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  1. Article ; Online: Pharmacokinetics of single and repeated oral doses of pregabalin oral solution formulation in cats.

    Lamminen, Terttu / Doedée, Anne / Hyttilä-Hopponen, Minja / Kaskinoro, Janne

    Journal of veterinary pharmacology and therapeutics

    2022  Volume 45, Issue 4, Page(s) 385–391

    Abstract: The study was designed to determine the pharmacokinetic profile and bioavailability of a novel pregabalin 50 mg/ml oral solution formulation ( ... ...

    Abstract The study was designed to determine the pharmacokinetic profile and bioavailability of a novel pregabalin 50 mg/ml oral solution formulation (Bonqat
    MeSH term(s) Administration, Intravenous/veterinary ; Administration, Oral ; Animals ; Area Under Curve ; Biological Availability ; Cats ; Half-Life ; Pregabalin
    Chemical Substances Pregabalin (55JG375S6M)
    Language English
    Publishing date 2022-04-25
    Publishing country England
    Document type Journal Article
    ZDB-ID 435216-6
    ISSN 1365-2885 ; 0140-7783
    ISSN (online) 1365-2885
    ISSN 0140-7783
    DOI 10.1111/jvp.13061
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Pharmacokinetics of single and repeated oral doses of pregabalin oral solution formulation in cats

    Lamminen, Terttu / Doedée, Anne / Hyttilä‐Hopponen, Minja / Kaskinoro, Janne

    Journal of veterinary pharmacology and therapeutics. 2022 July, v. 45, no. 4

    2022  

    Abstract: The study was designed to determine the pharmacokinetic profile and bioavailability of a novel pregabalin 50 mg/ml oral solution formulation (Bonqat®, Orion Corporation Orion Pharma) in 6 healthy laboratory cats. The cats received pregabalin as single ... ...

    Abstract The study was designed to determine the pharmacokinetic profile and bioavailability of a novel pregabalin 50 mg/ml oral solution formulation (Bonqat®, Orion Corporation Orion Pharma) in 6 healthy laboratory cats. The cats received pregabalin as single oral doses of 2.5, 5, and 7.5 mg/kg, dose 5 mg/kg on two consecutive days, and a single intravenous dose of 2.5 mg/kg. The washout period between each administration was four weeks. The cats were monitored for clinical signs and level of sedation, and blood samples were taken before pregabalin dosing and at pre‐defined time points up to 168 h after dosing. Plasma concentrations of pregabalin were determined using a validated liquid chromatography–tandem mass spectrometry method. The mean maximum plasma concentration of 10.1 μg/ml was reached between 0.5 and 1 h after oral administration of the clinical dose 5 mg/kg. The mean half‐life after oral administration of dose 5 mg/kg was 14.7 h and the mean systemic bioavailability was 94%. Pregabalin showed linear pharmacokinetics from 2.5 to 7.5 mg/kg. Exposures after a single dose and re‐dosing of 5 mg/kg at 24 h were comparable. Pregabalin was well tolerated with mild sedation and mildly uncoordinated movements observed in few cats at dose 7.5 mg/kg. As a conclusion, study results show rapid absorption, linear pharmacokinetics, and high oral bioavailability of pregabalin without safety concerns after administration of oral solution in cats.
    Keywords absorption ; bioavailability ; half life ; intravenous injection ; liquid chromatography ; oral administration ; pharmacokinetics ; sedation ; tandem mass spectrometry
    Language English
    Dates of publication 2022-07
    Size p. 385-391.
    Publishing place John Wiley & Sons, Ltd
    Document type Article
    Note JOURNAL ARTICLE
    ZDB-ID 435216-6
    ISSN 1365-2885 ; 0140-7783
    ISSN (online) 1365-2885
    ISSN 0140-7783
    DOI 10.1111/jvp.13061
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  3. Article ; Online: Inhibition of Canonical Transient Receptor Potential Channels 4/5 with Highly Selective and Potent Small-Molecule HC-070 Alleviates Mechanical Hypersensitivity in Rat Models of Visceral and Neuropathic Pain.

    Jalava, Niina / Kaskinoro, Janne / Chapman, Hugh / Morales, Miguel / Metsänkylä, Hanna / Heinonen, Satu-Maarit / Koivisto, Ari-Pekka

    International journal of molecular sciences

    2023  Volume 24, Issue 4

    Abstract: Transient receptor potential channels C4/C5 are widely expressed in the pain pathway. Here, we studied the putative analgesic efficacy of the highly selective and potent TRPC4/C5 antagonist HC-070 in rats. Inhibitory potency on human TRPC4 was assessed ... ...

    Abstract Transient receptor potential channels C4/C5 are widely expressed in the pain pathway. Here, we studied the putative analgesic efficacy of the highly selective and potent TRPC4/C5 antagonist HC-070 in rats. Inhibitory potency on human TRPC4 was assessed by using the whole-cell manual patch-clamp technique. Visceral pain sensitivity was assessed by the colonic distension test after intra-colonic trinitrobenzene sulfonic acid injection and partial restraint stress. Mechanical pain sensitivity was assessed by the paw pressure test in the chronic constriction injury (CCI) neuropathic pain model. We confirm that HC-070 is a low nanomolar antagonist. Following single oral doses (3-30 mg/kg in male or female rats), colonic hypersensitivity was significantly and dose-dependently attenuated, even fully reversed to baseline. HC-070 also had a significant anti-hypersensitivity effect in the established phase of the CCI model. HC-070 did not have an effect on the mechanical withdrawal threshold of the non-injured paw, whereas the reference compound morphine significantly increased it. Analgesic effects are observed at unbound brain concentrations near the 50% inhibitory concentration (IC
    MeSH term(s) Rats ; Male ; Female ; Humans ; Animals ; Neuralgia/metabolism ; Pain Threshold ; Analgesics/pharmacology ; Transient Receptor Potential Channels ; Disease Models, Animal ; Hyperalgesia/drug therapy
    Chemical Substances HC-070 ; Analgesics ; Transient Receptor Potential Channels
    Language English
    Publishing date 2023-02-08
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2019364-6
    ISSN 1422-0067 ; 1422-0067 ; 1661-6596
    ISSN (online) 1422-0067
    ISSN 1422-0067 ; 1661-6596
    DOI 10.3390/ijms24043350
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Ocular Administration of Palonosetron in the Prevention of Cisplatin-Induced Nausea and Vomiting.

    Levijoki, Jouko / Saloranta, Lasse / Tuunainen, Johanna / Kaskinoro, Janne / Pappinen, Sari / Nourry, Sandra / Betat, Anne-Marie / Maurin, Anne / Pakarinen, Maarit / Häkkinen, Sari / Tervapuro, Johanna / Pihlasvaara, Hertta / Drieu La Rochelle, Christophe / Joensuu, Heikki

    The Journal of pharmacology and experimental therapeutics

    2023  Volume 384, Issue 3, Page(s) 439–444

    Abstract: Cancer treatments are frequently associated with nausea and vomiting despite greatly improved preventive medication. Administration of antinausea agents as eye drops might provide easy and rapid access to the systemic circulation for prevention of nausea ...

    Abstract Cancer treatments are frequently associated with nausea and vomiting despite greatly improved preventive medication. Administration of antinausea agents as eye drops might provide easy and rapid access to the systemic circulation for prevention of nausea and vomiting and for the treatment of breakthrough nausea, but the ocular administration route has rarely been evaluated. Palonosetron is a second-generation 5-hydroxytryptamine 3 receptor antagonist approved for prevention and treatment of chemotherapy-induced nausea and vomiting. We compared ocular administration of palonosetron to non-active vehicle eye drops and to intravenous palonosetron in the prevention of cisplatin-induced nausea and vomiting in beagle dogs. Palonosetron ocular drops at the dose of 30
    MeSH term(s) Animals ; Dogs ; Palonosetron/adverse effects ; Cisplatin ; 2-Hydroxypropyl-beta-cyclodextrin ; Administration, Ophthalmic ; Isoquinolines/pharmacology ; Quinuclidines/pharmacology ; Vomiting/chemically induced ; Nausea/chemically induced ; Antineoplastic Agents/therapeutic use ; Dexamethasone
    Chemical Substances Palonosetron (5D06587D6R) ; Cisplatin (Q20Q21Q62J) ; 2-Hydroxypropyl-beta-cyclodextrin (1I96OHX6EK) ; Isoquinolines ; Quinuclidines ; Antineoplastic Agents ; Dexamethasone (7S5I7G3JQL)
    Language English
    Publishing date 2023-01-12
    Publishing country United States
    Document type Journal Article
    ZDB-ID 3106-9
    ISSN 1521-0103 ; 0022-3565
    ISSN (online) 1521-0103
    ISSN 0022-3565
    DOI 10.1124/jpet.122.001444
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. 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
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  6. 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
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  7. 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
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