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Chemical Compound Review

Xamoterol     N-[2-[[2-hydroxy-3-(4- hydroxyphenoxy)propy...

Synonyms: Carwin, Corwin, Xamtol, Xamoterolum, CHEMBL75753, ...
 
 
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Disease relevance of Xamoterol

 

High impact information on Xamoterol

 

Chemical compound and disease context of Xamoterol

 

Biological context of Xamoterol

  • Changes in exercise tolerance and resting haemodynamics during long-term treatment of heart failure with xamoterol [13].
  • Xamoterol produced significant improvements in resting cardiac index (2.51 +/- 0.15 to 2.80 +/- 0.14 l min-1 m-2; P less than 0.001), stroke volume (62 +/- 4 to 75 +/- 5 mljbeat-1; P less than 0.001) and stroke work index (42.4 +/- 3.6 to 47.7 +/- 3.9 gm beat-1 m-2; P less than 0.01) [14].
  • The effects of xamoterol 0.2 mg kg-1 i.v. on haemodynamics at rest and on exercise were tested in eight patients, before and after 60 days regular treatment with 200 mg b.d. Left ventricular function improved equally with xamoterol on both occasions [15].
  • Xamoterol (200 mg b.d. for 3 months) caused a fall in left ventricular end-diastolic pressure, an increase in dP/dTmax and a shorter systole in all groups of patients [16].
  • Echocardiographic assessment of lack of beta 1-receptor down-regulation during prolonged therapy with xamoterol [15].
 

Anatomical context of Xamoterol

  • The purpose of the study was to examine whether the prolonged administration of the beta 1-adrenoceptor partial agonist xamoterol could improve left ventricular diastolic function and affect the global remodeling process of the left ventricle after anterior myocardial infarction [3].
  • The effect of xamoterol in failing human myocardium [17].
  • The effects of xamoterol and pacing on myocardial blood flow and metabolism in patients with coronary artery disease [18].
  • Xamoterol (0.0001-100 mumol l-1) produced only negative inotropic effects, as measured by changes in isometric force of contraction in diseased human papillary muscle strips [17].
  • 5. ACVI myocyte responses were increased (E(max): GFP vs ACVI=3.16+/-0.77 vs 5.10+/-0.60, P<0.0001) to xamoterol (a partial beta(1)AR-selective agonist) under beta(2)AR blockade (+50 nm ICI 118, 551) [19].
 

Associations of Xamoterol with other chemical compounds

 

Gene context of Xamoterol

 

Analytical, diagnostic and therapeutic context of Xamoterol

  • The acute hemodynamic effects of xamoterol were measured at rest and during two multistaged symptom-limited supine bicycle exercise tests (Ex-T), a control Ex-T followed by an Ex-T with either xamoterol or placebo [4].
  • A large multicenter study program comprised of four studies demonstrated that patients with mild-to-moderate heart failure randomized to xamoterol (n = 617) 200 mg b.i.d. for 3 months significantly (p less than 0.0001) improved exercise capacity by 37% as compared with the placebo group (n = 300) with an increase of 18% [7].
  • To study the acute hemodynamic effects of xamoterol, 24 patients, 39-70 years old, with mild-to-moderate postinfarction left ventricular dysfunction entered a double-blind, between-patient comparison of a single 5-minute intravenous infusion of xamoterol (0.2 mg/kg) and placebo [4].
  • In a double-blind randomized placebo-controlled crossover study of xamoterol, a novel beta 1-partial agonist, 24 h ambulatory electrocardiograms were obtained in 26 patients prior to and at the end of 13-week treatment periods [27].
  • The clinical relevance of these haemodynamic and neurohumoral changes were examined in conjunction with the German-Austrian Xamoterol Group's study, screening 443 patients with mild to moderate heart failure and giving xamoterol or placebo for 3 months as part of a randomized, double-blind study [28].

References

  1. Treatment of idiopathic orthostatic hypotension with xamoterol. Yamashita, H., Yahara, O., Hasebe, N., Kawamura, Y., Obara, A., Honda, H., Kimura, T., Onodera, S. Lancet (1987) [Pubmed]
  2. Effects of the beta 1-adrenergic receptor partial agonist xamoterol on left ventricular diastolic function. An evaluation after 1-6 years of oral therapy. Pouleur, H., Etienne, J., Van Mechelen, H., Gurné, O., Rousseau, M.F. Circulation (1990) [Pubmed]
  3. Long-term effects of xamoterol on left ventricular diastolic function and late remodeling: a study in patients with anterior myocardial infarction and single-vessel disease. Pouleur, H., van Eyll, C., Hanet, C., Cheron, P., Charlier, A.A., Rousseau, M.F. Circulation (1988) [Pubmed]
  4. Improvement of left ventricular contractility and relaxation with the beta 1-adrenergic receptor partial agonist xamoterol at rest and during exercise in patients with postinfarction left ventricular dysfunction. A placebo-controlled randomized trial. de Feyter, P.J., Serruys, P.W., Suryapranata, H. Circulation (1990) [Pubmed]
  5. Effect of xamoterol in Shy-Drager syndrome. Obara, A., Yamashita, H., Onodera, S., Yahara, O., Honda, H., Hasebe, N. Circulation (1992) [Pubmed]
  6. Agonist-induced desensitization of beta-adrenoceptor function in humans. Subtype-selective reduction in beta 1- or beta 2-adrenoceptor-mediated physiological effects by xamoterol or procaterol. Brodde, O.E., Daul, A., Michel-Reher, M., Boomsma, F., Man in 't Veld, A.J., Schlieper, P., Michel, M.C. Circulation (1990) [Pubmed]
  7. Review of clinical experience with xamoterol. Effects on exercise capacity and symptoms in heart failure. Marlow, H.F. Circulation (1990) [Pubmed]
  8. Effects of beta receptor antagonists on left ventricular function in patients with clinical evidence of heart failure after myocardial infarction. A double-blind comparison of metoprolol and xamoterol. Echocardiographic results from the Metoprolol and Xamoterol Infarction Study (MEXIS). Persson, H., Eriksson, S.V., Erhardt, L. Eur. Heart J. (1996) [Pubmed]
  9. Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol. Hicks, P.E., Cavero, I., Manoury, P., Lefevre-Borg, F., Langer, S.Z. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  10. Differential effects of xamoterol and verapamil on ventricular rate regulation in patients with chronic atrial fibrillation. Lundström, T., Moor, E., Rydén, L. Am. Heart J. (1992) [Pubmed]
  11. A comparative study on the ventilatory and haemodynamic effects of xamoterol and atenolol in asthmatic patients. Lammers, J.W., Müller, M.E., Folgering, H.T., van Herwaarden, C.L. British journal of clinical pharmacology. (1986) [Pubmed]
  12. Treatment of heart failure in the elderly. McMurray, L., McDevitt, D.G. Br. Med. Bull. (1990) [Pubmed]
  13. Changes in exercise tolerance and resting haemodynamics during long-term treatment of heart failure with xamoterol. Kayanakis, J.G., Courtault, L., Fauvel, J.M., Boundhoure, J.P., Snow, H.M. Eur. Heart J. (1990) [Pubmed]
  14. The acute effects of intravenous xamoterol ('Corwin', I.C.I. 118, 587) on resting and exercise haemodynamics in patients with mild to moderate heart failure. Virk, S.J., Anfilogoff, N.H., Lawson, N., Sadler, A.M., Smith, S.J., Nuttall, A., Murray, R.G., Littler, W.A., Davies, M.K. Eur. Heart J. (1989) [Pubmed]
  15. Echocardiographic assessment of lack of beta 1-receptor down-regulation during prolonged therapy with xamoterol. Cheron, P., Nannan, M., Pouleur, H., Rousseau, M.F. Eur. Heart J. (1990) [Pubmed]
  16. Illustration of the effects of long-term xamoterol therapy on the time course of left ventricular pressure. van Mechelen, H., Ries, A., Pouleur, H., Rousseau, M.F. Eur. Heart J. (1990) [Pubmed]
  17. The effect of xamoterol in failing human myocardium. Schwinger, R.H., Böhm, M., Erdmann, E. Eur. Heart J. (1990) [Pubmed]
  18. The effects of xamoterol and pacing on myocardial blood flow and metabolism in patients with coronary artery disease. Simonsen, S. Eur. Heart J. (1990) [Pubmed]
  19. Effect of overexpressed adenylyl cyclase VI on beta 1- and beta 2-adrenoceptor responses in adult rat ventricular myocytes. Stark, J.C., Haydock, S.F., Foo, R., Brown, M.J., Harding, S.E. Br. J. Pharmacol. (2004) [Pubmed]
  20. Pharmacological analysis of the cardiac actions of xamoterol, a beta adrenoceptor antagonist with partial agonistic activity, in guinea pig heart: evidence for involvement of adenylate cyclase system in its cardiac stimulant actions. Hattori, Y., Sakuma, I., Nakao, Y., Kanno, M. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  21. Beta-adrenoceptor subtype expression and function in rat white adipocytes. Germack, R., Starzec, A.B., Vassy, R., Perret, G.Y. Br. J. Pharmacol. (1997) [Pubmed]
  22. In vitro and in vivo characterization of intrinsic sympathomimetic activity in normal and heart failure rats. Willette, R.N., Aiyar, N., Yue, T.L., Mitchell, M.P., Disa, J., Storer, B.L., Naselsky, D.P., Stadel, J.M., Ohlstein, E.H., Ruffolo, R.R. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  23. Beta 3-adrenergic receptors regulate retinal endothelial cell migration and proliferation. Steinle, J.J., Booz, G.W., Meininger, C.J., Day, J.N., Granger, H.J. J. Biol. Chem. (2003) [Pubmed]
  24. The in vitro pharmacology of xamoterol (ICI 118,587). Malta, E., Mian, M.A., Raper, C. Br. J. Pharmacol. (1985) [Pubmed]
  25. Effect of xamoterol on exercise capacity and left ventricular function in angina pectoris and in dilated cardiomyopathy. Boström, P.A., Johansson, B.W., Lecerof, H., Lilja, B., Torp, A. Eur. Heart J. (1990) [Pubmed]
  26. Selectivity of xamoterol, prenalterol and salbutamol as assessed by their effects in the presence and absence of ICI 118 551. McCaffrey, P.M., Riddell, J.G., Shanks, R.G. Eur. Heart J. (1990) [Pubmed]
  27. The effects of the partial beta 1-agonist xamoterol on heart rate and ventricular arrhythmias in patients with mild to moderate heart failure. Virk, S.J., Anfilogoff, N.H., Lawson, N., Qiang, F., Murray, R.G., Littler, W.A., Davies, M.K. Eur. Heart J. (1990) [Pubmed]
  28. Sympathetic modulation in practice: the German clinical experience. Kupper, W., Erlemeier, H.H., Bleifeld, W. Eur. Heart J. (1990) [Pubmed]
 
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