Reseptör stimole ve bloke edici ilaçların agonistik ve antagonistik kuvvetlerinin kantitatif değerlendirilmesi
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Date
1975
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Bursa Üniversitesi
Abstract
Biz bu çalışmada bir reseptör sistemi ile etki eden ilaçların etki güçlerinin kantitatif olarak değerlendirilmesini, model olarak aldığımız kalpteki beta 1 -adrenerjik reseptör sistemi üzerinde örneklemek istedik. Bu amaçla kalpte, kronotropik ve inotropik etki agonistlerle (isoprenaline ve adrenalin), kompetitif antagonistler varken ve yokken, doz-cevap eğrileri çizildi. Antagonistlerin (propranolol, alprenolol, LB-46 ve practolol) pA2 ve pA10 değerleri Arunlakshana ve Schiller'e göre hesaplanır. Antagonistlerin molar dozlarının algoritmalarına karşı, log (agonist doz oranı eski 1) değerli apsis-ordinat sisteminde işaretlendi. pA2 ve pA10, agonist doz ranını 2 ve 10 katı arttıran antagonist dozunun eksi logaritmasıdır. Maksimum etkinin % 50 sini meydana getiren agonist dozunun eksi logaritması olarak bilinen pD2 değerleri ise, agonistlerin kendi doz-cevap eğrilerinden hesaplandı.
In this study we have undertaken to give an example for the quantitative evaluation of agonistic and antagonistic activity of drugs on the cardiac adrenergic beta1 receptor system as a model. Dose-response curves for both the chronotropic and inotropic effects of agonists (Isoprenaline and Adrenaline) have been determined in the absence and presence of competitive antagonists (Propranolol, Alprenolol,LB-46 and Pactolol). pA2 and pA10 values of antagonists were calculated according to the method described by Arunlakshana and Schild (1959) Log (dose ratio of agonist minus 1) was plotted against the log of molar doses of antagonist. pA2 and pA10 are negative logarithms of the molar concentrations of the antagonist which increased the dose ratio 2- and 10-fold respectively. pD2 values of agonist calculated from its dose-response curve which is the negative logarithm of molar concentration of agonist produced 50 % effect of maximum.
In this study we have undertaken to give an example for the quantitative evaluation of agonistic and antagonistic activity of drugs on the cardiac adrenergic beta1 receptor system as a model. Dose-response curves for both the chronotropic and inotropic effects of agonists (Isoprenaline and Adrenaline) have been determined in the absence and presence of competitive antagonists (Propranolol, Alprenolol,LB-46 and Pactolol). pA2 and pA10 values of antagonists were calculated according to the method described by Arunlakshana and Schild (1959) Log (dose ratio of agonist minus 1) was plotted against the log of molar doses of antagonist. pA2 and pA10 are negative logarithms of the molar concentrations of the antagonist which increased the dose ratio 2- and 10-fold respectively. pD2 values of agonist calculated from its dose-response curve which is the negative logarithm of molar concentration of agonist produced 50 % effect of maximum.
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Keywords
Reseptör stimole, Bloke edici ilaçlar, Agonistik, Kantitatif değerlendirilmesi, Receptor stimole, Agonistic, Blocking drugs, Quantitative evaluation
Citation
Kıran, B. K. ve Ulus, İ. H. (1975). ''Reseptör stimole ve bloke edici ilaçların agonistik ve antagonistik kuvvetlerinin kantitatif değerlendirilmesi''. Bursa Tıp Fakültesi Dergisi, 2(3), 31-39.