Astrocytes support glutamatergic neurotransmission in the central nervous system through multiple mechanisms which include: (i) glutamate clearance and control over glutamate spillover due to operation of glutamate transporters; (ii) supply of obligatory glutamate precursor glutamine via operation of glutamate-glutamine shuttle; (iii) supply of L-serine, the indispensable precursor of positive NMDA receptors neuromodulator D-serine and (iv) through overall homoeostatic control of the synaptic cleft. Astroglial cells express an extended complement of ionotropic and metabotropic glutamate receptors, which mediate glutamatergic input to astrocytes. In particular a sub-population of astrocytes in the cortex and in the spinal cord express specific type of NMDA receptors assembled from two GluN1, one GluN2C or D and one GluN3 subunits. This composition underlies low Mg2+ sensitivity thus making astroglial NMDA receptors operational at resting membrane potential. These NMDA receptors generate ionic signals in astrocytes and are linked to several astroglial homoeostatic molecular cascades.

• Klíčová slova
• Astrocyte, Glutamate, NMDA receptors, Neurotransmitters,
• MeSH
• astrocyty metabolismus   MeSH
• lidé MeSH
• membránové potenciály fyziologie   MeSH
• mozková kůra metabolismus   MeSH
• nervová síť metabolismus   MeSH
• receptory N-methyl-D-aspartátu metabolismus   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• receptory N-methyl-D-aspartátu MeSH

Allosteric modulators are ligands that bind to a site on the receptor that is spatially separated from the orthosteric binding site for the endogenous neurotransmitter. Allosteric modulators modulate the binding affinity, potency, and efficacy of orthosteric ligands. Muscarinic acetylcholine receptors are prototypical allosterically-modulated G-protein-coupled receptors. They are a potential therapeutic target for the treatment of psychiatric, neurologic, and internal diseases like schizophrenia, Alzheimer's disease, Huntington disease, type 2 diabetes, or chronic pulmonary obstruction. Here, we reviewed the progress made during the last decade in our understanding of their mechanisms of binding, allosteric modulation, and in vivo actions in order to understand the translational impact of studying this important class of pharmacological agents. We overviewed newly developed allosteric modulators of muscarinic receptors as well as new spin-off ideas like bitopic ligands combining allosteric and orthosteric moieties and photo-switchable ligands based on bitopic agents.

• Klíčová slova
• acetylcholine, allosteric modulation, muscarinic receptors,
• MeSH
• agonisté muskarinových receptorů metabolismus   MeSH
• alosterická regulace fyziologie   MeSH
• antagonisté muskarinových receptorů metabolismus   MeSH
• lidé MeSH
• ligandy MeSH
• receptory muskarinové metabolismus   fyziologie   MeSH
• receptory spřažené s G-proteiny MeSH
• vazebná místa MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• přehledy MeSH
• Názvy látek
• agonisté muskarinových receptorů MeSH
• antagonisté muskarinových receptorů MeSH
• ligandy MeSH
• receptory muskarinové MeSH
• receptory spřažené s G-proteiny MeSH

The aim of current study was to evaluate the effect of the most common anthocyanidins (cyanidin, delphinidin, malvidin, pelargonidin, and peonidin) on the transcriptional activity of steroid and nuclear receptors. The activities of steroid receptors - progesterone receptor (PR), estrogen receptor (ER), androgen receptor (AR), glucocorticoid receptor (GR), and nuclear receptors - vitamin D receptor (VDR), retinoid X receptor (RXR), retinoic acid receptor (RAR), pregnane X receptor (PXR), and thyroid receptor (TR) were assessed using either stable transfected luciferase gene reporter cell lines or transiently transfected cell lines. The cytotoxicity assays and gene reporter assays were performed after the 24-h treatment of cells with increasing range of concentrations (10 nM to 50 µM) of selected anthocyanidins. The results of experiments indicate that none of the examined anthocyanidins in all tested concentrations caused remarkable changes of transcriptional activity of studied steroid receptors, but their increasing concentrations slightly inhibited transcriptional activity of nuclear receptors induced by model agonists.

• Klíčová slova
• Anthocyanidins, nuclear receptors, steroid receptors, transcriptional activity,
• MeSH
• anthokyaniny farmakologie   MeSH
• genetická transkripce účinky léků   MeSH
• lidé MeSH
• nádorové buňky kultivované MeSH
• receptory cytoplazmatické a nukleární genetika   MeSH
• steroidní receptory genetika   MeSH
• viabilita buněk účinky léků   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• anthokyaniny MeSH
• receptory cytoplazmatické a nukleární MeSH
• steroidní receptory MeSH

The term 'receptor' is generally accepted as the cell-surface component that participates in virus binding and facilitates subsequent viral infection. Recent advances in technology have permitted the identification of several virus receptors, increasing our understanding of the significance of this initial virus-cell and virus-host interaction. Virus binding was previously considered to involve simple recognition and attachment to a single cell surface molecule by virus attachment proteins. The classical concept of these as single entities that participate in a lock-and-key-type process has been superseded by new data indicating that binding can be a multistep process, often involving different virus-attachment proteins and more than one host-cell receptor.

• MeSH
• virové nemoci veterinární   virologie   MeSH
• virové receptory metabolismus   MeSH
• viry metabolismus   patogenita   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• přehledy MeSH
• Názvy látek
• virové receptory MeSH

Disruption of cholinergic signalling via muscarinic receptors is associated with various pathologies, like Alzheimer's disease or schizophrenia. Selective muscarinic agonists possess therapeutic potential in the treatment of diabetes, pain or Sjögren's syndrome. The orthosteric binding site of all subtypes of the muscarinic receptor is structurally identical, making the development of affinity-based selective agonists virtually impossible. Some agonists, however, are functionally selective; they activate only a subset of receptors or signalling pathways. Others may stabilise specific conformations of the receptor leading to non-uniform modulation of individual signalling pathways (biased agonists). Functionally selective and biased agonists represent a promising approach for selective activation of individual subtypes of muscarinic receptors. In this work we review chemical structures, receptor binding and agonist-specific conformations of currently known functionally selective and biased muscarinic agonists in the context of their intricate intracellular signalling. Further, we take a perspective on the possible use of biased agonists for tissue and organ-specific activation of muscarinic receptors.

• Klíčová slova
• Functional selectivity, G-proteins, Muscarinic receptors, Signalling bias, β-arrestins,
• MeSH
• agonisté muskarinových receptorů farmakologie   MeSH
• lidé MeSH
• receptory muskarinové účinky léků   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• přehledy MeSH
• Názvy látek
• agonisté muskarinových receptorů MeSH
• receptory muskarinové MeSH

BACKGROUND: Pathogenesis of epilepsy involves dysregulation of the neurotransmitter system contributing to hyper-excitability of neuronal cells. MicroRNA (miRNAs) are small non-coding RNAs known to play a crucial role in post-transcriptional regulation of gene expression. METHODS: The present review was prepared following the Preferred Reporting Items for Systematic Reviews and Meta-Analysis (PRISMA) guidelines, employing a comprehensive search strategy to identify and extract data from published research articles. Keywords suchas epilepsy, micro RNA (micro RNAs, miRNA, miRNAs, miR), neurotransmitters (specific names), and neurotransmitter receptors (specific names) were used to construct the query. RESULTS: A total of 724 articles were identified using the keywords epilepsy, microRNA along with select neurotransmitter and neurotransmitter receptor names. After exclusions, the final selection consisted of 17 studies, most of which centered on glutamate and gamma-aminobutyric acid (GABA) receptors. Singular studies also investigated miRNAs affecting cholinergic, purinergic, and glycine receptors. CONCLUSION: This review offers a concise overview of the current knowledge on miRNA-mediated regulation of neurotransmitter receptors in epilepsy and highlights their potential for future clinical application.

• Klíčová slova
• Epilepsy, Micro RNA, Neurotransmitter receptors,
• MeSH
• epilepsie * genetika   metabolismus   MeSH
• lidé MeSH
• mikro RNA * genetika   metabolismus   MeSH
• receptory neurotransmiterů * genetika   metabolismus   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH
• systematický přehled MeSH
• Názvy látek
• mikro RNA * MeSH
• receptory neurotransmiterů * MeSH

Chemokines mediate their multiple effects by binding to a variety of specific receptors, that comprise a subfamily of rhodopsin-like, 7-transmembrane domain receptors, coupled to G proteins. Some of these receptors serve as coreceptors for HIV, some of them could be expressed as markers for T lymphocyte functional differentiation. This review aims at summarising data on chemokine receptors, their function in vivo, their target cells and it also mentions association of chemokine receptor polymorphisms with human disease.

• MeSH
• buněčná diferenciace fyziologie   MeSH
• lidé MeSH
• ligandy MeSH
• myši knockoutované genetika   MeSH
• myši MeSH
• polymorfismus genetický MeSH
• receptory chemokinů genetika   metabolismus   fyziologie   MeSH
• T-lymfocyty cytologie   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• přehledy MeSH
• Názvy látek
• ligandy MeSH
• receptory chemokinů MeSH

More than four decades passed since sigma receptors were first mentioned. Since then, existence of at least two receptor subtypes and their tissue distributions have been proposed. Nowadays, it is clear, that sigma receptors are unique ubiquitous proteins with pluripotent function, which can interact with so many different classes of proteins. As the endoplasmic resident proteins, they work as molecular chaperones - accompany various proteins during their folding, ensure trafficking of the maturated proteins between cellular organelles and regulate their functions. In the heart, sigma receptor type 1 is more dominant. Cardiac sigma 1 receptors regulate response to endoplasmic reticulum stress, modulates calcium signaling in cardiomyocyte and can affect function of voltage-gated ion channels. They contributed in pathophysiology of cardiac hypertrophy, heart failure and many other cardiovascular disorders. Therefore, sigma receptors are potential novel targets for specific treatment of cardiovascular diseases.

• MeSH
• kardiomyocyty účinky léků   metabolismus   patologie   MeSH
• kardiovaskulární látky aplikace a dávkování   metabolismus   MeSH
• kardiovaskulární nemoci farmakoterapie   metabolismus   patologie   MeSH
• lidé MeSH
• myokard metabolismus   patologie   MeSH
• receptor sigma-1 MeSH
• receptory sigma antagonisté a inhibitory   metabolismus   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• kardiovaskulární látky MeSH
• receptory sigma MeSH
• sigma-2 receptor MeSH Prohlížeč

The functions of anterior pituitary cells are controlled by two major groups of hypothalamic and intrapituitary ligands: one exclusively acts on G protein-coupled receptors and the other activates both G protein-coupled receptors and ligand-gated receptor channels. The second group of ligands operates as neurotransmitters in neuronal cells and their receptors are termed as neurotransmitter receptors. Most information about pituitary neurotransmitter receptors was obtained from secretory studies, RT-PCR analyses of mRNA expression and immunohistochemical and biochemical analyses, all of which were performed using a mixed population of pituitary cells. However, recent electrophysiological and imaging experiments have characterized γ-aminobutyric acid-, acetylcholine-, and ATP-activated receptors and channels in single pituitary cell types, expanding this picture and revealing surprising differences in their expression between subtypes of secretory cells and between native and immortalized pituitary cells. The main focus of this review is on the electrophysiological and pharmacological properties of these receptors and their roles in calcium signaling and calcium-controlled hormone secretion.

• Klíčová slova
• Action potentials, Calcium signaling, G protein-coupled receptors, Hormone secretion, Ligand-gated receptor channels, Neurotransmitters, Pituitary,
• MeSH
• buněčný rodokmen MeSH
• hormony adenohypofýzy metabolismus   MeSH
• lidé MeSH
• ligandy MeSH
• receptory neurotransmiterů metabolismus   MeSH
• signální transdukce * MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• přehledy MeSH
• Research Support, N.I.H., Intramural MeSH
• Názvy látek
• hormony adenohypofýzy MeSH
• ligandy MeSH
• receptory neurotransmiterů MeSH

The development of melatonin receptors in the rat pituitary and median eminence was studied using [125I]melatonin as a ligand. The specific binding was detected in pituitaries of 20-day-old fetuses already. The affinity of the receptor to the ligand (Kd) was in the range 63-133 pM and it did not change significantly during development. The pituitary concentration of [125I]melatonin binding sites was highest in 20-day-old fetuses (Bmax = 31 fmol/mg protein) and then it gradually decreased in the course of postnatal development, until it reached 10% of that value in 29-day-old males. In contrast, the concentration of melatonin receptors in median eminence did not change markedly in the course of development and it was about 15 fmol/mg protein. The marked decrease in the number of the pituitary receptors may be the cause of the reported developmental loss of the melatonin inhibitory effect on LHRH-induced LH release from anterior pituitary.

• MeSH
• adenohypofýza embryologie   růst a vývoj   metabolismus   MeSH
• buněčná membrána metabolismus   MeSH
• eminentia medialis embryologie   růst a vývoj   metabolismus   MeSH
• inbrední kmeny potkanů MeSH
• krysa rodu Rattus MeSH
• melatonin metabolismus   MeSH
• melatoninové receptory MeSH
• receptory neurotransmiterů metabolismus   MeSH
• stárnutí MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• melatonin MeSH
• melatoninové receptory MeSH
• receptory neurotransmiterů MeSH