Study of β-adrenoreceptor antagonistic activity of DPJ 904 in rats

K. Nandakumar, S. K. Bansal, Randhir Singh, A. J. Mohite, S. L. Bodhankar, D. P. Jindal, Mohane S. Coumar, R. Balaraman, S. H. Bhardwaj

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Abstract

β-Adrenoreceptor antagonistic activity of a newly synthesized compound was evaluated in vivo by measuring the mean arterial blood pressure and heart rate of urethane-anesthetized rats treated with isoprenaline. In vitro β1-, β2- and β3-antagonism was studied using isolated rat right atria, isolated rat uterus and isolated rat colon preparations, respectively, in comparison to isoprenaline response. DPJ 904 (1,3 and 10 mg/kg, i.v.) produced dose-dependent hypotensive and bradycardia response in anesthetized rat. DPJ 904 (1, 3 and 10 mg/kg, i.v.) significantly inhibited both the tachycardial effects and hypotensive response induced by isoprenaline. DPJ 904-antagonized isoprenaline induced positive chronotropic effects of isolated rat right atria and a uterine relaxant effect indicating β1- and β2-blockade. The parallel shift to the right of the concentration-response curve of isoprenaline in the presence of DPJ 904 in KCI (30 mmol/l) induced contraction of the rat colon suggesting that DPJ 904 also possessed β3-adrenoreceptor antagonistic activity. The selectivity to β1-adrenoreceptor was nearly 20.5 times greater than to β2-adrenoreceptor. The present study indicates that DPJ 904 possesses β-adrenoreceptor antagonistic activity with slightly more affinity to the β1-adrenoreceptor subtype.

Original languageEnglish
Pages (from-to)1-5
Number of pages5
JournalPharmacology
Volume74
Issue number1
DOIs
Publication statusPublished - 01-04-2005

All Science Journal Classification (ASJC) codes

  • Pharmacology

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    Nandakumar, K., Bansal, S. K., Singh, R., Mohite, A. J., Bodhankar, S. L., Jindal, D. P., Coumar, M. S., Balaraman, R., & Bhardwaj, S. H. (2005). Study of β-adrenoreceptor antagonistic activity of DPJ 904 in rats. Pharmacology, 74(1), 1-5. https://doi.org/10.1159/000082861