dihydroalprenolol

Summary

Summary: Hydrogenated alprenolol derivative where the extra hydrogens are often tritiated. This radiolabeled form of ALPRENOLOL, a beta-adrenergic blocker, is used to label the beta-adrenergic receptor for isolation and study.

Top Publications

  1. Quach T, Duchemin A, Rose C, Schwartz J. [3H]glycogenolysis in brain slices mediated by beta-adrenoceptors: comparison of physiological response and [3H]dihydroalprenolol binding parameters. Neuropharmacology. 1988;27:629-35 pubmed
    ..conditions which were strictly identical to those used to measure glycogenolysis, a saturable binding of [3H]dihydroalprenolol to the slices occurred with Kd and Bmax values consistent with corresponding values on cell free ..
  2. Zeinstra E, Wilczak N, De Keyser J. [3H]dihydroalprenolol binding to beta adrenergic receptors in multiple sclerosis brain. Neurosci Lett. 2000;289:75-7 pubmed
    ..brain sections of six MS patients and six controls by using quantitative autoradiography with [(3)H]dihydroalprenolol. White matter contained no beta(1) adrenergic receptors...
  3. Heider M, Schliebs R, Rossner S, Bigl V. Basal forebrain cholinergic immunolesion by 192IgG-saporin: evidence for a presynaptic location of subpopulations of alpha 2- and beta-adrenergic as well as 5-HT2A receptors on cortical cholinergic terminals. Neurochem Res. 1997;22:957-66 pubmed
    ..The lesion-induced receptor changes suggest that the alterations in cortical 5-HT2 receptor binding observed in patients with Alzheimer's disease might be secondary to cholinergic deficits...
  4. Falkay G. Effects of antiprogestogen (RU-486) treatment on myometrial and cervical alpha and beta-adrenoceptors in pregnant rabbits. Hum Reprod. 1990;5:924-7 pubmed
    ..The results indicate a heterologous regulation of alpha-adrenoceptors by sex steroids, i.e. suppression of the alpha 2-adrenoceptor concentration by antiprogestogen treatment...
  5. Schaffer S, Allo S, Punna S, White T. Defective response to cAMP-dependent protein kinase in non-insulin-dependent diabetic heart. Am J Physiol. 1991;261:E369-76 pubmed
    ..b>Dihydroalprenolol binding assays revealed that neither beta-adrenergic receptor number nor binding affinity was affected by ..
  6. Sato N, Irie M, Kajinuma H, Suzuki K. Decreased glucagon binding and glucagon-stimulated lipolysis in adipocytes from streptozotocin-diabetic rats. Acta Endocrinol (Copenh). 1989;121:705-13 pubmed
    ..In contrast, beta-adrenergic receptors assessed by [3H]dihydroalprenolol binding and lipolysis stimulated by isoproterenol, dibutyryl 3'5'-cyclic AMP and 3-isobutyl-1-methylxanthine ..
  7. Cernohorský M, Hynie S. [3H-dihydroalprenolol binding to beta-adrenergic receptors in adipocyte membrane fractions of rats premedicated with estrogens]. Sb Lek. 1993;94:63-70 pubmed
    ..performed with membrane fraction of homogenates of epididymal adipose cells, the radioligand used was L-[3H]-dihydroalprenolol (3H-DHA)...
  8. Kaneko M, Chapman D, Ganguly P, Beamish R, Dhalla N. Modification of cardiac adrenergic receptors by oxygen free radicals. Am J Physiol. 1991;260:H821-6 pubmed
    ..The assay of beta-adrenergic receptors involving [3H]dihydroalprenolol (DHA) binding revealed that the maximal number of binding sites (Bmax) and dissociation constant (Kd) were ..
  9. Seifert R. Monovalent anions differentially modulate coupling of the beta2-adrenoceptor to G(s)alpha splice variants. J Pharmacol Exp Ther. 2001;298:840-7 pubmed
    ..Thus, monovalent anions differentially regulate beta2AR-coupling to G(s)alphaS and G(s)alphaL...

More Information

Publications62

  1. Sala R, Moriggi E, Della Bella D, Carenzi A. The specific binding of broxaterol, a new beta 2-selective agonist, to beta-adrenoceptors. Eur J Pharmacol. 1991;203:17-23 pubmed
    ..Broxaterol showed high affinity and selectivity for the beta 2-component of [3H]dihydroalprenolol binding in both lung (58% beta 2-sites, Ki = 130 nM) and heart membranes (19% beta 2-sites, Ki = 98 nM), ..
  2. Suryanarayana S, Daunt D, von Zastrow M, Kobilka B. A point mutation in the seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists. J Biol Chem. 1991;266:15488-92 pubmed
    ..These data suggest that the Asn residue is involved in conferring specificity for binding to a specific class of beta receptor antagonists...
  3. Vacas M, Elverdin J, Chiarenza A, Luchelli M. Daily changes in beta-adrenergic sensitivity of rat submandibular gland. Correlation with beta-adrenoceptor rhythm. Auton Neurosci. 2001;89:1-6 pubmed
    ..beta-Adrenoceptors were studied by 3H-dihydroalprenolol binding to membrane preparations...
  4. Zaccheo D, De Michele M, Mancini M, Amenta F. Decreased density of beta-adrenergic and muscarinic cholinergic receptor sites in the vasa nervorum of aged rats. Mech Ageing Dev. 1991;60:255-65 pubmed
    ..Sprague-Dawley rats of 4 and 24 months of age were used. [3H]Dihydroalprenolol (DHA) and [3H]quinuclidinyl benzilate (QNB) were used to label beta-adrenergic and muscarinic cholinergic ..
  5. Pesta M, Muszynska A, Kucharski J, Superata J, Kotwica J. Beta-adrenergic receptors in corpora lutea from different stages of the estrous cycle in conscious and slaughtered cattle. Biol Reprod. 1994;50:215-21 pubmed
    ..Using 3H-dihydroalprenolol (3H-DHA) as a ligand, we were unable to find specific binding in any of the tissues examined...
  6. Lopes A, Liberato M, Brentani M, Aiello V, Riso A, Ebaid M. Lung beta-adrenoceptors in pulmonary hypertension. A study of biopsy specimens in children with congenital heart disease. Chest. 1991;99:637-41 pubmed
    Characteristics of beta-adrenoceptors were analyzed using radioligand-binding techniques with 3H-dihydroalprenolol in lung specimens from 11 children with pulmonary hypertension (median age, three years) undergoing surgical repair of ..
  7. Seifert R, Lee T, Lam V, Kobilka B. Reconstitution of beta2-adrenoceptor-GTP-binding-protein interaction in Sf9 cells--high coupling efficiency in a beta2-adrenoceptor-G(s alpha) fusion protein. Eur J Biochem. 1998;255:369-82 pubmed
    ..The beta2AR-G(s alpha) fusion protein provides a very sensitive model system to study the regulation of Gs function by beta2AR agonists and inverse agonists directly at the level of the G-protein...
  8. Tsuda H, Ito M, Oguro K, Mutoh K, Shiraishi H, Shirasaka Y, et al. Involvement of the noradrenergic system in the seizures of epileptic El mice. Eur J Pharmacol. 1990;176:321-30 pubmed
    ..the anticonvulsant activity of adrenergic drugs was tested with a scoring method, and the binding of [3H]dihydroalprenolol, [3H]prazosin and [3H]yohimbine was evaluated in whole brains and various brain regions from stimulated and ..
  9. Liu F, Soares M, Audus K. Permeability properties of monolayers of the human trophoblast cell line BeWo. Am J Physiol. 1997;273:C1596-604 pubmed
    ..The basic permeability properties of the BeWo monolayers suggest that the cells grown on permeable supports may be examined as a convenient in vitro system to evaluate some transplacental transport mechanisms...
  10. Kallay Z, Smisterová J, Soltes L, Marko V. Evaluation of 3H-CGP 12177 and 3H-DHA binding to beta 2-adrenoceptors of rat reticulocytes by means of affinity spectra. J Recept Res. 1991;11:909-17 pubmed
    ..This observation further supports the preferred application of 3H-CGP 12177 over 3H-DHA for radio-receptor assay of beta-adrenoceptor blockers...
  11. Suh Y, Lee I, Kim S, Choi W, Park C, Chung M, et al. Ligand binding characteristics of [3H] dihydroalprenolol in cerebral cortical membranes of young and old senescence-accelerated mouse. Comp Biochem Physiol C. 1993;104:423-6 pubmed
    1. The values of both Kd and Bmax of [3H] dihydroalprenolol binding in the cerebral cortical membranes of old-aged (12 month old) SAM-P/1 were not significantly different compared with those of young (2 month old) SAM-P/1. 2...
  12. Parker E, Kameyama K, Higashijima T, Ross E. Reconstitutively active G protein-coupled receptors purified from baculovirus-infected insect cells. J Biol Chem. 1991;266:519-27 pubmed
    ..The beta-AR and m2 MAChR were characteristically stimulated by reduction of disulfides. These results demonstrate the general utility of the baculovirus system for production of large quantities of native G protein-coupled receptors...
  13. Odagaki Y, Koyama T, Matsubara S, Yamashita I. Effects of lithium on the beta-adrenergic receptor-adenylate cyclase system in rat cerebral cortical membranes. Jpn J Pharmacol. 1991;55:407-14 pubmed
    ..Administration of lithium carbonate for 21 days decreased the maximum number of [3H]dihydroalprenolol binding sites without changing the apparent dissociation constant...
  14. Chen C. [Age-dependent changes in the adenylate cyclase system of rat ventral prostate]. Nihon Yakurigaku Zasshi. 1992;99:333-43 pubmed
    ..These results show that changes in the binding ability of G proteins to GTP influence the function of ventral prostates of rats during the aging process, and this is mediated through the regulation of AC activity...
  15. Valet P, Montastruc J, Berlan M, Tran M, Lafontan M, Montastruc P. Differential regulation of fat cell beta-2 and beta-1 adrenoceptors by endogenous catecholamines in dog. J Pharmacol Exp Ther. 1989;249:271-7 pubmed
    ..The present study demonstrates a differential regulation of beta adrenoceptors: beta-2 but not beta-1 adrenoceptors are decreased by long-term exposure to high plasma levels of endogenous catecholamines in the dog...
  16. Evans E, Seifen E, Kennedy R, Kafiluddi R, Paule M, Scallet A, et al. Effects of chronic delta-9-THC treatment on cardiac beta-adrenoceptors in rats. Pharmacol Biochem Behav. 1987;28:171-4 pubmed
    ..Beta-adrenoceptor density and binding affinity estimated with (-)[3H]dihydroalprenolol; a beta-adrenergic antagonist, were not significantly affected by treatment with THC when compared to ..
  17. Popova J, Petkov V. Age-related changes in rat brain muscarinic receptors and beta-adrenoreceptors. Gen Pharmacol. 1989;20:581-4 pubmed
    ..5. The role of age for the changes in the activity of brain muscarinic and beta-adrenoreceptor systems is discussed...
  18. Ishikawa Y, Amano I, Chen C, Ishida H. Diurnal variation of amylase secretion is coupled with alterations of beta-adrenoceptors in the rat parotid gland. Res Exp Med (Berl). 1992;192:231-40 pubmed
    ..The number of maximal binding sites (Bmax) for [3H]dihydroalprenolol (DHA) in parotid membranes showed a diurnal variation with two marked peaks at 13 and 21 h, but the affinity ..
  19. Ireland M, Jacks L. Initial characterization of lens beta-adrenergic receptors. Invest Ophthalmol Vis Sci. 1989;30:2190-4 pubmed
    ..chick lens epithelial and fiber cells and assayed for specific binding of the beta-adrenergic antagonist dihydroalprenolol. Both membranes specifically bound the ligand, with the epithelial membranes exhibiting a greater number of ..
  20. Klimek V, Papp M. The effect of MK-801 and imipramine on beta-adrenergic and 5-HT2 receptors in the chronic mild stress model of depression in rats. Pol J Pharmacol. 1994;46:67-9 pubmed
    ..On the other hand, imipramine administered for 5 weeks reduced the number of beta-adrenergic and 5-HT2 receptors in both control and stressed rats...
  21. Miyamoto A, Ito K, Nishio A. Characterization of beta-adrenoceptors in pig basilar artery from functional and radioligand binding studies. Jpn J Pharmacol. 1993;61:93-9 pubmed
    ..by measuring the relaxation response to norepinephrine and by a radioligand binding assay with [3H]-dihydroalprenolol (DHA). Norepinephrine induced concentration-dependent relaxations...
  22. Hess M, Barasha B, Winters S, Levin R. Effect of thyroxine on urinary bladder autonomic receptor densities and contractility. Pharmacology. 1993;46:248-53 pubmed
  23. Lemmer B, Lang P. Circadian-phase-dependency in [3H]-dihydroalprenolol binding to rat heart ventricular membranes. Chronobiol Int. 1984;1:217-23 pubmed
    Binding studies with the beta-adrenoceptor antagonist ligand [3H]-dihydroalprenolol ([3H]-DHA, spec. act, 90-102 Ci/mmol) were performed with ventricular membranes L-D-synchronized (L:0...
  24. Polson J, Lockey R, Bukantz S, Lowitt S, Krzanowski J, Szentivanyi A. Effects of ketotifen on the responsiveness of peripheral blood lymphocyte beta-adrenergic receptors. Int J Immunopharmacol. 1988;10:657-63 pubmed
    ..Binding of 3H-dihydroalprenolol to beta-receptors was also evaluated...
  25. Koe B, Lebel L. Effects of serotoninergic agents on downregulation of beta-adrenoceptors by the selective serotonin reuptake inhibitor sertraline. Arch Int Pharmacodyn Ther. 1995;329:231-44 pubmed
    ..The respective drug combination produced a reduction in Bmax of [3H]dihydroalprenolol binding to cortical membranes of treated rats at a dose of the releaser, release enhancer, or sertraline, ..
  26. Yamazaki T, Uematsu T, Mizuno A, Takiguchi Y, Nakashima M. Alterations of cardiac adrenoceptors and calcium channels subsequent to production of aortic insufficiency in rats. Arch Int Pharmacodyn Ther. 1989;299:155-68 pubmed
    ..Bmax for 3H-dihydroalprenolol (3H-DHA) of AI rats significantly increased at 2 and 4 weeks and returned to the control level at 8 weeks...
  27. Baron B, Ogden A, Siegel B, Stegeman J, Ursillo R, Dudley M. Rapid down regulation of beta-adrenoceptors by co-administration of desipramine and fluoxetine. Eur J Pharmacol. 1988;154:125-34 pubmed
    ..Consequently, the combination of a norepinephrine and serotonin uptake inhibitor may be an advantageous and rapid treatment for the alleviation of certain forms of depression...
  28. Yamashita A, Kurokawa T, Dan ura T, Yanagiuchi H, Ishibashi S. Protein kinases induce isoproterenol desensitization of beta-adrenoceptor-coupled adenylate cyclase system: significance of receptor occupancy. Eur J Pharmacol. 1987;143:19-26 pubmed
    ..These results suggest that cyclic AMP- or phorbol ester-induced desensitization is enhanced by receptor occupation by beta-adrenoceptor agonists...
  29. Gether U, Lin S, Ghanouni P, Ballesteros J, Weinstein H, Kobilka B. Agonists induce conformational changes in transmembrane domains III and VI of the beta2 adrenoceptor. EMBO J. 1997;16:6737-47 pubmed
  30. Warburton D, Parton L, Buckley S, Cosico L, Saluna T. Beta-receptors and surface active material flux in fetal lamb lung: female advantage. J Appl Physiol (1985). 1987;63:828-33 pubmed
    ..01). beta-Adrenergic receptor binding, using [3H]dihydroalprenolol as the ligand, was saturable, linear, and stereospecific...
  31. Chalecka Franaszek E, Nalepa I, Vetulani J. Differences in beta-adrenergic regulation of cyclic AMP formation in cerebral cortical slices of the rat and spiny mouse--Acomys cahirinus. Pol J Pharmacol Pharm. 1990;42:29-38 pubmed
    ..This feature makes the Acomys an interesting animal model for investigating the role of alpha-beta-adrenoceptor coupling in generation of cyclic AMP and the mechanism of action of antidepressant treatment...
  32. Baran L, Siwanowicz J, Nowak G, Przegalinski E. Captopril lacks the antidepressant-like activity in animal models. Pol J Pharmacol Pharm. 1991;43:265-70 pubmed
    ..These results suggest that captopril has no antidepressant-like activity in animal models...
  33. Ma F, Ohkuma S, Kishi M, Kuriyama K. Ontogeny of beta-adrenergic receptor-mediated cyclic AMP generating system in primary cultured neurons. Int J Dev Neurosci. 1991;9:347-56 pubmed
    ..During neuronal growth in vitro, the number of binding sites for [3H]dihydroalprenolol (DHA) showed a tendency to increase (Bmax), while the affinity (Kd) for [3H]DHA did not show any noticeable ..
  34. Tang C, Yang J, Liu M. Progressive internalization of beta-adrenoceptors in the rat liver during different phases of sepsis. Biochim Biophys Acta. 1998;1407:225-33 pubmed
    ..and the light vesicle fractions of rat liver during different phases of sepsis were studied using [3H]dihydroalprenolol binding and photoaffinity labeling with [125I]iodocyanopindolol diazirine...
  35. Kondratenko T, Zacharova I, Kuzina N, Katukov VYu -, Severin E. The role of histamine H1-receptors in the modulation of neurotransmitter receptors activity in human lung cancer. Biochem Mol Biol Int. 1995;36:429-37 pubmed
    ..The above findings suggest the possibility of the interaction between neural and inflammatory systems in human lung cancer...
  36. Wu B, Yang C, Yang J, Chen I. A new beta-adrenoceptor blocking agent derived from dehydrozingerone. Gen Pharmacol. 1994;25:651-9 pubmed
    ..4. The order of potency of beta-adrenoceptor antagonists in competing for the [3H]dihydroalprenolol binding sites was (-)propranolol > DZPN > or = atenolol.
  37. Hammon H, Bruckmaier R, Honegger U, Blum J. Distribution and density of alpha- and beta-adrenergic receptor binding sites in the bovine mammary gland. J Dairy Res. 1994;61:47-57 pubmed
    ..3H-prazosin, 3H-rauwolscine and 3H-dihydroalprenolol were used for the regional characterization of alpha 1-, alpha 2- and beta-adrenergic receptors by ..
  38. Rossolini G, Viticchi C, Basso A, Zaia A, Piantanelli L. Thymus-induced recovery of age-related decrease of brain cortex alpha- and beta-adrenoceptors. Int J Neurosci. 1991;59:143-50 pubmed
  39. Seo D, Shin C, Ryu J, Cheong J, Choi C, Dailey J, et al. Effect of norepinephrine release on adrenoceptors in severe seizure genetically epilepsy-prone rats. Eur J Pharmacol. 2000;396:53-8 pubmed
    ..Whether the regulation of brain adrenoceptors is quantitatively different in GEPRs from normal animals remains to be established...
  40. Macho L, Kvetnansky R, Fickova M. The effect of hypokinesia on lipid metabolism in adipose tissue. Acta Astronaut. 1984;11:735-8 pubmed
    ..These results showed an important effect of hypokinesia on lipid mobilization, on lipogenesis and on the processes of hormone regulation in adipose tissue...
  41. Takita M, Kigoshi S, Muramatsu I. Effects of bevantolol HCl on immobilization stress-induced hypertension and central beta-adrenoceptors in rats. Pharmacol Biochem Behav. 1993;45:623-7 pubmed
    ..a beta-adrenoceptor blocker, and of repeated immobilization stress on blood pressure, body weight, and [3H]dihydroalprenolol ([3H]DHA) binding to the cerebral cortex were examined in rats...
  42. Styrt B, Klempner M. Lysosomotropic behavior of adrenergic antagonists in interactions with human neutrophils. Biochem Pharmacol. 1988;37:435-41 pubmed
    ..We examined the association of the beta-adrenergic antagonist [3H]dihydroalprenolol with human neutrophils and lysosome and membrane fractions derived from neutrophils, and the subcellular ..
  43. Schneyer C, Humphreys Beher M. Effects of chronic isoproterenol administration on beta 1-adrenoceptors and growth of pancreas of young and adult rats. Proc Soc Exp Biol Med. 1988;188:153-8 pubmed
    3H]Dihydroalprenolol (DHA) binding of membranes of adult pancreas differed from that of pancreas of young rats, and the DHA binding in the presence of atenolol or butoxamine also was different in the two age groups...
  44. Paul I, Duncan G, Kuhn C, Mueller R, Hong J, Breese G. Neural adaptation in imipramine-treated rats processed in forced swim test: assessment of time course, handling, rat strain and amine uptake. J Pharmacol Exp Ther. 1990;252:997-1005 pubmed
    ..abstract truncated at 250 words)..
  45. Watanabe K, Irie M, Kajinuma H, Suzuki K. Adrenalectomy-induced alterations in glucagon binding and lipolysis in isolated rat adipocytes. Horm Metab Res. 1990;22:215-20 pubmed
    ..Binding of the beta-adrenergic antagonist [3H]dihydroalprenolol and maximal lipolysis induced by (-)-isoproterenol, (Bu)2cAMP, 3-isobutyl-1-methylxanthine, and adenosine ..
  46. Stolba P, Opltová H, Husek P, Nedvidkova J, Kunes J, Dobesova Z, et al. Adrenergic overactivity and insulin resistance in nonobese hereditary hypertriglyceridemic rats. Ann N Y Acad Sci. 1993;683:281-8 pubmed
    ..The binding of [3H]-dihydroalprenol to the heart membrane fraction was similar in both groups, but the dissociation constant Kd was increased by 75% in the heart of HTG rats...
  47. Skala J, Shaikh I, Cannon de Rodriguez W. Alpha 2-adrenergic receptors in brown adipose tissue of infant rats--I. Identification and characteristics of binding sites in isolated plasma membranes. Int J Biochem. 1988;20:7-13 pubmed
    ..3. The presence of alpha 2-adrenoceptor subclass in brown fat of infant rats may play a role in the sympathetic regulation of this rapidly proliferating tissue...
  48. Karolewicz B, Bruce K, Lee B, Paul I. Nitric oxide synthase inhibitors have antidepressant-like properties in mice. 2. Chronic treatment results in downregulation of cortical beta-adrenoceptors. Eur J Pharmacol. 1999;372:215-20 pubmed
    ..3H]dihydroalprenolol binding to cortical beta-adrenoceptors was examined in mice treated with the nitric oxide (NO) synthase ..
  49. Moises H, Smith C. Electrophysiological responsiveness to isoproterenol in rat hippocampal slices correlates with changes in beta-adrenergic receptor density induced by chronic morphine treatment. Brain Res. 1989;485:67-78 pubmed
    ..of beta-adrenergic receptors in hippocampus, as measured by the binding of the specific antagonist [3H]dihydroalprenolol (DHA)...
  50. Manukhin B, Nesterova L, Smurova E, Kichikulova T. Interactions of radiolabelled ligands with specific receptors: an analysis. Membr Cell Biol. 2000;13:667-85 pubmed
    The binding and displacement of beta-adrenoceptor blockers, [3H]propranolol ([3H]PRP) and [3H]dihydroalprenolol ([3H]DHA), were studied on isolated rat erythrocytes, their membranes and ghosts; the binding of [3H]DHA and a M-..
  51. Karl P, Teichberg S, Fisher S. Na(+)-dependent amino acid uptake by human placental microvillous membrane vesicles: importance of storage conditions and preservation of cytoskeletal elements. Placenta. 1991;12:239-50 pubmed
    ..These data, especially with regard to storage conditions, highlight the importance of precise definition of preparation and storage conditions when interpreting results of amino acid uptake by human placental MMV...
  52. Paul I, Trullas R, Skolnick P, Nowak G. Down-regulation of cortical beta-adrenoceptors by chronic treatment with functional NMDA antagonists. Psychopharmacology (Berl). 1992;106:285-7 pubmed
    ..3H]Dihydroalprenolol (DHA) binding to cortical beta-adrenoceptors was examined in mice treated with the functional NMDA ..
  53. Andersson R, Johansson S, Salomonsson I. Time course of resensitization of rat uterine beta-adrenoceptor system. Pharmacol Toxicol. 1988;62:29-31 pubmed