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Chemical Compound Review

Alfeprol     1-(propan-2-ylamino)-3-(2- prop-2...

Synonyms: Apllobal, Gubernal, Regletin, Alpheprol, Aptine, ...
 
 
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Disease relevance of alprenolol

  • Effect of alprenolol on mortality among patients with definite or suspected acute myocardial infarction. Preliminary results [1].
  • Influence of alprenolol on hemodynamic and metabolic responses to prolonged exercise in subjects with hypertension [2].
  • The plasma concentrations of alprenolol and its metabolite 4-hydroxy-alprenolol and the inhibition of exercise tachycardia were studied for 7 hr after the alprenolol [3].
  • Depolarised and diseased myocardium is more sensitive to alprenolol and the drug's membrane depressant actions may be significant in terminating arrhythmias in such tissue [4].
  • The effects of IPC on calpain, alpha-fodrin, and LDH release were blunted by the application of the PKA inhibitor H89 or alprenolol during IPC, while transient stimulation of PKA with CPT-cAMP or isoproterenol before ischemia attenuated calpain activation, alpha-fodrin degradation, and markedly reduced LDH release (P<0.001) [5].
 

High impact information on alprenolol

 

Chemical compound and disease context of alprenolol

 

Biological context of alprenolol

 

Anatomical context of alprenolol

  • Identification of beta-adrenergic receptors in human lymphocytes by (-) (3H) alprenolol binding [6].
  • As an additional control, pooled inguinal adipose tissue from adult male Sprague-Dawley rats was incubated with the same concentrations of alprenolol [20].
  • A compound from another synthesis was shown be to effective in displacing specific [125I]iodocyanopindolol binding from neonatal rat cardiac myocyte membranes, with a dissociation constant of 13.8 nM, whereas native alprenolol had a dissociation constant of 1.3 nM [21].
  • Electrophysiological effects of alprenolol on depressed canine myocardium [4].
  • Fat cells from hypo- and hyperthyroid rats showed the same affinity (K = 1.4 X 10(10) M(-1) and binding capacity (N = 1.21 X 10(-13) mol/microgram DNA) toward alprenolol as those from normal animals [22].
 

Associations of alprenolol with other chemical compounds

 

Gene context of alprenolol

 

Analytical, diagnostic and therapeutic context of alprenolol

References

  1. Effect of alprenolol on mortality among patients with definite or suspected acute myocardial infarction. Preliminary results. Andersen, M.P., Bechsgaard, P., Frederiksen, J., Hansen, D.A., Jürgensen, H.J., Nielsen, B., Pedersen, F., Pedersen-Bjergaard, O., Rasmussen, S.L. Lancet (1979) [Pubmed]
  2. Influence of alprenolol on hemodynamic and metabolic responses to prolonged exercise in subjects with hypertension. Frisk-Holmberg, M., Jorfeldt, L., Juhlin-Dannfeldt, A. Clin. Pharmacol. Ther. (1977) [Pubmed]
  3. Influence of pentobarbital on effect and plasma levels of alprenolol and 4-hydroxy-alprenolol. Collste, P., Seideman, P., Borg, K.O., Haglund, K., von Bahr, C. Clin. Pharmacol. Ther. (1979) [Pubmed]
  4. Electrophysiological effects of alprenolol on depressed canine myocardium. Guse, P.A., Gaide, M.S., Myerburg, R.J., Epstein, K., Gelband, H., Bassett, A.L. Cardiovasc. Res. (1980) [Pubmed]
  5. Ischemic preconditioning attenuates calpain-mediated degradation of structural proteins through a protein kinase A-dependent mechanism. Inserte, J., Garcia-Dorado, D., Ruiz-Meana, M., Agulló, L., Pina, P., Soler-Soler, J. Cardiovasc. Res. (2004) [Pubmed]
  6. Identification of beta-adrenergic receptors in human lymphocytes by (-) (3H) alprenolol binding. Williams, L.T., Snyderman, R., Lefkowitz, R.J. J. Clin. Invest. (1976) [Pubmed]
  7. Reconstitution of beta-adrenergic receptor with components of adenylate cyclase. Hekman, M., Feder, D., Keenan, A.K., Gal, A., Klein, H.W., Pfeuffer, T., Levitzki, A., Helmreich, E.J. EMBO J. (1984) [Pubmed]
  8. Effects of acute and chronic administration of beta-adrenoceptor ligands on airway function in a murine model of asthma. Callaerts-Vegh, Z., Evans, K.L., Dudekula, N., Cuba, D., Knoll, B.J., Callaerts, P.F., Giles, H., Shardonofsky, F.R., Bond, R.A. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  9. beta-Adrenergic agonist activity of a monoclonal anti-idiotypic antibody. Guillet, J.G., Kaveri, S.V., Durieu, O., Delavier, C., Hoebeke, J., Strosberg, A.D. Proc. Natl. Acad. Sci. U.S.A. (1985) [Pubmed]
  10. Identification of cardiac beta-adrenergic receptors by (minus) [3H]alprenolol binding. Alexander, R.W., Williams, L.T., Lefkowitz, R.J. Proc. Natl. Acad. Sci. U.S.A. (1975) [Pubmed]
  11. Arrhythmia prophylaxis: Long-term suppressive medication. Lovell, R.R. Circulation (1975) [Pubmed]
  12. Different effects of propranolol, alprenolol, sotalol, atenolol and metoprolol on serum T3 and serum rT3 in hyperthyroidism. Perrild, H., Hansen, J.M., Skovsted, L., Christensen, L.K. Clin. Endocrinol. (Oxf) (1983) [Pubmed]
  13. Decreased plasma concentrations and clinical effects of alprenolol during combined treatment with pentobarbitone in hypertension. Seideman, P., Borg, K.O., Haglund, K., Von Bahr, C. British journal of clinical pharmacology. (1987) [Pubmed]
  14. Potentiation of haloperidol-induced catalepsy by beta-adrenoceptor antagonists in mice. Hara, C., Ogawa, N. Jpn. J. Pharmacol. (1986) [Pubmed]
  15. The effect of alprenolol on serum myoglobin levels in acute myocardial infarction. Pedersen, F., Rasmussen, S.L., Kølendorf, K., Christiansen, E. Scand. J. Clin. Lab. Invest. (1984) [Pubmed]
  16. Characterization of monoclonal antibodies to the beta-adrenergic antagonist alprenolol as models of the receptor binding site. Sawutz, D.G., Sylvestre, D., Homcy, C.J. J. Immunol. (1985) [Pubmed]
  17. A point mutation in the seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists. Suryanarayana, S., Daunt, D.A., Von Zastrow, M., Kobilka, B.K. J. Biol. Chem. (1991) [Pubmed]
  18. The immune response toward beta-adrenergic ligands and their receptors. VIII. Extensive diversity of VH and VL genes encoding anti-alprenolol antibodies. Nahmias, C., Strosberg, A.D., Emorine, L.J. J. Immunol. (1988) [Pubmed]
  19. Phosphorylation of the mammalian beta-adrenergic receptor by cyclic AMP-dependent protein kinase. Regulation of the rate of receptor phosphorylation and dephosphorylation by agonist occupancy and effects on coupling of the receptor to the stimulatory guanine nucleotide regulatory protein. Benovic, J.L., Pike, L.J., Cerione, R.A., Staniszewski, C., Yoshimasa, T., Codina, J., Caron, M.G., Lefkowitz, R.J. J. Biol. Chem. (1985) [Pubmed]
  20. Lack of beta 3-adrenergic effect on lipolysis in human subcutaneous adipose tissue. Rosenbaum, M., Malbon, C.C., Hirsch, J., Leibel, R.L. J. Clin. Endocrinol. Metab. (1993) [Pubmed]
  21. Electron microscopic localization of the beta-adrenergic receptor using a ferritin-alprenolol probe. Muntz, K.H., Calianos, T.A., Buja, L.M., Willerson, J.T., Bernatowicz, M., Homcy, C.J., Graham, R.M. Mol. Pharmacol. (1988) [Pubmed]
  22. Thyroid hormone modulation of epinephrine-induced lipolysis in rat adipocytes: a possible role of calcium. Goswami, A., Rosenberg, I.N. Endocrinology (1978) [Pubmed]
  23. Alpha 1-adrenergic stimulation of phosphatidylinositol turnover and respiration of brown fat cells. Mohell, N., Wallace, M., Fain, J.N. Mol. Pharmacol. (1984) [Pubmed]
  24. Metabolic changes in muscle on long-term alprenolol therapy. Frisk-Holmberg, M., Jorfeldt, L., Juhlin-Dannfelt, A., Karlsson, J. Clin. Pharmacol. Ther. (1979) [Pubmed]
  25. Study of the interaction between aryloxypropanolamines and Asn386 in helix VII of the human 5-hydroxytryptamine1A receptor. Kuipers, W., Link, R., Standaar, P.J., Stoit, A.R., Van Wijngaarden, I., Leurs, R., Ijzerman, A.P. Mol. Pharmacol. (1997) [Pubmed]
  26. Plasma protein binding of basic drugs. II. Importance of alpha 1-acid glycoprotein for interindividual variation. Piafsky, K.M., Borgå, O. Clin. Pharmacol. Ther. (1977) [Pubmed]
  27. The lymphocyte transformation test for diagnosis of drug-induced occupational allergy. Stejskal, V.D., Olin, R.G., Forsbeck, M. J. Allergy Clin. Immunol. (1986) [Pubmed]
  28. (-)Alprenolol potentiates the disrupting effects of dizocilpine on sensorimotor function in the rat. Zhang, J., Engel, J.A., Jackson, D.M., Johansson, C., Svensson, L. Psychopharmacology (Berl.) (1997) [Pubmed]
  29. The beta 1- and beta 2-adrenoceptor stimulatory effects of alprenolol, oxprenolol and pindolol: a study in the isolated right atrium and uterus of the rat. Abrahamsson, T. Br. J. Pharmacol. (1986) [Pubmed]
  30. L-5-HTP facilitates the electrically stimulated flexor reflex in pithed rats: evidence for 5-HT2-receptor mediation. Skarsfeldt, T., Arnt, J., Hyttel, J. Eur. J. Pharmacol. (1990) [Pubmed]
  31. Role of the inhibitory adrenergic alpha 2 and serotonergic 5-HT1A components of cocaine's actions on the DOI-induced head-twitch response in 5-HT2-receptor supersensitive mice. Darmani, N.A. Pharmacol. Biochem. Behav. (1993) [Pubmed]
  32. Ocular delivery of the beta-adrenergic antagonist alprenolol by sequential bioactivation of its methoxime analogue. Prokai, L., Wu, W.M., Somogyi, G., Bodor, N. J. Med. Chem. (1995) [Pubmed]
  33. Beta-adrenoceptors in the rat kidney. Immunohistochemical study. Amenta, F., Cavallotti, C., De Rossi, M., Vatrella, F. Naunyn Schmiedebergs Arch. Pharmacol. (1983) [Pubmed]
  34. Screening drugs for metabolic stability using pulsed ultrafiltration mass spectrometry. Geun Shin, Y., Bolton, J.L., van Breemen, R.B. Comb. Chem. High Throughput Screen. (2002) [Pubmed]
  35. Pharmacokinetics and pharmacodynamics of alprenolol in the treatment of hypertension. I. Relationship between plasma concentration and adrenergic beta-receptor blockade. Collste, P., Haglund, K., Frisk-Holmberg, M., Rawlins, M.D. Eur. J. Clin. Pharmacol. (1976) [Pubmed]
 
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