167 research outputs found

    Adenosine receptors in GtoPdb v.2021.2

    Get PDF
    Adenosine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Adenosine Receptors [110]) are activated by the endogenous ligand adenosine (potentially inosine also at A3 receptors). Crystal structures for the antagonist-bound [153, 313, 221, 61], agonist-bound [375, 203, 204] and G protein-bound A2A adenosine receptors [49] have been described. The structures of an antagonist-bound A1 receptor [128] and an adenosine-bound A1 receptor-Gi complex [86] have been resolved by cryo-electronmicroscopy. Another structure of an antagonist-bound A1 receptor obtained with X-ray crystallography has also been reported [57]. caffeine is a nonselective antagonist for adenosine receptors, while istradefylline, a selective A2A receptor antagonist, is on the market for the treatment of Parkinson's disease

    Adenosine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

    Get PDF
    Adenosine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Adenosine Receptors [103]) are activated by the endogenous ligand adenosine (potentially inosine also at A3 receptors). Crystal structures for the antagonist-bound [146, 305, 213, 55], agonist-bound [362, 196, 198] and G protein-bound A2A adenosine receptors [43] have been described. The structures of an antagonist-bound A1 receptor [123] and an adenosine-bound A1 receptor-Gi complex [80] have been resolved by cryo-electronmicroscopy. Another structure of an antagonist-bound A1 receptor obtained with X-ray crystallography has also been reported [51]

    Adenosine receptors in GtoPdb v.2023.1

    Get PDF
    Adenosine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Adenosine Receptors [112]) are activated by the endogenous ligand adenosine (potentially inosine also at A3 receptors). Crystal structures for the antagonist-bound [155, 316, 224, 62], agonist-bound [379, 205, 206] and G protein-bound A2A adenosine receptors [49] have been described. The structures of an antagonist-bound A1 receptor [130] and an adenosine-bound A1 receptor-Gi complex [87] have been resolved by cryo-electronmicroscopy. Another structure of an antagonist-bound A1 receptor obtained with X-ray crystallography has also been reported [58]. The structure of the A2B receptor has also been elucidated [57]. caffeine is a nonselective antagonist for adenosine receptors, while istradefylline, a selective A2A receptor antagonist, is on the market for the treatment of Parkinson's disease

    The Kinase Function of MSK1 Regulates BDNF Signaling to CREB and Basal Synaptic Transmission, But Is Not Required for Hippocampal Long-Term Potentiation or Spatial Memory

    Get PDF
    The later stages of long-term potentiation (LTP) in vitro and spatial memory in vivo are believed to depend upon gene transcription. Accordingly, considerable attempts have been made to identify both the mechanisms by which transcription is regulated and indeed the gene products themselves. Previous studies have shown that deletion of one regulator of transcription, the mitogen- and stress-activated kinase 1 (MSK1), causes an impairment of spatial memory. Given the ability of MSK1 to regulate gene expression via the phosphorylation of cAMP response element binding protein (CREB) at serine 133 (S133), MSK1 is a plausible candidate as a prime regulator of transcription underpinning synaptic plasticity and learning and memory. Indeed, prior work has revealed the necessity for MSK1 in homeostatic and experience-dependent synaptic plasticity. However, using a knock-in kinase-dead mouse mutant of MSK1, the current study demonstrates that, while the kinase function of MSK1 is important in regulating the phosphorylation of CREB at S133 and basal synaptic transmission in hippocampal area CA1, it is not required for metabotropic glutamate receptor-dependent long-term depression (mGluR-LTD), two forms of LTP or several forms of spatial learning in the watermaze. These data indicate that other functions of MSK1, such as a structural role for the whole enzyme, may explain previous observations of a role for MSK1 in learning and memory

    miR-132/212 knockout mice reveal roles for these miRNAs in regulating cortical synaptic transmission and plasticity

    Get PDF
    miR-132 and miR-212 are two closely related miRNAs encoded in the same intron of a small non-coding gene, which have been suggested to play roles in both immune and neuronal function. We describe here the generation and initial characterisation of a miR-132/212 double knockout mouse. These mice were viable and fertile with no overt adverse phenotype. Analysis of innate immune responses, including TLR-induced cytokine production and IFNÎČ induction in response to viral infection of primary fibroblasts did not reveal any phenotype in the knockouts. In contrast, the loss of miR-132 and miR-212, while not overtly affecting neuronal morphology, did affect synaptic function. In both hippocampal and neocortical slices miR-132/212 knockout reduced basal synaptic transmission, without affecting paired-pulse facilitation. Hippocampal long-term potentiation (LTP) induced by tetanic stimulation was not affected by miR-132/212 deletion, whilst theta burst LTP was enhanced. In contrast, neocortical theta burst-induced LTP was inhibited by loss of miR-132/212. Together these results indicate that miR-132 and/or miR-212 play a significant role in synaptic function, possibly by regulating the number of postsynaptic AMPA receptors under basal conditions and during activity-dependent synaptic plasticity

    The marine epilithic diatom Melosira brandinii sp. nov. (Bacillariophyta) from Elephant Island, Antarctic Peninsula, with comments on some related species

    Get PDF
    Uma nova espécie de diatomåcea eplítica é descrita sob microscopia eletrÎnica, a partir de amostras coletadas próximo à Ilha Elefante, Península Antårtica. As células de Melosira brandinii sp. nov. encontram-se reunidas em cadeias filamentosas através de longos tubos mucilaginosos. As valvas são circulares, com superfície valvar provida de lóculos pentagonais arranjados irregularmente. Cada lóculo possui 6-12 poros na superfície externa, abrindo-se para o interior através de aréolas do tipo rota. A corona é composta exclusivamente por grùnulos grosseiros, os quais estão mais concentrados na borda do manto. ComparaçÔes com as espécies próximas Melosira arctica, M. moniliformis e M. nummuloides foram realizadas. Adicionalmente, são fornecidas fotomicrografias de M. arctica provenientes do material tipo e do Mar de Barents (Ártico), e de M. moniliformis de estuårios do Sul do Brasil.A new species of epilithic diatom is described from samples collected near Elephant Island, Antarctic Peninsula. The cells of Melosira brandinii sp. nov. are joined in filamentous chains and attached by means of long mucilaginous stalks. The valves are circular with the valvar surface composed of irregularly arranged pentagonal Ioculi. Each loculus bears 6-12 pores on the external surface, opening to the innerside through rotae. The corona is only composed of coarse granules. A mantle is well developed, presenting rimoportulae and bearing coarse granules, which are more concentrated at the mantle edge. Comparisons with the related species Melosira arctica, M. moniliformis and M. nummuloides are made. Additionally, photomicrographs of M. arctica from the type material and Barents Sea, and of M. moniliformis from estuaries of Southern Brazil are included

    Recommended Terminology for Aerobiological Studies

    Get PDF
    Aerobiology is an interdisciplinary science where researchers with different backgrounds are involved in different topics related to microorganism, airborne biological particles, e.g. pollen and spores, and phenology. Some concepts, words or expressions used in aerobiology have a clear definition, but are however frequently misused. Therefore, the working group “Quality Control” of the European Aerobiology Society (EAS) and the International Association of Aerobiology (IAA) would like to clarify some of them, their use and presentation

    Synedrella nodiflora extract depresses excitatory synaptic transmission and chemically-induced in vitro seizures in the rat hippocampus

    Get PDF
    Extracts of the tropical Cinderella plant Synedrella nodiflora are used traditionally to manage convulsive conditions in the West African sub-region. This study sought to determine the neuronal basis of the effectiveness of these plant extracts to suppress seizure activity. Using the hippocampal slice preparation from rats, the ability of the extract to depress excitatory synaptic transmission and in vitro seizure activity were investigated. Bath perfusion of the hydro-ethanolic extract of Synedrella nodiflora (SNE) caused a concentration-dependent depression of evoked field excitatory postsynaptic potentials (fEPSPs) recorded extracellularly in the CA1 region of the hippocampus with maximal depression of about 80% and an estimated IC50 of 0.06 mg/ml. The SNE-induced fEPSP depression was accompanied by an increase in paired pulse facilitation. The fEPSP depression only recovered partially after 20 min washing out. The effect of SNE was not stimulus dependent as it was present even in the absence of synaptic stimulation. Furthermore, it did not show desensitization as repeat application after 10 min washout produced the same level of fEPSP depression as the first application. The SNE effect on fEPSPs was not via adenosine release as it was neither blocked nor reversed by 8-CPT, an adenosine A1 receptor antagonist. In addition, SNE depressed in vitro seizures induced by zero Mg2+ and high K+ -containing artificial cerebrospinal fluid (aCSF) in a concentration-dependent manner. The results show that SNE depresses fEPSPs and spontaneous bursting activity in hippocampal neurons that may underlie its ability to abort convulsive activity in persons with epilepsy
    • 

    corecore