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Chemical Compound Review

DIHYDROALPRENOLOL     1-(propan-2-ylamino)-3-(2...

Synonyms: CHEMBL1159723, LS-176066, PDSP1_000153, PDSP2_000152, AC1L29EI, ...
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Disease relevance of DIHYDROALPRENOLOL


High impact information on DIHYDROALPRENOLOL


Biological context of DIHYDROALPRENOLOL

  • Spielberger State anxiety scores correlated with baseline mean heart rate, and Spielberger Trait anxiety scores with lymphocyte DHA binding [7].
  • Using DHA, we demonstrated that the concentration of pulmonary beta-receptors increased significantly between 28 and 31 days of gestation; however, there was no change in the dissociation constant during gestation [8].
  • The Kd value for dihydroalprenolol was approximately the same when determined from equilibrium binding studies or from association and dissociation kinetics, suggesting that the ligand binding is a single step bi-molecular reaction [9].
  • Down regulation of dihydroalprenolol and imipramine binding sites in brain of rats repeatedly treated with imipramine [10].
  • Cold acclimation produced, in isolated cells only, a decrease of 41% in the [3H] dihydroalprenolol binding sites and a beta-adrenergic agonist affinity increase [11].

Anatomical context of DIHYDROALPRENOLOL

  • Binding properties of the receptor for both antagonist and agonist, as assessed by KD for dihydroalprenolol and Ki for (-)-isoproterenol, are also normal in the CF lymphocytes [5].
  • The equilibrium dissociation constant (KD) for the interaction of receptors with dihydroalprenolol was the same (2 to 15 nM) in membranes from control and hyperthyroid rats [12].
  • Crude plasma membranes were prepared from chick lens epithelial and fiber cells and assayed for specific binding of the beta-adrenergic antagonist dihydroalprenolol [13].
  • Myocardial beta-adrenoceptor binding was investigated, with (-)3H dihydroalprenolol as radioligand, in microsomes derived from anterior (ALV) and inferior (ILV) myocardial wall sections of the canine left ventricle [14].
  • We used [3H] dihydroalprenolol (DHA) to investigate the development of pulmonary beta-adrenergic receptors in rabbit fetuses and to study the effect of glucocorticoid treatment on the beta-receptor number [8].

Associations of DIHYDROALPRENOLOL with other chemical compounds

  • No binding of the alpha 1 adrenoceptor antagonist prazosin was observed and the binding properties of beta adrenergic receptors (assayed with 3H-labelled dihydroalprenolol), were similar to those described for normal lymphocytes [15].
  • When the concentration of beta-adrenergic receptors was measured by various concentrations of [3H] dihydroalprenolol (DHA), the maximal binding sites of C6 and C6V-1 cells were 760 and 230 fmol/mg protein, respectively, without any changes in the association constant for DHA [16].
  • These purified membranes were enriched 25-fold in Na+/K(+)-adenosine triphosphate (ATPase), 37-fold in [3H] dihydroalprenolol binding sites, and fivefold in alkaline phosphatase activity compared with the placenta homogenates [17].
  • Moclobemide administered subchronically down-regulates beta adrenoceptors as shown by binding experiments with brain cortical membranes using dihydroalprenolol as ligand [18].
  • Transport of DHA in GH3 was saturable, with an apparent Km of 1.4 microM, was temperature and pH dependent, and was inhibited by the ionophore monensin and the amine transport inhibitor reserpine [1].



Analytical, diagnostic and therapeutic context of DIHYDROALPRENOLOL


  1. Transport of beta-adrenergic antagonists in the absence of beta-adrenergic receptors in rat pituitary tumor cells. Henneberry, R.C., Jahangeer, S., Lysko, P.G. Biochem. Pharmacol. (1986) [Pubmed]
  2. A strong influence of serotonin axons on beta-adrenergic receptors in rat brain. Stockmeier, C.A., Martino, A.M., Kellar, K.J. Science (1985) [Pubmed]
  3. Presynaptic location and axonal transport of beta 1-adrenoreceptors in the rat brain. Levin, B.E. Science (1982) [Pubmed]
  4. beta-Adrenergic receptors in aged rat brain: reduced number and capacity of pineal gland to develop supersensitivity. Greenberg, L.H., Weiss, B. Science (1978) [Pubmed]
  5. Beta adrenergic receptors in lymphocytes and granulocytes from patients with cystic fibrosis. Davis, P.B., Dieckman, L., Boat, T.F., Stern, R.C., Doershuk, C.F. J. Clin. Invest. (1983) [Pubmed]
  6. Ectopic beta-adrenergic receptor binding sites. possible molecular basis of aberrant catecholamine responsiveness of an adrenocortical tumor adenylate cyclase. Williams, L.T., Gore, T.B., Lefkowitz, R.J. J. Clin. Invest. (1977) [Pubmed]
  7. Biological correlates of lactate sensitivity in panic disorder. Aronson, T.A., Carasiti, I., McBane, D., Whitaker-Azmitia, P. Biol. Psychiatry (1989) [Pubmed]
  8. Glucocorticoids increase pulmonary beta-adrenergic receptors in fetal rabbit. Cheng, J.B., Goldfien, A., Ballard, P.L., Roberts, J.M. Endocrinology (1980) [Pubmed]
  9. Characterization of the beta-adrenergic receptors of cultured human epidermal keratinocytes. Gazith, J., Cavey, M.T., Cavey, D., Shroot, B., Reichert, U. Biochem. Pharmacol. (1983) [Pubmed]
  10. Down regulation of dihydroalprenolol and imipramine binding sites in brain of rats repeatedly treated with imipramine. Kinnier, W.J., Chuang, D.M., Costa, E. Eur. J. Pharmacol. (1980) [Pubmed]
  11. Characteristics of beta-adrenergic receptors in isolated cells and in crude membranes of brown adipose tissue. Senault, C., Le Comte, V., Portet, R. Biochimie (1984) [Pubmed]
  12. Thyroid hormone regulation of beta-adrenergic receptor number. Williams, L.T., Lefkowitz, R.J., Watanabe, A.M., Hathaway, D.R., Besch, H.R. J. Biol. Chem. (1977) [Pubmed]
  13. Initial characterization of lens beta-adrenergic receptors. Ireland, M.E., Jacks, L.A. Invest. Ophthalmol. Vis. Sci. (1989) [Pubmed]
  14. Differences in beta-adrenoceptor binding in anterior and inferior myocardial wall microsomes of normal canine left ventricle. Burnam, M.H., Sethna, D.H., Rose, D.M., Stern, C.S., Shell, W.E. Cardiovasc. Res. (1981) [Pubmed]
  15. Active alpha 2 and beta adrenoceptors in lymphocytes from patients with chronic lymphocytic leukemia. Goin, J.C., Sterin-Borda, L., Borda, E.S., Finiasz, M., Fernández, J., de Bracco, M.M. Int. J. Cancer (1991) [Pubmed]
  16. Receptor-associated changes of the catecholamine-sensitive adenylate cyclase in glioma cells doubly transformed with Moloney sarcoma virus. Higashida, H., Miki, N., Tanaka, T., Kato, K., Nakano, T., Nagatsu, T., Kano-Tanaka, K. J. Cell. Physiol. (1982) [Pubmed]
  17. Characterization of calcium transport by basal plasma membranes from human placental syncytiotrophoblast. Lafond, J., Leclerc, M., Brunette, M.G. J. Cell. Physiol. (1991) [Pubmed]
  18. Neurochemical profile of moclobemide, a short-acting and reversible inhibitor of monoamine oxidase type A. Da Prada, M., Kettler, R., Keller, H.H., Burkard, W.P., Muggli-Maniglio, D., Haefely, W.E. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  19. Adenylate cyclase and beta adrenergic receptor development in the mouse heart. Chen, F.C., Yamamura, H.I., Roeske, W.R. J. Pharmacol. Exp. Ther. (1982) [Pubmed]
  20. The synthesis and high-level expression of a beta2-adrenergic receptor gene in a tetracycline-inducible stable mammalian cell line. Chelikani, P., Reeves, P.J., Rajbhandary, U.L., Khorana, H.G. Protein Sci. (2006) [Pubmed]
  21. Isolation and purification of human placental plasma membranes from normal and pre-eclamptic pregnancies. a comparative study. Jimenez, V., Henriquez, M., Llanos, P., Riquelme, G. Placenta (2004) [Pubmed]
  22. Autoradiographic localization of peripheral benzodiazepine, dihydroalprenolol and arginine vasopressin binding sites in the pituitaries of control, stalk transected and Brattleboro rats. Bunn, S.J., Hanley, M.R., Wilkin, G.P. Neuroendocrinology (1986) [Pubmed]
  23. Ligand binding to the porcine adipose tissue beta-adrenergic receptor. Mersmann, H.J., McNeel, R.L. J. Anim. Sci. (1992) [Pubmed]
  24. In vivo autoradiographic demonstration of beta-adrenergic binding sites in adult rat type II alveolar epithelial cells. Smith, D.M., Sidhu, N.K. Life Sci. (1984) [Pubmed]
  25. Evidence that dl-propranolol increases thymidine kinase activity, cell mitosis, and beta-adrenoceptors during rat liver regeneration. Reyes-Salcido, V., Villalobos-Molina, R. Arch. Med. Res. (2003) [Pubmed]
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