical calculations of energy, structural parameters and vibrational wavenumbers of 4-bromoisoquinoline (4BIQ) were carried out by using B3LYP method using 6-311++G**, cc-pVTZ and LANL2DZ basis sets. The optimised geometrical parameters obtained by DFT calculations are in good agreemen...

The dopamine D4 receptor is a potential target for novel antipsychotic drugs. Most available compounds with affinity for the dopamine D4 receptor also bind to dopamine D2 receptors. This report describes the affinity of the 5-HT2A receptor antagonist RP 62203 (fananserin) for the human dopamine ...

It is now known that many neurotransmitter systems are responsible for diseases of the central nervous system (CNS). One of the most common CNS disease is depression. Considering that in the treatment and the genesis of depression, the most important are the serotonin receptors from 5-HT1A, 5-HT...

SummaryThe M2 channel of influenza A is a target of the adamantane family antiviral drugs. Two different drug-binding sites have been reported: one inside the pore, and the other is a lipid-facing pocket. A previous study showed that a chimera of M2 variants from influenza A and B that contains ...

2-(1-Adamantyl)-2-methyl-pyrrolidines 3 and 4, 2-(1-adamantyl)-2-methyl-azetidines 5 and 6, and 2-(1-adamantyl)-2-methyl-aziridines 7 and 8 were synthesized and tested for their antiviral activity against influenza A. Parent molecules 3, 5, and 7 contain the α-methyl-1-adamantan-methanamine 2 p...

The physicochemical and biopharmaceutical properties, such as pKa, crystal habit, water solubility, logD, molecular structure and dynamics, and membrane permeability of CR3124 (endo-2-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1H-benz[e]isoindol-1-one, a novel potent 5-HT3 receptor antag...

Hox gene expression imparts segment identity to body structures along the anterior–posterior axis and is tightly governed by higher order chromatin mechanisms. Chromatin regulatory features of the homeotic complex are best defined in Drosophila melanogaster, where multiple cis-regulatory elemen...

The development of dental adhesive resins with long-lasting antibacterial properties is a possible solution to overcome the problem of secondary caries in modern adhesive dentistry.

In this work, a novel hyperbranched poly (urethane-phosphine oxide) (HPUPO) was facilely synthesized from 4,4′-diphenylmethane diisocyanate and trihydroxymethylphosphine oxide at room temperature. When HPUPO was incorporated, flame retardancy and toughness of epoxy resin are improved with maint...

The surfaces of indium tin oxide coated glass substrates were functionalized with a surface grafted, covalently bound photoinitiator. These surface functionalized substrates were used to assemble liquid crystal (LC) test cells. The LC test cells obtained were filled with reactive mixtures of a n...

Excitatory amino acid (EAA) transporters are of physiological importance in the regulation of the extracellular concentration of excitatory amino acids and the neuroexcitation in CNS. Among four identified transporters, the Na+-dependent high-affinity l-glutamate/l-aspartate transporter (GLAST) ...

Myricetin is a natural dietary flavonoid compound with multiple activities, such as anti-oxidant, anti-inflammatory, anti-carcinogenic and anti-proliferative effects. However, myricetin exhibited substantial limitations, such as poor water-solubility, and low stability in body when it was admini...

Amino acids are considered as a new class of solvents, which can be used in CO2 capture processes. Designing such processes requires simple and precise models for predicting thermodynamic parameters. In this study, Adaptive Neuro-Fuzzy Inference System (ANFIS) was employed to develop a precise t...