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001-es BibID:BIBFORM074794
035-os BibID:(WoS)000447365100097 (Scopus)85052651287
Első szerző:Erdei Tamás Dániel (kísérletes farmakológus)
Cím:FSCPX, a chemical widely used as an irreversible A1 adenosine receptor antagonist, modifies the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium / Tamas Erdei, Adrienn Monika Szabo, Nora Lampe, Katalin Szabo, Rita Kiss, Judit Zsuga, Csaba Papp, Akos Pinter, Andras Jozsef Szentmiklosi, Zoltan Szilvassy, Bela Juhasz, Rudolf Gesztelyi
Dátum:2018
ISSN:1420-3049
Megjegyzések:Based on in silico results, recently we have assumed that FSCPX, an irreversible A1 adenosine receptor antagonist, inhibits the action of NBTI that is apparent on E/c curves of adenosine receptor agonists. As a mechanism for this unexpected effect, we hypothesized that FSCPX might modify the equilibrative and NBTI-sensitive nucleoside transporter (ENT1) in a way that it allows ENT1 to transport adenosine but impedes NBTI to inhibit this transport. This assumption implies that our method developed to estimate receptor reserve for agonists with short half-life such as adenosine, in its original form, overestimates the receptor reserve. In this study, therefore, our goals were to experimentally test our assumption on this effect of FSCPX, to improve our receptor reserve-estimating method, and then to compare the original and improved forms of this method. Thus, we improved our method and assessed the receptor reserve for the direct negative inotropic effect of adenosine with both forms of this method in guinea pig atria. We have found that FSCPX inhibits the effects of NBTI that are mediated by increasing the interstitial concentration of adenosine of endogenous (but not exogenous) origin. As a mechanism for this action of FSCPX, inhibition of enzymes participating in the interstitial adenosine production can be hypothesized, while modification of ENT1 can be excluded. Furthermore, we have shown that, in comparison with the improved form, the original version of our method overestimates receptor reserve, but only to a small extent. Nevertheless, use of the improved form is recommended in the future.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
adenosine
CPA
FSCPX
NBTI
A1 adenosine receptor
receptorial responsiveness method
atrium
Megjelenés:Molecules. - 23 : 9 (2018), p. 1-17. -
További szerzők:Szabó Adrienn Mónika (1982-) (orvos) Lampé Nóra Szabó Katalin (1989-) (táplálkozástudományi szakember) Kiss Rita (1974-) (laboratóriumi diagnosztika szakorvos) Zsuga Judit (1973-) (neurológus, pszichoterapeuta, egészségügyi szakmanager) Papp Csaba (1966-) (aneszteziológus és intenzív terápiás szakorvos) Pintér Ákos (1967-) (matematikus) Szentmiklósi József András (1948-) (farmakológus, klinikai laboratóriumi szakorvos) Szilvássy Zoltán (1957-) (belgyógyász, farmakológus, klinikai farmakológus) Juhász Béla (1978-) (kísérletes farmakológus) Gesztelyi Rudolf (1969-) (kísérletes farmakológus)
Pályázati támogatás:EFOP-3.6.2-16-2017-00015
EFOP
GINOP-2.3.2-15-2016-00043
GINOP
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
DOI
Szerző által megadott URL
Borító:

2.

001-es BibID:BIBFORM012829
Első szerző:Grenczer Maria (gyógyszerész)
Cím:Effect of asymmetry of concentration-response curves on the results obtained by the receptorial responsiveness method (RRM) : an in silico study / Grenczer Maria, Zsuga Judit, Majoros Laszlo, Pinter Akos, Kemeny-Beke Adam, Juhasz Bela, Tosaki Arpad, Gesztelyi Rudolf
Dátum:2010
ISSN:0008-4212
Megjegyzések:The receptorial responsiveness method (RRM) was proposed to estimate changes in the concentration of an agonist in the microenvironment of its receptor. Usually, this is done by providing the equieffective concentration of another agonist for the same receptor or for a largely overlapping postreceptorial signaling ("test agonist"). The RRM is a special nonlinear regression algorithm to analyze a concentration-response (E/c) curve that represents the simultaneous actions of a single agonist concentration to be estimated and of increasing concentrations of the test agonist. The aim of this study was to explore whether asymmetry of the E/c curve to be analyzed influences the reliability of the RRM. For this purpose, computer simulation was performed by constructing symmetric and asymmetric E/c curves using the operational model of agonism, and then these curves were analyzed with the RRM. To perform the RRM, 2 types of equations were used: one involving the Hill equation, the simplest model of the E/c relationship, and one containing the Richards equation, an advanced model properly handling E/c curve asymmetry. Results of this study indicate that E/c curve asymmetry does not significantly influence the accuracy of the estimates provided by the RRM. Thus, when using the RRM, it is not necessary to replace the Hill equation with the Richards equation to obtain useful estimates. Furthermore, it was found that estimation of a high concentration of a high-efficacy agonist can fail when the RRM is performed with a low-efficacy test agonist in a system characterized by a small operational slope factor.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Molekulatudomány
concentration-response curve
symmetry
operational model
efficacy
slope
concentration estimation
receptorial responsiveness method
RRM
Megjelenés:Canadian Journal Of Physiology And Pharmacology. - 88 : 11 (2010), p. 1074-1083. -
További szerzők:Zsuga Judit (1973-) (neurológus, pszichoterapeuta, egészségügyi szakmanager) Majoros László (1966-) (szakorvos, klinikai mikrobiológus) Pintér Ákos (1967-) (matematikus) Kemény-Beke Ádám (1968-2021) (szemész) Juhász Béla (1978-) (kísérletes farmakológus) Tósaki Árpád (1958-) (kísérletes farmakológus, gyógyszerész) Gesztelyi Rudolf (1969-) (kísérletes farmakológus)
Pályázati támogatás:TÁMOP-4.2.1/B-09/1 KONV-2010-0007
TÁMOP
Kardiovaszkuláris megbetegedések génterápiás befolyásolása
TÁMOP-4.2.2-08/1-2008-0007
TÁMOP
PD 78223
OTKA
K 72315
OTKA
Internet cím:Szerző által megadott URL
DOI
Intézményi repozitóriumban (DEA) tárolt változat
Borító:

3.

001-es BibID:BIBFORM012828
Első szerző:Grenczer Maria (gyógyszerész)
Cím:The influence of affinity, efficacy, and slope factor on the estimates obtained by the receptorial responsiveness method (RRM) : a computer simulation study / Grenczer Maria, Pinter Akos, Zsuga Judit, Kemeny-Beke Adam, Juhasz Bela, Szodoray Peter, Tosaki Arpad, Gesztelyi Rudolf
Dátum:2010
ISSN:0008-4212
Megjegyzések:The receptorial responsiveness method (RRM) was proposed to characterize changes in the concentration of degradable agonists in the microenvironment of their receptors. The characterization is done by providing concentrations of a stable agonist for the same receptor that is equieffective with the change in concentration to be characterized. RRM is based on the analysis of concentration-effect (E/c) curves reflecting the simultaneous action of the degradable and the stable agonist. In the present study, we investigated whether dissimilar affinity and (or) efficacy of the coacting agonists as well as the steepness of the E/c curves influence the reliability of RRM. E/c curves were simulated based on the operational model and then analyzed with RRM. We found that dissimilarity in affinity of the coacting agonists did not affect the accuracy of RRM estimates. In contrast, accuracy of the estimation depended on the magnitude of the concentration to be assessed, the operational slope factor, and the operational efficacy ratio of the coacting agonists. However, our results suggest that proper choice of a stable agonist for a degradable one can help to ensure reliable results, since information about the change in concentration of a degradable agonist is otherwise difficult to obtain.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Molekulatudomány
concentration estimation
affinity
efficacy
slope
receptorial responsiveness method
RRM
Megjelenés:Canadian Journal Of Physiology And Pharmacology. - 88 : 11 (2010), p. 1061-1073. -
További szerzők:Pintér Ákos (1967-) (matematikus) Zsuga Judit (1973-) (neurológus, pszichoterapeuta, egészségügyi szakmanager) Kemény-Beke Ádám (1968-2021) (szemész) Juhász Béla (1978-) (kísérletes farmakológus) Szodoray Péter (1973-) (belgyógyász, orvos) Tósaki Árpád (1958-) (kísérletes farmakológus, gyógyszerész) Gesztelyi Rudolf (1969-) (kísérletes farmakológus)
Pályázati támogatás:TÁMOP-4.2.1/B-09/1/KONV-2010-0007
TÁMOP
Kardiovaszkuláris megbetegedések génterápiás befolyásolása
TÁMOP-4.2.2-08/1-2008-0007
TÁMOP
PD 78223
OTKA
K 72315
OTKA
Internet cím:Szerző által megadott URL
DOI
Intézményi repozitóriumban (DEA) tárolt változat
Borító:

4.

001-es BibID:BIBFORM082554
035-os BibID:(PMID)31842299 (cikkazonosító)6264 (scopus)85076680797 (wos)000506840100158
Első szerző:Szabó Adrienn Mónika (orvos)
Cím:Accuracy and Precision of the Receptorial Responsiveness Method (RRM) in the Quantification of A1 Adenosine Receptor Agonists / Adrienn Monika Szabo, Gabor Viczjan, Tamas Erdei, Ildiko Simon, Rita Kiss, Andras Jozsef Szentmiklosi, Bela Juhasz, Csaba Papp, Judit Zsuga, Akos Pinter, Zoltan Szilvassy, Rudolf Gesztelyi
Dátum:2019
ISSN:1661-6596 1422-0067
Megjegyzések:The receptorial responsiveness method (RRM) is a procedure that is based on a simple nonlinear regression while using a model with two variables (X, Y) and (at least) one parameter to be determined (cx). The model of RRM describes the co-action of two agonists that consume the same response capacity (due to the use of the same postreceptorial signaling in a biological system). While using RRM, uniquely, an acute increase in the concentration of an agonist (near the receptors) can be quantified (as cx), via evaluating E/c curves that were constructed with the same or another agonist in the same system. As this measurement is sensitive to the implementation of the curve fitting, the goal of the present study was to test RRM by combining di erent ways and setting options, namely: individual vs. global fitting, ordinary vs. robust fitting, and three weighting options (no weighting vs. weighting by 1/Y2 vs. weighting by 1/SD2). During the testing, RRM was used to estimate the known concentrations of stable synthetic A1 adenosine receptor agonists in isolated, paced guinea pig left atria. The estimates were then compared to the known agonist concentrations (to assess the accuracy of RRM); furthermore, the 95% confidence limits of the best-fit values were also considered (to evaluate the precision of RRM). It was found that, although the global fitting o ered the most convenient way to perform RRM, the best estimates were provided by the individual fitting without any weighting, almost irrespective of the fact whether ordinary or robust fitting was chosen.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
A1 adenosine receptor
atrium
heart
receptorial responsiveness method
RRM
Megjelenés:International Journal Of Molecular Sciences. - 20 : 24 (2019), p. 1-14. -
További szerzők:Viczján Gábor (1993-) (kísérletes farmakológus) Erdei Tamás Dániel (1992-) (kísérletes farmakológus) Simon Ildikó (1987-) (radiográfus (BSc) Kiss Rita (1974-) (laboratóriumi diagnosztika szakorvos) Szentmiklósi József András (1948-) (farmakológus, klinikai laboratóriumi szakorvos) Juhász Béla (1978-) (kísérletes farmakológus) Papp Csaba (1966-) (aneszteziológus és intenzív terápiás szakorvos) Zsuga Judit (1973-) (neurológus, pszichoterapeuta, egészségügyi szakmanager) Pintér Ákos (1967-) (matematikus) Szilvássy Zoltán (1957-) (belgyógyász, farmakológus, klinikai farmakológus) Gesztelyi Rudolf (1969-) (kísérletes farmakológus)
Pályázati támogatás:EFOP-3.6.2-16-2017-00015
EFOP
GINOP-2.3.4-15-2016-00002
GINOP
NKFIH-1150-6/2019
Egyéb
Internet cím:Szerző által megadott URL
DOI
Intézményi repozitóriumban (DEA) tárolt változat
Borító:

5.

001-es BibID:BIBFORM079164
035-os BibID:(cikkazonosító)2207 (Wos)000473816900013 (Scopus)85067308414
Első szerző:Szabó Adrienn Mónika (orvos)
Cím:An Advanced in silico Modelling of the Interaction between FSCPX, an Irreversible A1 Adenosine Receptor Antagonist, and NBTI, a Nucleoside Transport Inhibitor, in the Guinea Pig Atrium / Adrienn Monika Szabo, Tamas Erdei, Gabor Viczjan, Rita Kiss, Judit Zsuga, Csaba Papp, Akos Pinter, Bela Juhasz, Zoltan Szilvassy, Rudolf Gesztelyi
Dátum:2019
ISSN:1420-3049
Megjegyzések:In earlier studies, we generated concentration-response (E/c) curves with CPA (N6- cyclopentyladenosine; a selective A1 adenosine receptor agonist) and adenosine, in the presence or absence of S-(2-hydroxy-5-nitrobenzyl)-6-thioinosine (NBTI, a selective nucleoside transport inhibitor), and with or without a pretreatment with 8-cyclopentyl-N3-[3-(4-(fluorosulfonyl)- benzoyloxy)propyl]-N1-propylxanthine (FSCPX, a chemical known as a selective, irreversible A1 adenosine receptor antagonist), in isolated, paced guinea pig left atria. Meanwhile, we observed a paradoxical phenomenon, i.e. the co-treatment with FSCPX and NBTI appeared to enhance the direct negative inotropic response to adenosine. In the present in silico study, we aimed to reproduce eight of these E/c curves. Four models (and two additional variants of the last model) were constructed, each one representing a set of assumptions, in order to find the model exhibiting the best fit to the ex vivo data, and to gain insight into the paradoxical phenomenon in question. We have obtained in silico evidence for an interference between effects of FSCPX and NBTI upon our ex vivo experimental setting. Regarding the mechanism of this interference, in silico evidence has been gained for the assumption that FSCPX inhibits the effect of NBTI on the level of endogenous (but not exogenous) adenosine. As an explanation, it may be hypothesized that FSCPX inhibits an enzyme participating in the interstitial adenosine formation. In addition, our results suggest that NBTI does not stop the inward adenosine flux in the guinea pig atrium completely.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
receptorial responsiveness method
RRM
computer simulation
FSCPX
NBTI
adenosine
Megjelenés:Molecules. - 24 : 12 (2019), p. 1-16. -
További szerzők:Erdei Tamás Dániel (1992-) (kísérletes farmakológus) Viczján Gábor (1993-) (kísérletes farmakológus) Kiss Rita (1974-) (laboratóriumi diagnosztika szakorvos) Zsuga Judit (1973-) (neurológus, pszichoterapeuta, egészségügyi szakmanager) Papp Csaba (1966-) (aneszteziológus és intenzív terápiás szakorvos) Pintér Ákos (1967-) (matematikus) Juhász Béla (1978-) (kísérletes farmakológus) Szilvássy Zoltán (1957-) (belgyógyász, farmakológus, klinikai farmakológus) Gesztelyi Rudolf (1969-) (kísérletes farmakológus)
Pályázati támogatás:EFOP-3.6.2-16-2017-00015
EFOP
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
DOI
Borító:

6.

001-es BibID:BIBFORM069057
035-os BibID:(cikkazonosító)839 (WoS)000404522900156 (Scopus)85020236730
Első szerző:Zsuga Judit (neurológus, pszichoterapeuta, egészségügyi szakmanager)
Cím:Methodical Challenges and a Possible Resolution in the Assessment of Receptor Reserve for Adenosine, an Agonist with Short Half-Life / Judit Zsuga, Tamas Erdei, Katalin Szabó, Nora Lampe, Csaba Papp, Akos Pinter, Andras Jozsef Szentmiklosi, Bela Juhasz, Zoltán Szilvássy, Rudolf Gesztelyi
Dátum:2017
ISSN:1420-3049
Megjegyzések:The term receptor reserve, first introduced and used in the traditional receptor theory, is an integrative measure of response-inducing ability of the interaction between an agonist and a receptor system (consisting of a receptor and its downstream signaling). The underlying phenomenon, i.e., stimulation of a submaximal fraction of receptors can apparently elicit the maximal effect (in certain cases), provides an opportunity to assess the receptor reserve. However, determining receptor reserve is challenging for agonists with short half-lives, such as adenosine. Although adenosine metabolism can be inhibited several ways (in order to prevent the rapid elimination of adenosine administered to construct concentration?effect (E/c) curves for the determination), the consequent accumulationof endogenous adenosine biases the results. To address this problem, we previously proposed a method, by means of which this bias can be mathematically corrected (utilizing a traditionalreceptor theory-independent approach). In the present investigation, we have offered in silico validation of this method by simulating E/c curves with the use of the operational model of agonism and then by evaluating them using our method. We have found that our method is suitable to reliably assess the receptor reserve for adenosine in our recently published experimental setting, suggesting that it may be capable for a qualitative determination of receptor reserve for rapidlyeliminating agonists in general. In addition, we have disclosed a possible interference between FSCPX (8-cyclopentyl-N3-[3-(4-(fluorosulfonyl)benzoyloxy)propyl]-N1-propylxanthine), an irreversible A1 adenosine receptor antagonist, and NBTI (S-(2-hydroxy-5-nitrobenzyl)-6-thioinosine), a nucleoside transport inhibitor, i.e., FSCPX may blunt the effect of NBTI.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
adenozin
szív
A1 adenozin receptor
pitvar
RRM
receptor rezerv
Megjelenés:Molecules. - 22 : 5 (2017), p. 1-17. -
További szerzők:Erdei Tamás Dániel (1992-) (kísérletes farmakológus) Szabó Katalin (1989-) (táplálkozástudományi szakember) Lampé Nóra Papp Csaba (1966-) (aneszteziológus és intenzív terápiás szakorvos) Pintér Ákos (1967-) (matematikus) Szentmiklósi József András (1948-) (farmakológus, klinikai laboratóriumi szakorvos) Juhász Béla (szülész-nőgyógyász) Szilvássy Zoltán (1957-) (belgyógyász, farmakológus, klinikai farmakológus) Gesztelyi Rudolf (1969-) (kísérletes farmakológus)
Pályázati támogatás:EFOP-3.6.2-16-2017-00015
Egyéb
Internet cím:DOI
Intézményi repozitóriumban (DEA) tárolt változat
Borító:
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