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  1. Article ; Online: Development of benzodioxine-heteroarylpiperazines as highly potent and selective α2c antagonists.

    Wang, Shouming / Haikarainen, Anssi / Pohjakallio, Antti / Sipilä, Julius / Kaskinoro, Janne / Juhila, Satu / Jalava, Niina / Koskinen, Mikko / Vesajoki, Marja / Kumpulainen, Esa / Pystynen, Jarmo / Koskelainen, Tuula / Holm, Patrik / Din Belle, David

    Bioorganic & medicinal chemistry letters

    2022  Volume 77, Page(s) 129005

    Abstract: Here is reported the design and synthesis of a series of highly potent and selective α2C antagonists using benzodioxine methyl piperazine as a central scaffold by pharmacophoric analysis to improve the pharmacokinetics of suboptimal clinical candidate ... ...

    Abstract Here is reported the design and synthesis of a series of highly potent and selective α2C antagonists using benzodioxine methyl piperazine as a central scaffold by pharmacophoric analysis to improve the pharmacokinetics of suboptimal clinical candidate molecules.
    MeSH term(s) Receptors, Adrenergic, alpha-2
    Chemical Substances Receptors, Adrenergic, alpha-2
    Language English
    Publishing date 2022-09-26
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2022.129005
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3203: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  2. Article ; Online: 2,3-Dihydrobenzo-dioxine piperidine derivatives as potent and selective α2c antagonists.

    Wang, Shouming / Haikarainen, Anssi / Pohjakallio, Antti / Sipilä, Julius / Kaskinoro, Janne / Juhila, Satu / Jalava, Niina / Koskinen, Mikko / Vesajoki, Marja / Kumpulainen, Esa / Pystynen, Jarmo / Koskelainen, Tuula / Holm, Patrik / Din Belle, David

    Bioorganic & medicinal chemistry letters

    2022  Volume 69, Page(s) 128783

    Abstract: In this manuscript, we report a series of benzodioxine methyl piperidine derivatives as highly potent and selective α2C antagonists by ligand design to improve the pharmacokinetics of a previous candidate molecule. ...

    Abstract In this manuscript, we report a series of benzodioxine methyl piperidine derivatives as highly potent and selective α2C antagonists by ligand design to improve the pharmacokinetics of a previous candidate molecule.
    MeSH term(s) Dioxins ; Piperidines/pharmacology ; Receptors, Adrenergic, alpha-2
    Chemical Substances Dioxins ; Piperidines ; Receptors, Adrenergic, alpha-2
    Language English
    Publishing date 2022-05-13
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2022.128783
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3203: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  3. Article ; Online: GABA

    de Miguel, Elena / Vekovischeva, Olga / Kuokkanen, Katja / Vesajoki, Marja / Paasikoski, Nelli / Kaskinoro, Janne / Myllymäki, Mikko / Lainiola, Mira / Janhunen, Sanna K / Hyytiä, Petri / Linden, Anni-Maija / Korpi, Esa R

    Addiction biology

    2018  Volume 24, Issue 6, Page(s) 1191–1203

    Abstract: Drugs of abuse induce widespread synaptic adaptations in the mesolimbic dopamine (DA) neurons. Such drug-induced neuroadaptations may constitute an initial cellular mechanism eventually leading to compulsive drug-seeking behavior. To evaluate the impact ... ...

    Abstract Drugs of abuse induce widespread synaptic adaptations in the mesolimbic dopamine (DA) neurons. Such drug-induced neuroadaptations may constitute an initial cellular mechanism eventually leading to compulsive drug-seeking behavior. To evaluate the impact of GABA
    MeSH term(s) Allosteric Regulation ; Animals ; Baclofen/pharmacology ; Behavior, Animal/drug effects ; Benzofurans/pharmacology ; CHO Cells ; Central Nervous System Depressants/pharmacology ; Cocaine/pharmacology ; Cricetulus ; Dopamine Uptake Inhibitors/pharmacology ; Dopaminergic Neurons/drug effects ; Ethanol/pharmacology ; GABA Modulators/pharmacology ; GABA-B Receptor Agonists/pharmacology ; Humans ; Mice ; Neuronal Plasticity/drug effects ; Quinazolinones/pharmacology ; Rats ; Receptors, GABA-B/drug effects ; Receptors, Glutamate/drug effects ; Receptors, Glutamate/metabolism ; Reward ; Self Administration ; Ventral Tegmental Area/cytology ; Ventral Tegmental Area/drug effects
    Chemical Substances (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one ; Benzofurans ; Central Nervous System Depressants ; Dopamine Uptake Inhibitors ; GABA Modulators ; GABA-B Receptor Agonists ; Quinazolinones ; Receptors, GABA-B ; Receptors, Glutamate ; Ethanol (3K9958V90M) ; Baclofen (H789N3FKE8) ; Cocaine (I5Y540LHVR)
    Language English
    Publishing date 2018-11-13
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1324314-7
    ISSN 1369-1600 ; 1355-6215
    ISSN (online) 1369-1600
    ISSN 1355-6215
    DOI 10.1111/adb.12688
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 4586: Show issues Location:
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