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ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF NEW ANALOGUES OF HC-030031: A TRPA1 CHANNEL ANTAGONIST

100%
Bryła A., Ślusarczyk M., Zygmunt M., Chłoń-Rzepa G., Kazek G.
Acta Poloniae Pharmaceutica - Drug Research
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2020
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vol. 77
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issue 1
113-119
EN
One of our study direction is research in the group of compounds affecting the TRPA1 ion channel which can perform an important function in pain (including neuropathic pain) and inflammation for example in asthma and other chronic respiratory diseases. The aim of this study was to evaluate the analgesic and anti-inflammatory activity of two analogues of HC-030031 analogues belonging to nitrogen derivatives of heterocyclic system: xanthine (cmpd 1) and benzimidazole (cmpd 2) with hydrazide and amide moieties respectively In this paper, for two derivatives (cmpd 1 and cmpd 2) potential analgesic and anti-inflammatory/anti-edematous activities were evaluated in animal models of pain in mice (writhing response test, formalin test) and inflammation in rats (carrageenan-induced paw edema test). Both the tested compounds 1 and 2 showed a significant analgesic and anti-inflammatory activity.
2
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ANTIARRHYTHMIC AND HYPOTENSIVE ACTIVITY OF NEW ANALOGUES OF THEOPHYLLINE

73%
Sapa J., Zygmunt M., Krawczyk Ł., Dudek M., Bednarski M., Nowiński L., Knutelska J., Chłoń-Rzepa G., Pawłowski M.
Medicina Internacia Revuo
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2013
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vol. 25
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issue 100
128-135
EN
On the basis of our earlier studies in the group of 7,8-disubstituted derivatives of 1,3-dimetyl-3,7-dihydro-purine-2,6-dione, some new derivatives of theophylline were synthesized and tested for their electrocardiographic, antiarrhythmic and hypotensive activity as well as for α1-adrenoreceptor affinities. The performed preliminary tests indicated that new compounds did not significantly affect the normal ECG in vivo. As the result of present studies it may be concluded that all compounds did not possess hypotensive and arrhythmic activity. The results of the binding assays on α1-adrenergic receptors showed, that these derivatives display no affinity for α1-adrenergic receptors. Lack of antiarrhythmic and antihypertensive activity may result from the absence of affinity for the α1-adrenergic receptor. Performed chemical modifications lead to the loss of pharmacological activity previously observed among other derivatives in this group. Generally in comparison with the previously reported derivatives, replacing the phenoxyethylpiperazine by other moiety, changed the antiarrhythmic and hypotensive activity.
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