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Ennio Ongini - One of the best experts on this subject based on the ideXlab platform.
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synthesis of imidazo 1 2 c pyrazolo 4 3 e pyrimidines pyrazolo 4 3 e 1 2 4 triazolo 1 5 c pyrimidines and 1 2 4 triazolo 5 1 i purines new potent Adenosine A2 Receptor antagonists
European Journal of Medicinal Chemistry, 1993Co-Authors: Franco Gatta, M R Del Giudice, Anna Borioni, Pier Andrea Borea, Silvio Dionisotti, Ennio OnginiAbstract:Abstract A number of 2- or 4-fluorobenzylderivatives of imidazo[1,2-c]pyrazolo[4,3-e]pyrimidine, pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine and 1,2,4-triazolo[5,1-i] purine have been synthesized. The interaction with the Adenosine A2 and A1 Receptors was evaluated using selected biological assays. The highest degree of activity was displayed by the 5-amino-2-(2-furyl)-7-(or 8-)-fluorobenzyl-pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine 13e, f and 18e, f and -3-fluorobenzyl-1-2-4-triazolo[5,1-i] purines 19e, f. The compound 18f was found to be the most potent A2 antagonist in our series with a selectivity similar to that of the reference compound CGS 15943, but with 75-fold more activity in the platelet aggregation model.
Jon D. Levine - One of the best experts on this subject based on the ideXlab platform.
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modulation of bradykinin induced plasma extravasation in the rat knee joint by sympathetic co transmitters
Neuroscience, 1993Co-Authors: Paul Green, J Luo, Philip H Heller, Jon D. LevineAbstract:We describe the contribution of various sympathetic post-ganglionic neuron mediators to bradykinin-induced plasma extravasation in the knee joint of the rat. Co-perfusion of the sympathetic post-ganglionic neuron mediators, norepinephrine or neuropeptide Y with bradykinin resulted in diminished plasma extravasation. In contrast, the putative sympathetic post-ganglionic neuron mediators of bradykinin-induced plasma extravasation, namely prostaglandin E2, ATP, the selective Adenosine A2-Receptor agonist, CGS21680 or the endothelium-derived relaxing factor (as its precursor L-arginine) all greatly enhanced bradykinin-induced plasma extravasation, but produced little or no increase in plasma extravasation administered alone. The data show that sympathetic post-ganglionic neuron-derived mediators may either inhibit or enhance plasma extravasation induced by bradykinin, and we hypothesize that differential release of mediators from the sympathetic post-ganglionic neuron terminal, in response to varying stimuli, regulates local plasma extravasation during inflammation.
Franco Gatta - One of the best experts on this subject based on the ideXlab platform.
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synthesis of imidazo 1 2 c pyrazolo 4 3 e pyrimidines pyrazolo 4 3 e 1 2 4 triazolo 1 5 c pyrimidines and 1 2 4 triazolo 5 1 i purines new potent Adenosine A2 Receptor antagonists
European Journal of Medicinal Chemistry, 1993Co-Authors: Franco Gatta, M R Del Giudice, Anna Borioni, Pier Andrea Borea, Silvio Dionisotti, Ennio OnginiAbstract:Abstract A number of 2- or 4-fluorobenzylderivatives of imidazo[1,2-c]pyrazolo[4,3-e]pyrimidine, pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine and 1,2,4-triazolo[5,1-i] purine have been synthesized. The interaction with the Adenosine A2 and A1 Receptors was evaluated using selected biological assays. The highest degree of activity was displayed by the 5-amino-2-(2-furyl)-7-(or 8-)-fluorobenzyl-pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine 13e, f and 18e, f and -3-fluorobenzyl-1-2-4-triazolo[5,1-i] purines 19e, f. The compound 18f was found to be the most potent A2 antagonist in our series with a selectivity similar to that of the reference compound CGS 15943, but with 75-fold more activity in the platelet aggregation model.
Paul Green - One of the best experts on this subject based on the ideXlab platform.
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modulation of bradykinin induced plasma extravasation in the rat knee joint by sympathetic co transmitters
Neuroscience, 1993Co-Authors: Paul Green, J Luo, Philip H Heller, Jon D. LevineAbstract:We describe the contribution of various sympathetic post-ganglionic neuron mediators to bradykinin-induced plasma extravasation in the knee joint of the rat. Co-perfusion of the sympathetic post-ganglionic neuron mediators, norepinephrine or neuropeptide Y with bradykinin resulted in diminished plasma extravasation. In contrast, the putative sympathetic post-ganglionic neuron mediators of bradykinin-induced plasma extravasation, namely prostaglandin E2, ATP, the selective Adenosine A2-Receptor agonist, CGS21680 or the endothelium-derived relaxing factor (as its precursor L-arginine) all greatly enhanced bradykinin-induced plasma extravasation, but produced little or no increase in plasma extravasation administered alone. The data show that sympathetic post-ganglionic neuron-derived mediators may either inhibit or enhance plasma extravasation induced by bradykinin, and we hypothesize that differential release of mediators from the sympathetic post-ganglionic neuron terminal, in response to varying stimuli, regulates local plasma extravasation during inflammation.
M R Del Giudice - One of the best experts on this subject based on the ideXlab platform.
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synthesis of imidazo 1 2 c pyrazolo 4 3 e pyrimidines pyrazolo 4 3 e 1 2 4 triazolo 1 5 c pyrimidines and 1 2 4 triazolo 5 1 i purines new potent Adenosine A2 Receptor antagonists
European Journal of Medicinal Chemistry, 1993Co-Authors: Franco Gatta, M R Del Giudice, Anna Borioni, Pier Andrea Borea, Silvio Dionisotti, Ennio OnginiAbstract:Abstract A number of 2- or 4-fluorobenzylderivatives of imidazo[1,2-c]pyrazolo[4,3-e]pyrimidine, pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine and 1,2,4-triazolo[5,1-i] purine have been synthesized. The interaction with the Adenosine A2 and A1 Receptors was evaluated using selected biological assays. The highest degree of activity was displayed by the 5-amino-2-(2-furyl)-7-(or 8-)-fluorobenzyl-pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine 13e, f and 18e, f and -3-fluorobenzyl-1-2-4-triazolo[5,1-i] purines 19e, f. The compound 18f was found to be the most potent A2 antagonist in our series with a selectivity similar to that of the reference compound CGS 15943, but with 75-fold more activity in the platelet aggregation model.