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  1. Artikel: Basic aspects of the pharmacodynamics of tolperisone, a widely applicable centrally acting muscle relaxant.

    Tekes, Kornelia

    The open medicinal chemistry journal

    2014  Band 8, Seite(n) 17–22

    Abstract: Tolperisone (2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one hydro-chloride) was introduced in the clinical practice more than forty years ago and is still evaluated as a widely applicable compound in pathologically elevated skeletal muscle tone ...

    Abstract Tolperisone (2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one hydro-chloride) was introduced in the clinical practice more than forty years ago and is still evaluated as a widely applicable compound in pathologically elevated skeletal muscle tone (spasticity) and related pains of different origin. In the present review, basic pharmacodynamic effects measured on whole animals, analyses of its actions on cell and tissue preparations and molecular mechanism of action on sodium and calcium channels are summarized as recently significantly new data were reported.
    Sprache Englisch
    Erscheinungsdatum 2014-07-11
    Erscheinungsland United Arab Emirates
    Dokumenttyp Journal Article
    ZDB-ID 2395968-X
    ISSN 1874-1045
    ISSN 1874-1045
    DOI 10.2174/1874104501408010017
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  2. Artikel ; Online: An Update on the Molecular and Cellular Basis of Pharmacotherapy in Type 2 Diabetes Mellitus.

    Mahgoub, Mohamed Omer / Ali, Ifrah Ismail / Adeghate, Jennifer O / Tekes, Kornélia / Kalász, Huba / Adeghate, Ernest A

    International journal of molecular sciences

    2023  Band 24, Heft 11

    Abstract: Diabetes mellitus (DM) is a chronic illness with an increasing global prevalence. More than 537 million cases of diabetes were reported worldwide in 2021, and the number is steadily increasing. The worldwide number of people suffering from DM is ... ...

    Abstract Diabetes mellitus (DM) is a chronic illness with an increasing global prevalence. More than 537 million cases of diabetes were reported worldwide in 2021, and the number is steadily increasing. The worldwide number of people suffering from DM is projected to reach 783 million in 2045. In 2021 alone, more than USD 966 billion was spent on the management of DM. Reduced physical activity due to urbanization is believed to be the major cause of the increase in the incidence of the disease, as it is associated with higher rates of obesity. Diabetes poses a risk for chronic complications such as nephropathy, angiopathy, neuropathy and retinopathy. Hence, the successful management of blood glucose is the cornerstone of DM therapy. The effective management of the hyperglycemia associated with type 2 diabetes includes physical exercise, diet and therapeutic interventions (insulin, biguanides, second generation sulfonylureas, glucagon-like peptide 1 agonists, dipeptidyl-peptidase 4 inhibitors, thiazolidinediones, amylin mimetics, meglitinides, α-glucosidase inhibitors, sodium-glucose cotransporter-2 inhibitors and bile acid sequestrants). The optimal and timely treatment of DM improves the quality of life and reduces the severe burden of the disease for patients. Genetic testing, examining the roles of different genes involved in the pathogenesis of DM, may also help to achieve optimal DM management in the future by reducing the incidence of DM and by enhancing the use of individualized treatment regimens.
    Mesh-Begriff(e) Humans ; Diabetes Mellitus, Type 2/complications ; Hypoglycemic Agents/therapeutic use ; Hypoglycemic Agents/pharmacology ; Quality of Life ; Sodium-Glucose Transporter 2 Inhibitors/therapeutic use ; Dipeptidyl-Peptidase IV Inhibitors/pharmacology ; Dipeptidyl-Peptidase IV Inhibitors/therapeutic use
    Chemische Substanzen Hypoglycemic Agents ; Sodium-Glucose Transporter 2 Inhibitors ; Dipeptidyl-Peptidase IV Inhibitors
    Sprache Englisch
    Erscheinungsdatum 2023-05-26
    Erscheinungsland Switzerland
    Dokumenttyp Journal Article ; Review
    ZDB-ID 2019364-6
    ISSN 1422-0067 ; 1422-0067 ; 1661-6596
    ISSN (online) 1422-0067
    ISSN 1422-0067 ; 1661-6596
    DOI 10.3390/ijms24119328
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  3. Artikel ; Online: Pharmacokinetics of Two Chlorine-Substituted Bis-Pyridinium Mono-Aldoximes with Regenerating Effect on Butyrylcholinesterase.

    Kalász, Huba / Szimrók, Zoltán / Karvaly, Gellért / Adeghate, Jennifer / Tekes, Kornélia

    Molecules (Basel, Switzerland)

    2020  Band 25, Heft 5

    Abstract: Our aim was to find chlorine-substituted antidotes against organophosphate poisoning and compare their pharmacokinetics to their parent compound, K-203. White male Wistar rats were intramuscularly injected with K-203, K-867 or K-870. Serum, brain, ... ...

    Abstract Our aim was to find chlorine-substituted antidotes against organophosphate poisoning and compare their pharmacokinetics to their parent compound, K-203. White male Wistar rats were intramuscularly injected with K-203, K-867 or K-870. Serum, brain, kidneys, liver, lung, eyes, and testes tissues were taken after 5, 15, 30, 60, and 120 min and analyzed using reversed-phase high-performance liquid chromatography. K-203, K-867, or K-870 was present in every tissue that was analyzed, including the serum, the eyes, testes, liver, kidneys, lungs, and the brain. The serum levels of K-867 and K-870 (chlorine-substituted derivatives of K-203) were nearly constant between 15 and 30 min, while their parent compound (K-203) showed peak level at 15 min after the administration of 30 µmol/rat. Neither K-203, nor K-867 or K-870 were toxic at a dose of 100 µmol/200 g in rats. Chlorine-substitution of K-867 and K-870 produced limited absorbance and distribution compared to their parent compound, K203.
    Mesh-Begriff(e) Animals ; Antidotes/metabolism ; Butyrylcholinesterase/metabolism ; Chlorine ; Male ; Organophosphate Poisoning/drug therapy ; Oximes/pharmacokinetics ; Pyridinium Compounds/pharmacokinetics ; Rats ; Rats, Wistar
    Chemische Substanzen Antidotes ; Oximes ; Pyridinium Compounds ; Chlorine (4R7X1O2820) ; Butyrylcholinesterase (EC 3.1.1.8)
    Sprache Englisch
    Erscheinungsdatum 2020-03-10
    Erscheinungsland Switzerland
    Dokumenttyp Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules25051250
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  4. Artikel: HPLC determination of serotonin and its metabolites from human platelet-rich plasma; shift to 5-hydroxytryptophol formation following alcohol consumption.

    Tekes, Kornélia

    Journal of chromatographic science

    2008  Band 46, Heft 2, Seite(n) 169–173

    Abstract: A sensitive, simple, and reliable high-performance liquid chromatographic method with electrochemical detection is developed for the measurement of four natural products, the serotonin-related indols from human platelet-rich plasma (PRP) using N- ... ...

    Abstract A sensitive, simple, and reliable high-performance liquid chromatographic method with electrochemical detection is developed for the measurement of four natural products, the serotonin-related indols from human platelet-rich plasma (PRP) using N-methylserotonin as internal standard. Separation of serotonin (5HT), 5-hydroxytryptophan (5HTP), 5-hydroxytryptophol (5HTOL), and 5-hydroxyindole-acetic acid (5HIAA) is carried out on Supelcosil LC-18DB stationary phase. A mixture of 48 mM citric acid, 28 mM sodium phosphate dibasic, 0.027 mM Na2EDTA, and 3% methanol (pH 3.18) serves as the mobile phase. Measurements are carried out at 25 degrees C at Eox=0.65 V. The calibration curves are linear through the range of 10-200 pg/mL. Method validation is performed according to internationally accepted criteria. Blood is collected from healthy controls and schizophrenic subjects. Significantly higher PRP serotonin is measured in schizophrenics; patients with recent alcohol consumption could be characterized with significantly elevated 5HTOL/5HIAA ratio.
    Mesh-Begriff(e) 5-Hydroxytryptophan/blood ; Adult ; Alcohol Drinking/metabolism ; Chromatography, High Pressure Liquid ; Female ; Humans ; Hydroxyindoleacetic Acid/blood ; Hydroxytryptophol/blood ; Hydroxytryptophol/metabolism ; Male ; Middle Aged ; Platelet-Rich Plasma/chemistry ; Schizophrenia/metabolism ; Serotonin/analogs & derivatives ; Serotonin/blood ; Serotonin/metabolism ; Statistics, Nonparametric
    Chemische Substanzen N-methylserotonin (1134-01-6) ; Hydroxytryptophol (154-02-9) ; Serotonin (333DO1RDJY) ; Hydroxyindoleacetic Acid (54-16-0) ; 5-Hydroxytryptophan (C1LJO185Q9)
    Sprache Englisch
    Erscheinungsdatum 2008-03-19
    Erscheinungsland United States
    Dokumenttyp Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 80141-0
    ISSN 1945-239X ; 0021-9665
    ISSN (online) 1945-239X
    ISSN 0021-9665
    DOI 10.1093/chromsci/46.2.169
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  5. Artikel ; Online: Tackling type 2 diabetes-associated cardiovascular and renal comorbidities: a key challenge for drug development.

    Adeghate, Ernest A / Kalász, Huba / Al Jaberi, Saeeda / Adeghate, Jennifer / Tekes, Kornelia

    Expert opinion on investigational drugs

    2020  Band 30, Heft 2, Seite(n) 85–93

    Mesh-Begriff(e) Animals ; Cardiovascular Diseases/prevention & control ; Diabetes Mellitus, Type 2/complications ; Diabetes Mellitus, Type 2/drug therapy ; Diabetic Nephropathies/prevention & control ; Drug Development ; Humans ; Hypoglycemic Agents/therapeutic use
    Chemische Substanzen Hypoglycemic Agents
    Sprache Englisch
    Erscheinungsdatum 2020-12-28
    Erscheinungsland England
    Dokumenttyp Editorial
    ZDB-ID 1182884-5
    ISSN 1744-7658 ; 0967-8298 ; 1354-3784
    ISSN (online) 1744-7658
    ISSN 0967-8298 ; 1354-3784
    DOI 10.1080/13543784.2021.1865914
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  6. Artikel: Nociceptin Increases Antioxidant Expression in the Kidney, Liver and Brain of Diabetic Rats.

    Adeghate, Ernest / D'Souza, Crystal M / Saeed, Zulqarnain / Al Jaberi, Saeeda / Tariq, Saeed / Kalász, Huba / Tekes, Kornélia / Adeghate, Ernest A

    Biology

    2021  Band 10, Heft 7

    Abstract: Nociceptin (NC) consists of 17 amino acids (aa) and takes part in the processing of learning and memory. The role of NC in the induction of endogenous antioxidants in still unclear. We examined the effect of NC on the expression of endogenous ... ...

    Abstract Nociceptin (NC) consists of 17 amino acids (aa) and takes part in the processing of learning and memory. The role of NC in the induction of endogenous antioxidants in still unclear. We examined the effect of NC on the expression of endogenous antioxidants in kidney, liver, cerebral cortex (CC), and hippocampus after the onset of diabetes mellitus, using enzyme-linked immunosorbent assay and immunohistochemistry. Exogenous NC (aa chain 1-17; 10 µg/kg body weight) was given intraperitoneally to normal and diabetic rats for 5 days. Our results showed that catalase (CAT) is present in the proximal (PCT) and distal (DCT) convoluted tubules of kidney, hepatocytes, and neurons of CC and hippocampus. The expression of CAT was significantly (
    Sprache Englisch
    Erscheinungsdatum 2021-07-03
    Erscheinungsland Switzerland
    Dokumenttyp Journal Article
    ZDB-ID 2661517-4
    ISSN 2079-7737
    ISSN 2079-7737
    DOI 10.3390/biology10070621
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  7. Artikel: Nociceptin Increases Antioxidant Expression in the Kidney, Liver and Brain of Diabetic Rats

    Adeghate, Ernest / D’Souza, Crystal M. / Saeed, Zulqarnain / Al Jaberi, Saeeda / Tariq, Saeed / Kalász, Huba / Tekes, Kornélia / Adeghate, Ernest A.

    Biology. 2021 July 03, v. 10, no. 7

    2021  

    Abstract: Nociceptin (NC) consists of 17 amino acids (aa) and takes part in the processing of learning and memory. The role of NC in the induction of endogenous antioxidants in still unclear. We examined the effect of NC on the expression of endogenous ... ...

    Abstract Nociceptin (NC) consists of 17 amino acids (aa) and takes part in the processing of learning and memory. The role of NC in the induction of endogenous antioxidants in still unclear. We examined the effect of NC on the expression of endogenous antioxidants in kidney, liver, cerebral cortex (CC), and hippocampus after the onset of diabetes mellitus, using enzyme-linked immunosorbent assay and immunohistochemistry. Exogenous NC (aa chain 1–17; 10 µg/kg body weight) was given intraperitoneally to normal and diabetic rats for 5 days. Our results showed that catalase (CAT) is present in the proximal (PCT) and distal (DCT) convoluted tubules of kidney, hepatocytes, and neurons of CC and hippocampus. The expression of CAT was significantly (p < 0.05) reduced in the kidney of normal and diabetic rats after treatment with NC. However, NC markedly (p < 0.001) increased the expression CAT in the liver and neurons of CC of diabetic rats. Superoxide dismutase (SOD) is widely distributed in the PCT and DCT of kidney, hepatocytes, and neurons of CC and hippocampus. NC significantly (p < 0.001) increased the expression of SOD in hepatocytes and neurons of CC and the hippocampus but not in the kidney. Glutathione reductase (GRED) was observed in kidney tubules, hepatocytes and neurons of the brain. NC markedly increased (p < 0.001) the expression of GRED in PCT and DCT cells of the kidney and hepatocytes of liver and neurons of CC. In conclusion, NC is a strong inducer of CAT, SOD, and GRED expression in the kidney, liver and brain of diabetic rats.
    Schlagwörter antioxidants ; body weight ; catalase ; cerebral cortex ; diabetes mellitus ; enzyme-linked immunosorbent assay ; glutathione-disulfide reductase ; hepatocytes ; hippocampus ; immunohistochemistry ; liver ; memory ; superoxide dismutase
    Sprache Englisch
    Erscheinungsverlauf 2021-0703
    Erscheinungsort Multidisciplinary Digital Publishing Institute
    Dokumenttyp Artikel
    ZDB-ID 2661517-4
    ISSN 2079-7737
    ISSN 2079-7737
    DOI 10.3390/biology10070621
    Datenquelle NAL Katalog (AGRICOLA)

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  8. Artikel ; Online: Circulating nociceptin and CGRP in medication-overuse headache.

    Munksgaard, Signe B / Ertsey, Csaba / Frandsen, Erik / Bendtsen, Lars / Tekes, Kornelia / Jensen, Rigmor H

    Acta neurologica Scandinavica

    2018  Band 139, Heft 3, Seite(n) 269–275

    Abstract: Background: Previous studies found low serum levels of nociceptin in migraine patients but high serum levels of calcitonin gene-related peptide (CGRP). CGRP can elicit migraine-like headache. Medication-Overuse Headache (MOH) often has migraine features ...

    Abstract Background: Previous studies found low serum levels of nociceptin in migraine patients but high serum levels of calcitonin gene-related peptide (CGRP). CGRP can elicit migraine-like headache. Medication-Overuse Headache (MOH) often has migraine features and can mimic chronic migraine. We therefore hypothesized that as in migraine, serum levels of nociceptin would be lower and CGRP serum levels higher in MOH patients compared with those in healthy volunteers. We hypothesized that the serum levels would normalize after detoxification.
    Methods: Seventeen MOH patients, hereof 70.6% with chronic migraine and MOH, and 30 sex and age matched headache-free controls were included. MOH patients underwent a 2-month outpatient detoxification program and after 6 months, 10 patients and 19 controls were retested. Blood samples were analyzed blinded.
    Results: We found no differences in the levels of nociceptin and CGRP between MOH patients and controls (P = 0.65 and P = 0.59). The mean headache frequency reduction was 43% and 70% of patients reverted to episodic headache after 6 months, but the levels of nociceptin and CGRP were unchanged (P = 0.71 and P = 0.82).
    Conclusion: In contrast to previous findings in migraine patients, we found normal serum levels of nociceptin and CGRP in MOH patients. Thus, we find no evidence that the increased headache frequency of MOH patients could be caused by altered nociceptin and CGRP levels. This underlines the importance of identifying medication overuse in chronic headache and treating the MOH.
    Mesh-Begriff(e) Adult ; Calcitonin Gene-Related Peptide/blood ; Female ; Headache Disorders, Secondary/blood ; Headache Disorders, Secondary/drug therapy ; Humans ; Male ; Middle Aged ; Opioid Peptides/blood ; Nociceptin
    Chemische Substanzen Opioid Peptides ; Calcitonin Gene-Related Peptide (JHB2QIZ69Z)
    Sprache Englisch
    Erscheinungsdatum 2018-12-11
    Erscheinungsland Denmark
    Dokumenttyp Journal Article
    ZDB-ID 90-5
    ISSN 1600-0404 ; 0001-6314
    ISSN (online) 1600-0404
    ISSN 0001-6314
    DOI 10.1111/ane.13053
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  9. Artikel ; Online: Penetration of polar organic compounds through the blood-brain barrier

    Kalász Huba / Musílek Kamil / Tekes Kornélia

    BMC Pharmacology, Vol 11, Iss Suppl 2, p A

    2011  Band 51

    Schlagwörter Therapeutics. Pharmacology ; RM1-950 ; Medicine ; R ; DOAJ:Therapeutics ; DOAJ:Medicine (General) ; DOAJ:Health Sciences
    Sprache Englisch
    Erscheinungsdatum 2011-09-01T00:00:00Z
    Verlag BioMed Central
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  10. Artikel ; Online: Novel biological therapies for the treatment of diabetic foot ulcers.

    Adeghate, Jennifer / Nurulain, Syed / Tekes, Kornélia / Fehér, Erzsébet / Kalász, Huba / Adeghate, Ernest

    Expert opinion on biological therapy

    2017  Band 17, Heft 8, Seite(n) 979–987

    Abstract: Introduction: The number of people with diabetes mellitus (DM) is estimated to exceed 640 million by the year 2040. Diabetic foot ulcer (DFU) is a debilitating illness that affects more than 2% of DM patients. DFU is caused by DM-induced neural and ... ...

    Abstract Introduction: The number of people with diabetes mellitus (DM) is estimated to exceed 640 million by the year 2040. Diabetic foot ulcer (DFU) is a debilitating illness that affects more than 2% of DM patients. DFU is caused by DM-induced neural and vascular lesions leading to a reduced sensation and microcirculation. The increase in the prevalence of DFU has prompted researchers to find new therapies for the management of DFU. Areas covered: This review presents the current status of novel biological therapies used in the treatment of DFU. Literature information and data analysis were collected from PubMed, the website of the American Diabetes Association, and ClinicalTrials.gov. The keywords used in the search were: DM, DFU, complications of DM. Expert opinion: Many biological agents have been investigated in a bid to find an effective therapy for DFU. These include growth factors (platelet-derived growth factor, vascular endothelial growth factor etc), stem cells (epithelial progenitor-, adipose-derived stem cells etc), anti-diabetic drugs (insulin, exendin-4), herbs, urokinase, dalteparin, statins and bio-agents such as acid peptide matrix. Biological agents that can reduce hyperglycaemia, increase sensation, microcirculation and oxygenation and repair lost tissue are the most ideal for the treatment of DFU.
    Mesh-Begriff(e) Biological Products/therapeutic use ; Diabetic Foot/drug therapy ; Diabetic Foot/etiology ; Diabetic Foot/therapy ; Diabetic Neuropathies/complications ; Humans ; Hypoglycemic Agents/therapeutic use ; Immunomodulation ; Intercellular Signaling Peptides and Proteins/therapeutic use ; Stem Cell Transplantation ; Urokinase-Type Plasminogen Activator/therapeutic use ; Wound Healing
    Chemische Substanzen Biological Products ; Hypoglycemic Agents ; Intercellular Signaling Peptides and Proteins ; Urokinase-Type Plasminogen Activator (EC 3.4.21.73)
    Sprache Englisch
    Erscheinungsdatum 2017-08
    Erscheinungsland England
    Dokumenttyp Journal Article ; Review
    ZDB-ID 2052501-1
    ISSN 1744-7682 ; 1471-2598
    ISSN (online) 1744-7682
    ISSN 1471-2598
    DOI 10.1080/14712598.2017.1333596
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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