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Norepinephrine elicits beta2-receptor-mediated dilation of isolated human coronary arterioles.
Circulation
July 2002
Department of Physiology, New York Medical College, Valhalla 10595, USA.
Background: The exact role of adrenoceptors in norepinephrine (NE)-mediated regulation of the human coronary circulation has yet to be elucidated. Thus, the goals of this study were to characterize the adrenoceptors involved in the responses to NE in isolated human coronary arterioles and small arteries.
Methods And Results: Arterioles (n=39) and small arteries from the left ventricle of explanted human hearts were isolated and cannulated.
Investigation of the metabolism of 14C/13C-practolol in rat using directly coupled radio-HPLC-NMR-MS.
Xenobiotica
July 2000
Biological Chemistry, Biomedical Sciences Division, Imperial College of Science, Technology and Medicine, South Kensington, London, UK.
1. The metabolic fate of 14C/13C-practolol was investigated using on-line HPLC-NMR-MS following oral administration to rat. The major route of elimination for the radiolabel was via the urine with the principal biotransformation products confirmed as the 2-hydroxy- and 2-hydroxyglucronide metabolites.
View Article and Find Full Text PDFPharmacodynamic models of various beta blockers: an explanation for the long duration of action of bopindolol.
J Cardiovasc Pharmacol
August 1987
Models describing the time course of effects (pharmacodynamic models) of various beta blockers in man are used to explain the long duration of action of bopindolol. No matter what effect is used [reduction in exercise heart rate (RER) or isoproterenol dose ratio (DR)] human data show clearly that bopindolol is very potent compared to other beta blockers such as atenolol, metoprolol, pindolol, practolol, and propranolol. In pharmacokinetic terms, however, these drugs show no pronounced difference in their elimination half-life (ranging between 4 and 8 h).
View Article and Find Full Text PDFCharacterization of beta-adrenoceptors mediating relaxation of the guinea-pig ileum.
J Pharm Pharmacol
September 1984
Relaxation responses to sympathomimetic amines were recorded in potassium-contracted segments of guinea-pig ileum. Experiments were performed in the presence of phentolamine (5 X 10(-6) M) to eliminate beta-adrenoceptor-mediated effects. Metanephrine (10(-5) M) and desmethylimipramine (5 X 10(-7) M) were also present to prevent extraneuronal and neuronal uptake respectively.
View Article and Find Full Text PDFIn two series of antiarrhythmic drugs tested, as the octanol/water partition coefficient increases so do the following: elimination from the body by biotransformation, first-pass biotransformation in the liver and gastrointestinal tract after oral administration, protein binding to some extent, and penetration into brain tissue. Patients receiving lipophilic beta-adrenoreceptor blocking drugs may experience more central nervous system side effects than those receiving hydrophilic beta blockers. Structural modification of a drug, guided by the concept of bioisosterism, may allow the disassociation of therapeutic from toxic activities.
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