Drugs online research references
J Anal Toxicol. 1990 Mar-Apr;14(2):132-6.
Use of cyclic boronates for GC/MS screening and quantitation of beta-adrenergic blockers and some bronchodilators.
Zamecnik J.
Health and Welfare Canada, Bureau of Drug Research, Ottawa, Ontario.
Gas chromatographic and mass spectrometric properties of cyclic methyl and n-butyl boronates of 13 beta blockers and bronchodilators were investigated for potential use in screening and quantitation in biological materials of interest. The tested compounds included acebutolol, atenolol, labetalol, levobunolol, metoprolol, nadolol, oxprenolol, pindolol, propranolol, sotalol, albuterol, and isoproterenol. The cyclic methyl boronates were superior in gas chromatographic properties to the corresponding n-butylboronates of these compounds. Higher weights of fragments obtained with n-butyl boronation may be advantageous for analyses of complex biological matrices. Mass spectra and retention times relative to SKF-525A are provided.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1969974&dopt=Abstract
Cardiovasc Res. 1986 Sep;20(9):637-44.
Effects of beta blocking agents on the density of beta adrenoceptors and adenylate cyclase response in human myocardium: intrinsic sympathomimetic activity favours receptor upregulation.
Golf S, Hansson V.
The density of beta adrenoceptors, the relative number of beta 1 and beta 2 adrenoceptor subtypes, and adenylate cyclase activity were studied in preparations from atrial biopsy specimens of 32 patients with coronary heart disease. Six patients were not receiving beta blocking agents, whereas the others were treated with different beta blocking drugs (timolol, propranolol, pindolol, metoprolol, and atenolol). Clinical and haemodynamic variables were similar in the different groups of patients. Beta adrenoceptor density was 17% significantly lower in the non-treated group than in the groups treated with beta blocking drugs. Among these, the group treated with pindolol, a drug with intrinsic sympathomimetic activity, had receptor densities that were 38% significantly higher than those treated with other beta blocking drugs and 51% significantly higher than the non-treated group. The relative numbers of beta 1 and beta 2 adrenoceptor subtypes were very similar in the different groups (beta 1 receptors 75-80%, beta 2 receptors 20-25%). A significant increase in the ratios of terbutaline stimulated to basal and terbutaline stimulated to isoproterenol stimulated adenylate cyclase activities was found in patients treated with beta 1 selective blockers (metoprolol, atenolol), indicating that beta 1 selective drugs may improve beta 2 receptor-adenylate cyclase coupling. In contrast, pindolol caused a significant reduction in the ratio of terbutaline stimulated to isoproterenol stimulated adenylate cyclase activity, indicating that this drug may cause a reduction in beta 2 receptor-adenylate cyclase coupling efficacy. Thus treatment with beta blocking agents causes upregulation of human myocardial beta receptor density. Intrinsic sympathomimetic activity seems to favour receptor upregulation.(ABSTRACT TRUNCATED AT 250 WORDS)
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2878724&dopt=Abstract
Biochem Biophys Res Commun. 1987 Jul 31;146(2):889-97.
The effect of epidermal growth factor on chronotropic response in cardiac cells in culture.
Rabkin SW, Sunga P, Myrdal S.
Cardiac chronotropic response to epidermal growth factor (EGF) was assessed in chick embryonic ventricular cell aggregates. EGF at a concentration of 10 ug/mL but not at 5 ug/mL produced a significant (p less than 0.05) increase in cardiac beating rate. This was evident within 10 min, reached a peak at about 15 min and remained at that level for 1.5 hr or the rest of the observation period. The effect of EGF on cardiac automaticity was reduced but not abolished at a lower temperature (22oC) that is known to decrease the affinity of the EGF receptor and reduce the internalization of EGF. Hypothermia did not change the maximum increase in heart rate response from isoproterenol although it altered the pattern of the response. Beta adrenoreceptor blockade with metoprolol only slightly altered the response to EGF. These data indicate that EGF produces functional effects on the heart that may be mediated through EGF receptor linked mechanisms.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3497635&dopt=Abstract
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