The Experts below are selected from a list of 36 Experts worldwide ranked by ideXlab platform
Aron Jurkiewicz - One of the best experts on this subject based on the ideXlab platform.
-
effects of Indoramin in rat vas deferens and aorta concomitant α1 adrenoceptor and neuronal uptake blockade
British Journal of Pharmacology, 1999Co-Authors: Andre S Pupo, Daniela L C Cavenaghi, Marcelo Campos, Paola De Lucena Morais, Neide H Jurkiewicz, Aron JurkiewiczAbstract:1 The actions of the a1-adrenoceptor antagonist Indoramin have been examined against the contractions induced by noradrenaline in the rat vas deferens and aorta taking into account a putative neuronal uptake blocking activity of this antagonist which could result in self-cancelling actions. 2 Indoramin behaved as a simple competitive antagonist of the contractions induced by noradrenaline in the vas deferens and aorta yielding pA2 values of 7.38+0.05 (slope=0.98+0.03) and 6.78+0.14 (slope=1.08+0.06), respectively. 3 When the experiments were repeated in the presence of cocaine (6 mM) the potency (pA2 )o f Indoramin in antagonizing the contractions of the vas deferens to noradrenaline was increased to 8.72+0.07 (slope=1.10+0.05) while its potency remained unchanged in the aorta (pA2=6.69+0.12; slope=1.04+0.05). 4 In denervated vas deferens, Indoramin antagonized the contractions to noradrenaline with a potency similar to that found in the presence of cocaine (8.79+0.07; slope=1.09+0.06). 5 It is suggested that Indoramin blocks a1-adrenoceptors and neuronal uptake in rat vas deferens resulting in Schild plots with slopes not diAerent from unity even in the absence of selective inhibition of neuronal uptake. As a major consequence of this double mechanism of action, the pA2 values for this antagonist are underestimated when calculated in situations where the neuronal uptake is active, yielding spurious pKB values.
Andre S Pupo - One of the best experts on this subject based on the ideXlab platform.
-
effects of Indoramin in rat vas deferens and aorta concomitant α1 adrenoceptor and neuronal uptake blockade
British Journal of Pharmacology, 1999Co-Authors: Andre S Pupo, Daniela L C Cavenaghi, Marcelo Campos, Paola De Lucena Morais, Neide H Jurkiewicz, Aron JurkiewiczAbstract:1 The actions of the a1-adrenoceptor antagonist Indoramin have been examined against the contractions induced by noradrenaline in the rat vas deferens and aorta taking into account a putative neuronal uptake blocking activity of this antagonist which could result in self-cancelling actions. 2 Indoramin behaved as a simple competitive antagonist of the contractions induced by noradrenaline in the vas deferens and aorta yielding pA2 values of 7.38+0.05 (slope=0.98+0.03) and 6.78+0.14 (slope=1.08+0.06), respectively. 3 When the experiments were repeated in the presence of cocaine (6 mM) the potency (pA2 )o f Indoramin in antagonizing the contractions of the vas deferens to noradrenaline was increased to 8.72+0.07 (slope=1.10+0.05) while its potency remained unchanged in the aorta (pA2=6.69+0.12; slope=1.04+0.05). 4 In denervated vas deferens, Indoramin antagonized the contractions to noradrenaline with a potency similar to that found in the presence of cocaine (8.79+0.07; slope=1.09+0.06). 5 It is suggested that Indoramin blocks a1-adrenoceptors and neuronal uptake in rat vas deferens resulting in Schild plots with slopes not diAerent from unity even in the absence of selective inhibition of neuronal uptake. As a major consequence of this double mechanism of action, the pA2 values for this antagonist are underestimated when calculated in situations where the neuronal uptake is active, yielding spurious pKB values.
Daniela L C Cavenaghi - One of the best experts on this subject based on the ideXlab platform.
-
effects of Indoramin in rat vas deferens and aorta concomitant α1 adrenoceptor and neuronal uptake blockade
British Journal of Pharmacology, 1999Co-Authors: Andre S Pupo, Daniela L C Cavenaghi, Marcelo Campos, Paola De Lucena Morais, Neide H Jurkiewicz, Aron JurkiewiczAbstract:1 The actions of the a1-adrenoceptor antagonist Indoramin have been examined against the contractions induced by noradrenaline in the rat vas deferens and aorta taking into account a putative neuronal uptake blocking activity of this antagonist which could result in self-cancelling actions. 2 Indoramin behaved as a simple competitive antagonist of the contractions induced by noradrenaline in the vas deferens and aorta yielding pA2 values of 7.38+0.05 (slope=0.98+0.03) and 6.78+0.14 (slope=1.08+0.06), respectively. 3 When the experiments were repeated in the presence of cocaine (6 mM) the potency (pA2 )o f Indoramin in antagonizing the contractions of the vas deferens to noradrenaline was increased to 8.72+0.07 (slope=1.10+0.05) while its potency remained unchanged in the aorta (pA2=6.69+0.12; slope=1.04+0.05). 4 In denervated vas deferens, Indoramin antagonized the contractions to noradrenaline with a potency similar to that found in the presence of cocaine (8.79+0.07; slope=1.09+0.06). 5 It is suggested that Indoramin blocks a1-adrenoceptors and neuronal uptake in rat vas deferens resulting in Schild plots with slopes not diAerent from unity even in the absence of selective inhibition of neuronal uptake. As a major consequence of this double mechanism of action, the pA2 values for this antagonist are underestimated when calculated in situations where the neuronal uptake is active, yielding spurious pKB values.
-
Effects of Indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
'Springer Science and Business Media LLC', 1999Co-Authors: Pupo A. S., Daniela L C Cavenaghi, Morais P. D., Campos Marcelo, Jurkiewicz, Neide Hyppolito, Jurkiewicz AronAbstract:1 the actions of the alpha(1)-adrenoceptor antagonist Indoramin have been examined against the contractions induced by noradrenaline in the rat vas deferens and aorta taking into account a putative neuronal uptake blocking activity of this antagonist which could. result in self-cancelling actions.2 Indoramin behaved as a simple competitive antagonist of the contractions induced by noradrenaline in the vas deferens and aorta yielding pA(2) values of 7.38 +/- 0.05 (slope = 0.98 +/- 0.03) and 6.78 +/- 0.14 (slope = 1.08 +/- 0.06), respectively.3 When the experiments were repeated in the presence of cocaine (6 mu M) the potency (pA(2)) of Indoramin in antagonizing the contractions of the vas deferens to noradrenaline was increased to 8.72 +/- 0.07 (slope = 1.10 +/- 0.05) while its potency remained unchanged in the aorta (pA(2) = 6.69 +/- 0.12; slope = 1.04 +/- 0.05).4 in denervated vas deferens, Indoramin antagonized the contractions to noradrenaline with a potency similar to that found in the presence of cocaine (8.79 +/- 0.07; slope = 1.09 +/- 0.06).5 It is suggested that Indoramin blocks alpha(1)-adrenoceptors and neuronal uptake in rat vas deferens resulting in Schild plots with slopes not different from unity even in the absence of selective inhibition of neuronal uptake. As a major consequence of this double mechanism of action, the pA(2) values for this antagonist are underestimated when calculated in situations where the neuronal uptake is active, yielding spurious pK(B) values.UNESP, Inst Biociencias, Dept Pharmacol, BR-18600000 Botucatu, SP, BrazilUNIFESP, Escola Paulista Med, Dept Pharmacol, BR-0403406 São Paulo, BrazilUNIFESP, Escola Paulista Med, Dept Pharmacol, BR-0403406 São Paulo, BrazilWeb of Scienc
Paola De Lucena Morais - One of the best experts on this subject based on the ideXlab platform.
-
effects of Indoramin in rat vas deferens and aorta concomitant α1 adrenoceptor and neuronal uptake blockade
British Journal of Pharmacology, 1999Co-Authors: Andre S Pupo, Daniela L C Cavenaghi, Marcelo Campos, Paola De Lucena Morais, Neide H Jurkiewicz, Aron JurkiewiczAbstract:1 The actions of the a1-adrenoceptor antagonist Indoramin have been examined against the contractions induced by noradrenaline in the rat vas deferens and aorta taking into account a putative neuronal uptake blocking activity of this antagonist which could result in self-cancelling actions. 2 Indoramin behaved as a simple competitive antagonist of the contractions induced by noradrenaline in the vas deferens and aorta yielding pA2 values of 7.38+0.05 (slope=0.98+0.03) and 6.78+0.14 (slope=1.08+0.06), respectively. 3 When the experiments were repeated in the presence of cocaine (6 mM) the potency (pA2 )o f Indoramin in antagonizing the contractions of the vas deferens to noradrenaline was increased to 8.72+0.07 (slope=1.10+0.05) while its potency remained unchanged in the aorta (pA2=6.69+0.12; slope=1.04+0.05). 4 In denervated vas deferens, Indoramin antagonized the contractions to noradrenaline with a potency similar to that found in the presence of cocaine (8.79+0.07; slope=1.09+0.06). 5 It is suggested that Indoramin blocks a1-adrenoceptors and neuronal uptake in rat vas deferens resulting in Schild plots with slopes not diAerent from unity even in the absence of selective inhibition of neuronal uptake. As a major consequence of this double mechanism of action, the pA2 values for this antagonist are underestimated when calculated in situations where the neuronal uptake is active, yielding spurious pKB values.
Marcelo Campos - One of the best experts on this subject based on the ideXlab platform.
-
effects of Indoramin in rat vas deferens and aorta concomitant α1 adrenoceptor and neuronal uptake blockade
British Journal of Pharmacology, 1999Co-Authors: Andre S Pupo, Daniela L C Cavenaghi, Marcelo Campos, Paola De Lucena Morais, Neide H Jurkiewicz, Aron JurkiewiczAbstract:1 The actions of the a1-adrenoceptor antagonist Indoramin have been examined against the contractions induced by noradrenaline in the rat vas deferens and aorta taking into account a putative neuronal uptake blocking activity of this antagonist which could result in self-cancelling actions. 2 Indoramin behaved as a simple competitive antagonist of the contractions induced by noradrenaline in the vas deferens and aorta yielding pA2 values of 7.38+0.05 (slope=0.98+0.03) and 6.78+0.14 (slope=1.08+0.06), respectively. 3 When the experiments were repeated in the presence of cocaine (6 mM) the potency (pA2 )o f Indoramin in antagonizing the contractions of the vas deferens to noradrenaline was increased to 8.72+0.07 (slope=1.10+0.05) while its potency remained unchanged in the aorta (pA2=6.69+0.12; slope=1.04+0.05). 4 In denervated vas deferens, Indoramin antagonized the contractions to noradrenaline with a potency similar to that found in the presence of cocaine (8.79+0.07; slope=1.09+0.06). 5 It is suggested that Indoramin blocks a1-adrenoceptors and neuronal uptake in rat vas deferens resulting in Schild plots with slopes not diAerent from unity even in the absence of selective inhibition of neuronal uptake. As a major consequence of this double mechanism of action, the pA2 values for this antagonist are underestimated when calculated in situations where the neuronal uptake is active, yielding spurious pKB values.