Interaction of azimilide with neurohumoral and channel receptors.

  title={Interaction of azimilide with neurohumoral and channel receptors.},
  author={Robert R. Brooks and Schwe Fang Pong and Nicholas J. Izzo and Thomas John Moorehead and Murali Gopalakrishnan and David J. Triggle},
  journal={Biochemical pharmacology},
  volume={62 7},
Effects of azimilide on the muscarinic acetylcholine receptor-operated K+ current and experimental atrial fibrillation in guinea-pig hearts.
In isolated hearts, perfusion of CCh shortened the duration of the monophasic action potential (MAP) and effective refractory period (ERP) of the left atrium and lowered the atrial fibrillation threshold (AFT).
Influence of ketanserin on the effects of methylenedioxymethamphetamine on body temperature in the mouse.
Ketanserin modulates the hyperthermic actions of MDMA in mice and is consistent with α1 -adrenoceptor antagonism, although there is no clear evidence from this study that 5HT2-receptors mediate thehyperthermic response to MDMA.
Inhibitory effect of azimilide on Na+/Ca2+ exchange current in guinea-pig cardiac myocytes.
Azimilide attenuated I(NCX) in the presence of trypsin in the patch pipette, indicating that azimilide is aTrypsin-insensitive NCX inhibitor.
Pharmacological Properties and Functional Role of Kslow Current in Mouse Pancreatic β-Cells
The results strongly support a functional role for SK channel-mediated Kslow current in β-cells, and suggest that drugs that target SK channels may represent a new approach for increasing glucose-dependent insulin secretion.
New mechanisms and therapeutic potential of curcumin for colorectal cancer.
An update of the bioavailability and pharmacokinetics of curcumin is provided and the recently identified molecular pathways responsible of its anticancer potential in CRC are described.
Tail Current and Modulate Insulin Secretion
  • 2005


Interaction of the antiarrhythmic drug amiodarone with the muscarinic receptor in rat heart and brain.
The possible interaction between the muscarinic receptor and the antiarrythmic drug amiodarone was studied physiologically in the guinea pig ileum, as well as by competition binding experiments in
Muscarinic receptor heterogeneity revealed by interaction with bretylium tosylate. Different ligand-receptor conformations versus different receptor subclasses.
The interaction of the antiarrhythmic drug, bretylium tosylate, with the muscarinic receptor in tissue homogenates from regions of rat brain and heart and from submandibular gland and ileal wall was investigated, showing heterogeneous binding characteristics.
Pharmacologic and radioligand binding analysis of the actions of 1,4-dihydropyridine activator-antagonist pairs in smooth muscle.
The biphasic response to (-)- (S)-Bay K 8644 and (+)-(S)-202-791 suggests that the properties of Ca++ channel activation and antagonism may reside within a single 1,4-dihydropyridine molecule.
Characterization of binding of the Ca++ channel antagonist, [3H]nitrendipine, to guinea-pig ileal smooth muscle.
The data suggest that [3H]nitrendipine binding in smooth muscle is to a site which mediates the pharmacologic response, which is consistent with previous reports.
Voltage-dependent binding of 1,4-dihydropyridine Ca2+ channel antagonists and activators in cultured neonatal rat ventricular myocytes.
Binding of 1,4-dihydropyridine Ca2+ channel ligands was characterized as a function of membrane potential using saturation, competition, and kinetic measurements in cultured neonatal rat ventricular myocytes to derive KD values calculated from the ratio of k-1/k1 accorded well with those determined from equilibrium binding assays.
Antifibrillatory efficacy of concomitant beta adrenergic receptor blockade with dilevalol, the R,R-isomer of labetalol, and muscarinic receptor blockade with methylscopolamine.
The antiarrhythmic and antifibrillatory actions of dilevalol, the R,R-isomer of labetalol, were evaluated in conscious dogs 4 to 6 days after anterior myocardial infarction and methylscopolamine alone failed to suppress the development of ischemic ventricular fibrillation in 5 of 6 (83%) postinfarction dogs.