British Journal of Pharmacology

Cover image for Vol. 174 Issue 9

Editor-in-Chief: A. Ahluwalia

Impact Factor: 5.259

ISI Journal Citation Reports © Ranking: 2015: 17/255 (Pharmacology & Pharmacy)

Online ISSN: 1476-5381

Associated Title(s): British Journal of Clinical Pharmacology, Pharmacology Research & Perspectives

Editors' Choice - Volume 174, Issue 6

  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    Outline of the experimental protocols. Experimental Series 1. Hearts were perfused with an activator of both PKA and Epac (8-Br, 5 μM), an inhibitor of PKA (H-89) and Epac (ESI-09). Groups of hearts: Control, 8-Br, 8-Br + H-89 and 8-Br + ESI-09. Experimental Series 2. Hearts were perfused with 8-Br (10 μM), a PKC inhibitor chelerythrine (Chel) and a specific PKA inhibitor peptide PKI. Groups of hearts: Control, 8-Br, 8-Br + PKI and 8-Br + Chel. Experimental Series 3. Hearts were perfused with a PKA activator (6-Bnz) and an Epac activator (CPT). Groups of hearts: Control, 6-Bnz, CPT and 6-Bnz + CPT.

  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    The effect of cAMP analogues on RPP of rat isolated Langendorff-perfused hearts. The data are presented as percentage of pretreatment values calculated for each heart. Panel A – Changes in RPP induced by heart perfusion with 8-Br (5 μM) alone or in the presence of 1 μM ESI-09 or 10 μM H-89. Groups of hearts: 8-Br, n = 7; 8-Br + ESI-09, n = 7; 8-Br + H-89, n = 6. *P < 0.05, significant effect of inhibitor (H-89 or ESI-09). Panel B – Changes of RPP induced by heart perfusion with 8-Br (10 μM) alone or in the presence of 3 μM PKI. Groups of hearts: 8-Br, n = 7; PKI, n = 5; 8-Br + PKI, n = 5. Panel C – Changes of RPP induced by the heart perfusion with 6-Bnz (10 μM) and CPT (10 μM) alone or in combination. Groups of hearts: 6-Bnz, n = 5; CPT, n = 5; 6-Bnz + CPT, n = 6. *P < 0.05, significantly different from the combination of 6-Bnz and CPT.

  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    The effect of 8-Br on translocation of PKCδ and PKCε from the cytosol to membrane fraction. PKC translocation, reflecting its activation, was assessed by Western blots and expressed as a ratio of the optical density of the membrane-to-cytosol fraction. Groups of hearts: control, n = 6; 8-Br, n = 6. Panel A – 8-Br (5 μM) had no effect on PKCδ translocation. Panel B – 8-Br (5 μM) promoted PKCε translocation. *P < 0.05, significantly different from control.

  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    The effect of 8-Br with or without ESI-09, H-89 and PKI on RPP recovery after I/R. For clarity, RPP is expressed as percentage of the initial value measured at the end of equilibration period prior to any intervention. Panel A – Groups of hearts: Control, n = 7; 8-Br, n = 7; ESI-09, n = 7; 8-Br + ESI-09, n = 7; 8-Br + H-89, n = 6. Pretreatment of hearts with 8-Br (5 μM) fully restored RPP after 30 min global ischaemia and 60 min reperfusion, but ESI-09 (1 μM) and H-89 (10 μM) abolished this effect. Perfusion of hearts with ESI-09 alone had no effect on the RPP recovery. Panel B – Groups of hearts: Control, n = 7; 8-Br, n = 7; PKI, n = 5; 8-Br + PKI, n = 5. Pretreatment of hearts with 8-Br (10 μM, n = 7) fully restored RPP, but PKI (3 μM, n = 5) inhibited this effect. Perfusion of hearts with PKI alone had no effect on the RPP recovery. *P < 0.05, significantly different from control; #P < 0.05, significantly different from 8-Br.

  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    The effect of 8-Br with or without ESI-09 and H-89 on cardiac injury following I/R. Groups of hearts: Control, n = 7; 8-Br, n = 7; ESI-09, n = 7; 8-Br + ESI-09, n = 7; 8-Br + H-89, n = 6. Panel A – Activity of LDH in the effluent perfusate was reduced by pretreatment of hearts with 8-Br (5 μM), but ESI-09 (1 μM) and H-89 (10 μM) abolished this effect. Insert – Mean area under the curve reflecting the total release of LDH. The column-fills in the insert correspond to the column-fills in Panel B. Panel B – Infarct size was calculated as percentage of the whole heart area. Infarct size during reperfusion was reduced by pretreatment of hearts with 8-Br (5 μM), but ESI-09 (1 μM) and H-89 (10 μM) abolished this effect. ESI-09 alone had no effect on cardiac injury. Representative heart slices with infarcted myocardium (pale white area) are shown under the corresponding columns. *P < 0.05, significantly different from control.

  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    The effect of 8-Br with or without PKI on cardiac injury following I/R. Groups of hearts: Control, n = 7; 8-Br, n = 7; PKI, n = 5; 8-Br + PKI, n = 5. Panel A – LDH activity in the effluent perfusate was reduced by pretreatment of hearts with 8-Br (10 μM) during reperfusion, but PKI (3 μM) inhibited this effect. Insert – Mean area under the curve reflecting the total release of LDH. The column-fills in the insert correspond to the column-fills in Panel B. Panel B – Infarct size was calculated as percentage of the whole heart area. Infarct size was significantly reduced by 8-Br (10 μM), but PKI (3 μM) inhibited this effect. PKI alone had no effect on cardiac injury. Representative heart slices with infarcted myocardium (pale white area) are shown under the corresponding columns. *P < 0.05, significantly different from control (n = 7); # P < 0.05, significantly different from 8-Br.

  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    The effect of 6-Bnz or CPT on RPP recovery and cardiac injury following I/R. Groups of hearts: Control, n = 7; 6-Bnz + CPT, n = 6; CPT, n = 5; 6-Bnz, n = 5. Panel A – RPP is expressed as percentage of the initial value measured at the end of equilibration period prior to any intervention. Neither 6-Bnz (10 μM) nor CPT (10 μM) had any effect on RPP recovery after 30 min ischaemia and 60 min of reperfusion, but the mixture of 6-Bnz and CPT significantly improved the recovery. Panel B – LDH activity in the effluent perfusate was reduced by pretreatment of hearts with 6-Bnz (10 μM) starting from 15 min of reperfusion; pretreatment of hearts with CPT (10 μM) had no effect, but the mixture of 6-Bnz and CPT significantly reduced LDH activity starting from the beginning of reperfusion. Insert – Mean area under the curve reflecting the total release of LDH. The column-fills in the insert correspond to the column-fills in Panels A and C. Panel C – Infarct size was calculated as percentage of the whole heart area. Neither 6-Bnz nor CPT alone reduced infarct size whilst the mixture of 6-Bnz and CPT significantly reduced infarct size. Representative heart slices with infarcted myocardium (pale white area) are shown under the corresponding columns. *P < 0.05, 6-Bnz + CPT significantly different from control; #P < 0.05, 6-Bnz significantly different from control.

  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

    The effect of 8-Br and chelerythrine (Chel) on cardiac injury following I/R. Cardiac injury was assessed by measuring LDH activity and infarct size. Groups of hearts: Control, n = 7; 8-Br, n = 7; 8-Br + Chel, n = 5. Panel A – 8-Br (10 μM) reduced LDH activity in the effluent perfusate during reperfusion, but chelerythrine (10 μM) reversed this effect. Panel B – 8-Br (10 μM) significantly reduced infarct size during reperfusion, but chelerythrine (10 μM) attenuated this effect. *P < 0.05, significantly different from control; #P < 0.05, significantly different from 8-Br.

  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac
  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac
  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac
  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac
  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac
  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac
  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac
  • Functional and cardioprotective effects of simultaneous and individual activation of protein kinase A and Epac

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