Wyniki wyszukiwania

1

Anticoagulant-related gastrointestinal bleeding: a real-life data analysis on bleeding profiles, frequency and etiology of patients receiving direct oral anticoagulants versus vitamin K antagonists

100%

Albrecht H., Maass L. S., Hagel A. F., Neurath M. F., Konturek P. C., Raithel M.

Journal of Physiology and Pharmacology

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2019

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tom 70

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nr 6

2

Impaired effect of activation of rat hippocampal 5-HT7 receptors, induced by treatment with the 5-HT7 receptor antagonist SB 269970

86%

Kusek M., Sowa J., Tokarski K., Hess G.

Journal of Physiology and Pharmacology

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2015

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tom 66

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nr 2

3

Four close bupranolol analogues are antagonists at the low-affinity state of beta1-adrenoceptors

86%

Zelaszczyk D., Kozlowska H., Baranowska U., Baranowska M., Reutelsterz A., Kiec-Kononowicz K., Malinowska B., Schlicker E.

Journal of Physiology and Pharmacology

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2009

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tom 60

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nr 1

51-60

Bupranolol is an antagonist at the cardiostimulatory low-affinity state of ß1-adrenoceptors and we were interested whether this effect is shared by its fluorine (GD-6), methyl (DZ-51) and isopropyl analogue (DZ-13) and by the analogue hydroxylated at the tertiary butyl moiety (DZ-52). (-)-Bupranolol and compounds (-)-GD-6, (+)-GD-6, (-)-DZ-13, (+)-DZ-13, DZ-51 and DZ-52 antagonized the CGP 12177-induced tachycardia in pithed rats with “apparent pA2 values” of 6.1, 6.1, 4.6, 5.5, 4.6, 5.1 and 5.3, respectively. For comparison, their potencies and affinities at the high-affinity state of ß1-adrenoceptors were determined, using the xamoterol-induced tachycardia in pithed rats and [3H]CGP 12177 binding to rat cerebrocortical membranes. The respective “apparent pA2 values” in the functional experiments were 7.9, 8.1, 5.4, 8.4, 5.7, 7.3 and 6.8 and the pKi values in the binding experiments were 8.8, 8.4, 6.9, 8.5, 6.7, 8.4 and 8.2. In conclusion, (-)-bupranolol and its fluorine analogue (-)-GD-6 are equipotent at the low-affinity state of ß1-adrenoceptors. The stereoselectivity of GD-6 and DZ-13 suggests that the low-affinity state is indeed a receptor.

4

The antagonists of slow-calcium channel; toxicological problems

86%

Borowiak K., Waloszczyk P.

Acta Poloniae Toxicologica

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1996

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tom 04

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nr 2

5

Opioids modulate the plasma cortisol

86%

Pierzchala-Koziec K.

Acta Agraria et Silvestria. Series Zootechnica

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2000

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tom 38

6

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Anti-schizophrenic activities of histamine H3 receptor antagonists in rats treated with MK-801

72%

Mahmood D., Akhtar M.

Journal of Pre-Clinical and Clinical Research

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2015

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tom 09

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nr 1

Animal models based on N-methyl-d-aspartate (NMDA) receptor blockade have been widely reported. Ketamine and MK- 801, the two noncompetitive antagonists of NMDA receptors, produce behaviors related to schizophrenia and exacerbated symptoms in patients with schizophrenia. The study presented here investigated the effect of subchronic dosing (once-daily, 7 day) of histamine H3 receptor (H3R) antagonists, ciproxifan (CPX) (3 mg/kg, i.p.) and clobenpropit (CBP) (15 mg/kg, i.p) including clozapine (CLZ) (3.0 mg/kg, i.p.) and chlorpromazine (CPZ) (3.0 mg/kg, i.p.), the atypical and typical antipsychotic, respectively, on MK-801(0.2 mg/kg, i.p.)-induced locomotor activity, and dopamine and histamine levels in rats. Atypical and typical antipsychotic was used to serve as clinically relevant reference agents to compare the effects of the H3R antagonists. MK-801 significantly increased horizontal activity which was reduced with CPX and CBP. The attenuation of MK-801-induced locomotor hyperactivity produced CPX and CBP were comparable to CLZ and CPZ. Dopamine and histamine levels were measured in striatum and hypothalamus, respectively, of rat brain. The MK-801 induced increase of the striatal dopamine level was reduced in rats pretreated with CPX and CBP including CLZ. CPZ also significantly lowered striatal dopamine levels, though the decrease was less robust compared to CLZ, CPX and CBP. MK-801 increased histamine content although to a lesser degree. Subchronic treatment with CPX and CBP exhibited further increased histamine levels in the hypothalamus compared to MK-801 treatment alone. Histamine H3 receptor agonist, R-α methylhistamine (10 mg/kg, i.p.) counteracted the effect of CPX and CBP. The findings of the present study support our previous work showing positive effects of CPX and CBP on MK-801-induced schizophrenia like behaviors in rodents. However, clinical studies have reported no antipsychotic effects with histamine H3 receptor antagonists.

7

Viscoelastic properties of plasma fibrin clots are similar in patients on rivaroxaban and vitamin K antagonists

72%

Kopytek M., Zabczyk M., Natorska J., Siudut J., Malinowski K. P., Ptaszek P., Glajcar A., Goralczyk T., Undas A.

Journal of Physiology and Pharmacology

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2019

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tom 70

|

nr 1

8

Thioperamide, antagonist of histamine H3 receptors, increases brain production of kynurenic acid

72%

Jaroslawska-Zych A., Kowalczyk M. S., Kloc R., Urbanska E. M.

Journal of Pre-Clinical and Clinical Research

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2010

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tom 04

|

nr 1

9

Involvement of the histaminergic system in the resuscitating effect of centrally acting leptin in haemorrhagic shock in rats

72%

Jochem J., Altinbas B., Yalcin M., Ottani A., Giuliani D., Savci V., Kasperska-Zajac A., Guarini S.

Journal of Physiology and Pharmacology

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2016

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tom 67

|

nr 1

10

In vitro interactions between Trichoderma harzianum and pathogenic fungi damaging horse-chestnut (Aesculus hippocastanum) leaves and fruits

72%

Pastircakova K.

Biological Letters

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2019

|

tom 54

|

nr 1

11

Orexin A reverses propofol and thiopental induced cytoskeletal rearrangement in rat neurons

72%

Turina D., Gerhardsson H., Bjornstrom K.

Journal of Physiology and Pharmacology

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2014

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tom 65

|

nr 4

12

Suppression of growth of Fusarium verticillioides Niren. using strains of Trichoderma harzianum from maize [Zea mays] plant parts and its rhizosphere

72%

Sobowale A. A., Odebode A. C., Cardwell K. F., Bandyopadhyay R.

Journal of Plant Protection Research

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2009

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tom 49

|

nr 4

452-459

Three strains of Trichoderma harzianum (strain 1: IMI 380934; strain 2: IMI 380935; strain 3: IMI 380938) were compared for their ability to suppress radial growth of Fusarium verticillioides in vitro. Each Trichoderma strain was paired with the pathogen F. verticillioides on 9 cm Petri plates of acidified potato dextrose agar using three pairing methods. Varying growth suppression of pathogen by Trichoderma strains was rated and ratings were analysed using GLM Procedure of SAS. Growth inhibition of F. verticillioides by each of the T. harzianum strains was significantly different from control irrespective of pairing method (p = 0.01, R2 = 0.96). Higher inhibition of F. verticillioides was obtained by inoculating antagonist before pathogen even at p = 0.01. Mode of suppression includes mycoparasitism and competition for space and nutrients. Growth inhibition of pathogen differed significantly among (p > 0.0001) and within (p > 0.026) pairing methods. T. harzianum strain 1 had better suppression of pathogen than the other two strains when it was inoculated before the pathogen while T. harzianum strain 3 was better when pathogen and antagonist were inoculated simultaneously (p = 0.05). Different strains of T. harzianum could thus be employed as promising antagonists of F. verticillioides.

13

Some behavioral effects of AMPA-kainate receptor agonist and antagonists

72%

Czlonkowska A., Siemiatkowski M., Plaznik A.

Journal of Physiology and Pharmacology

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1997

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tom 48

|

nr 3

14

Biocontrol research in Uppsala - mostly disappointments, but some promises

72%

Gerhardson B.

Bulletin of the Polish Academy of Sciences. Biological Sciences

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1999

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tom 47

|

nr 2-4

15

Novel nociceptin analogues

72%

Bartosz-Bechowski H., Miedzybrodzki R., Szymaniec S.

Acta Biochimica Polonica

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2001

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tom 48

|

nr 4

A series of new nociceptin analogues containing cysteine was tested for their nociceptive effects in tail-flick test on mice after icv injection. The cysteines were introduced in order to get irreversibly binding analogues based on the assumption that the cysteines in the ligand can interact with the cysteines from the receptor to form an S-S bridge. In vivo tests revealed that CysX-nociceptin (1-13)-NH2 (Cys1-NC) is an antagonist, whereas Cys7-NC is an agonist. Gly1 ,[Phe(p-NO2)]4 -NC was less active indicating that the antagonist properties of Cys1-NC are associated with the presence of the sulfhydryl group of cysteine. The analogues D-Cys2 and Cys3 were also almost inactive.

16

Adenosine diphosphate receptors on blood platelets - potential new targets for antiplatelet therapy

72%

Rozalski M., Nocun M., Watala C.

Acta Biochimica Polonica

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2005

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tom 52

|

nr 2

Platelets play a key role not only in physiological haemostasis, but also under pathological conditions such as thrombosis. Platelet activation may be initiated by a variety of agonists including thrombin, collagen, thromboxane or adenosine diphosphate (ADP). Although ADP is regarded as a weak agonist of blood platelets, it remains an important mediator of platelet activation evoked by other agonists, which induce massive ADP release from dense granules, where it occurs in molar concentrations. Thus, ADP action underlies a positive feedback that facilitates further platelet aggregation and leads to platelet plug formation. Additionally, ADP acts synergistically to other, even weak, agonists such as serotonin, adrenaline or chemokines. Blood platelets express two types of P2Y ADP receptors: P2Y1 and P2Y12. ADP-dependent platelet aggregation is initiated by the P2Y1 receptor, whereas P2Y12 receptor augments the activating signal and promotes platelet release reaction. Stimulation of P2Y12 is also essential for ADP-mediated complete activation of GPIIb-IIIa and GPIa-IIa, and further stabilization of platelet aggregates. The crucial role in blood platelet biology makes P2Y12 an ideal candidate for pharmacological approaches for anti-platelet therapy.

17

Molecular modelling of the vasopressin V2 receptor-antagonist interactions

72%

Czaplewski C., Kazmierkiewicz R., Ciarkowski J.

Acta Biochimica Polonica

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1998

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tom 45

|

nr 1

We predict some essential interactions between the V2 vasopressin renal receptor (V2R) and its selective peptide antagonist desGly9-[Mca1,D-Ile2,Ile4]AVP, and compare these predictions with the earlier ones for the non-peptide OPC-36120 antagonist- and the [Arg8]vasopressin (AVP) agonist-V2 receptor interactions. V2R controls antidiuresis in mammals and belongs to the superfamily of the heptahelical transmembrane (7TM) G protein-coupled receptors (GPCR)s. V2R was built, the ligands docked and the structures relaxed using advanced molecular modeling techniques. Both the agonist and the antagonists (no matter whether of peptide- or non-peptide type) appear to prefer a common V2R compartment for docking. The receptor amino-acid residues, potentially important in ligand binding, are mainly in the TM3-TM7 helices. A few of these residues are invariant for the whole GPCR superfamily while most of them are conserved in the subfamily of neurohypophyseal receptors, to which V2R belongs. Some of the equivalent residues in a related V1a receptor have been earlier reported as critical for the ligand affinity.

18

Selection and testing of microorganisms antagonistic toward Cephalosporium gramineum

72%

Martyniuk S., Martyniuk M.

Bulletin of the Polish Academy of Sciences. Biological Sciences

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2001

|

tom 49

|

nr 4

19

Effect of ghrelin receptor agonist and antagonist on the activity of arcuate nucleus tyrosine hydroxylase containing neurons in C57BL/6 male mice exposed to normal or high fat diet

58%

Pirnik Z., Majercikova Z., Holubova M., Pirnik R., Zelezna B., Maletinska L., Kiss A.

Journal of Physiology and Pharmacology

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2014

|

tom 65

|

nr 4

20

The effect of selected agonists and antagonists of cholinergic receptors on the motor activity of epithelium of Achatina fulica

58%

Kaczorowski P.

Folia Malacologica

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2016

|

tom 24

|

nr 1

Ograniczanie wyników

Anticoagulant-related gastrointestinal bleeding: a real-life data analysis on bleeding profiles, frequency and etiology of patients receiving direct oral anticoagulants versus vitamin K antagonists

Impaired effect of activation of rat hippocampal 5-HT7 receptors, induced by treatment with the 5-HT7 receptor antagonist SB 269970

Four close bupranolol analogues are antagonists at the low-affinity state of beta1-adrenoceptors

The antagonists of slow-calcium channel; toxicological problems

Opioids modulate the plasma cortisol

Anti-schizophrenic activities of histamine H3 receptor antagonists in rats treated with MK-801

Viscoelastic properties of plasma fibrin clots are similar in patients on rivaroxaban and vitamin K antagonists

Thioperamide, antagonist of histamine H3 receptors, increases brain production of kynurenic acid

Involvement of the histaminergic system in the resuscitating effect of centrally acting leptin in haemorrhagic shock in rats

In vitro interactions between Trichoderma harzianum and pathogenic fungi damaging horse-chestnut (Aesculus hippocastanum) leaves and fruits

Orexin A reverses propofol and thiopental induced cytoskeletal rearrangement in rat neurons

Suppression of growth of Fusarium verticillioides Niren. using strains of Trichoderma harzianum from maize [Zea mays] plant parts and its rhizosphere

Some behavioral effects of AMPA-kainate receptor agonist and antagonists

Biocontrol research in Uppsala - mostly disappointments, but some promises

Novel nociceptin analogues

Adenosine diphosphate receptors on blood platelets - potential new targets for antiplatelet therapy

Molecular modelling of the vasopressin V2 receptor-antagonist interactions

Selection and testing of microorganisms antagonistic toward Cephalosporium gramineum

Effect of ghrelin receptor agonist and antagonist on the activity of arcuate nucleus tyrosine hydroxylase containing neurons in C57BL/6 male mice exposed to normal or high fat diet

The effect of selected agonists and antagonists of cholinergic receptors on the motor activity of epithelium of Achatina fulica