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Chemical Compound Review

TERTATOLOL     1-(tert-butylamino)-3- thiochroman-8-yloxy...

Synonyms: Tertatololum, dl-Tertatalol, dl-Tertatolol, rac Tertatolol, SureCN49634, ...
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Disease relevance of TERTATOLOL

  • Tertatolol-induced lupus [1].
  • Considering that beta-blockers prevent arrhythmias specially in hyperadrenergic states, the suppression of the ventricular SNCP by S-2395 could thus be the mechanism by which this drug and possibly other beta-blockers might exert their antiarrhythmic action [2].
  • We compared the central and renal haemodynamic effects of tertatolol, a new non-cardioselective beta-adrenergic blocking drug without partial agonist activity, with those of an equipotent dosage of propranolol in two groups of 10 patients each with acute cerebral injury who had developed systemic hypertension [3].
  • Hemodynamic and pharmacokinetic study of tertatolol in patients with alcoholic cirrhosis and portal hypertension [4].
  • Systemic, splanchnic and renal hemodynamics were evaluated before and 30 min after the simultaneous administration of 2.5 mg tertatolol p.o. and 1.25 mg deuterated tertatolol i.v. in 10 cirrhotic patients with esophageal varices [4].

Psychiatry related information on TERTATOLOL


High impact information on TERTATOLOL

  • We have previously reported that a potent new beta-blocker, tertatolol, when given at therapeutic doses to healthy volunteers, rapidly reduced the number of human mononuclear leukocyte beta-receptors [6].
  • In rats naive to the plus-maze, neither 8-OH-DPAT (50, 100, or 200 ng) nor the 5-HT1A receptor antagonist (+/-)tertatolol (3 microgram) had any significant effect when administered to the dorsal hippocampus [7].
  • Tertatolol is a potent new beta-blocker with no intrinsic sympathomimetic activity or beta 1/beta 2-receptor subtype selectivity [8].
  • In in vitro competitive binding experiments tertatolol was found to be a competitive inhibitor of beta-adrenergic receptors [8].
  • However, on intact human lymphocytes preincubated with this drug, tertatolol reduced the density of beta-adrenergic receptors [8].

Chemical compound and disease context of TERTATOLOL

  • The acute systemic and renal hemodynamic effects of tertatolol, a new noncardioselective beta-blocker without partial agonist activity, were compared to those of an equipotent dose of nadolol in eight patients with essential hypertension [9].
  • The bradycardic effect was abolished by cutting both vagal nerves when the dogs were pretreated with a beta-adrenoceptor blocking agent (S 2395, 50 mug/kg i.v.). The results provide evidence that the NTS is not the main site of action either for the hypotensive effect or for the vagally mediated bradycardia of fentanyl [10].
  • Clonidine (2 mug/kg), injected into the vertebral artery of anaesthetized dogs pretreated with a beta-adrenergic blocking agent (S 2395: 50 mug/kg i.v.) or guanethidine, induced a bradycardia but the discharges of the carotid sinus nerve were not increased [11].
  • Previous administration of the beta-adrenoceptor blocking drug, tertatolol (50 micrograms/kg i.v.), prevented the nicardipine-induced bradycardia and hypotension after injection into the NTS [12].
  • Comparative renal and cardiac effects of tertatolol and enalapril in essential hypertension [13].

Biological context of TERTATOLOL


Anatomical context of TERTATOLOL


Associations of TERTATOLOL with other chemical compounds


Gene context of TERTATOLOL

  • Exercise-induced increase in plasma ANP was potently amplified by oral tertatolol [19].
  • The binding of tertatolol to hippocampal 5-HT1A receptors was stereospecific in that the affinity of (+)-tertatolol to these receptors (Ki = 311.6 nM) was about 20 times lower as compared to that of (-)-tertatolol [17].
  • Levels of UCP1 mRNA were augmented in the Tertatolol-treated group as compared to non-treated high-fat fed animals, while the beta(3)-adrenergic agonist treatment significantly decreased the expression levels of aP2 and transcription factors such as PPARgamma2 and the ratio RXRalpha/RARalpha as compared to obese rats [20].
  • Preserved renal perfusion during beta blockade by tertatolol with and without cyclooxygenase inhibition in normal humans [21].
  • Inulin and PAH clearances were performed before and after 3 months treatment and oral tertatolol, 5 mg daily in eight hypertensive patients with moderate chronic renal failure [22].

Analytical, diagnostic and therapeutic context of TERTATOLOL


  1. Tertatolol-induced lupus. Roudier, J., Delmas, P.D. Arthritis Rheum. (1988) [Pubmed]
  2. Intracardiac electrophysiological study of S-2395 in intact and chemically sympathectomized dogs. Guimond, C., Vasseur, C., Godin, D., LeBlanc, A.R., Nadeau, R. Eur. Heart J. (1983) [Pubmed]
  3. Acute central and renal haemodynamic responses to tertatolol and propranolol in patients with arterial hypertension following head injury. Leeman, M., Naeije, R., Degaute, J.P., Brackman, F., Prost, J.F. J. Hypertens. (1986) [Pubmed]
  4. Hemodynamic and pharmacokinetic study of tertatolol in patients with alcoholic cirrhosis and portal hypertension. Calès, P., Caillau, H., Crambes, O., Vinel, J.P., Desmorat, H., Rocher, I., Jung, L., Urien, S., Brouard, R., Pascal, J.P. J. Hepatol. (1993) [Pubmed]
  5. 5-HT1A receptors in the median raphe nucleus and dorsal hippocampus may mediate anxiolytic and anxiogenic behaviours respectively. Andrews, N., Hogg, S., Gonzalez, L.E., File, S.E. Eur. J. Pharmacol. (1994) [Pubmed]
  6. Certain beta-blockers can decrease beta-adrenergic receptor number: I. Acute reduction in receptor number by tertatolol and bopindolol. De Blasi, A., Fratelli, M., Marasco, O. Circ. Res. (1988) [Pubmed]
  7. Comparative study of pre- and postsynaptic 5-HT1A receptor modulation of anxiety in two ethological animal tests. File, S.E., Gonzalez, L.E., Andrews, N. J. Neurosci. (1996) [Pubmed]
  8. Reduction of beta-adrenergic receptors by tertatolol: an additional mechanism for beta-adrenergic blockade. De Blasi, A., Lipartiti, M., Pirone, F., Rochat, C., Prost, J.F., Garattini, S. Clin. Pharmacol. Ther. (1986) [Pubmed]
  9. Acute effects of tertatolol and nadolol on systemic and renal hemodynamics in patients with essential hypertension. Degaute, J.P., Naeije, R., Abramowicz, M., Leeman, M., Schoutens, A., Prost, J.F. Am. J. Hypertens. (1988) [Pubmed]
  10. Central sites and mechanisms of the hypotensive and bradycardic effects of the narcotic analgesic agent fentanyl. Laubie, M., Schmitt, H., Drouillat, M. Naunyn Schmiedebergs Arch. Pharmacol. (1977) [Pubmed]
  11. Action of clonidine on the baroreceptor pathway and medullary sites mediating vagal bradycardia. Laubie, M., Schmitt, H., Drouillat, M. Eur. J. Pharmacol. (1976) [Pubmed]
  12. Nicardipine decreases blood pressure and heart rate at nucleus tractus solitarii of spontaneously hypertensive rats. Champéroux, P., Brisac, A.M., Laurent, S., Schmitt, H. J. Cardiovasc. Pharmacol. (1989) [Pubmed]
  13. Comparative renal and cardiac effects of tertatolol and enalapril in essential hypertension. Ribstein, J., Du Cailar, G., Brouard, R., Mimran, A. Cardiology (1993) [Pubmed]
  14. The beta adrenoceptor blocker tertatolol causes vasodilatation in the isolated perfused vasoconstricted rat kidney. Verbeuren, T.J., Zonnekeyn, L.L., Prost, J.F., Rochat, C., Thomas, J.R., Herman, A.G. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  15. Effects of tertatolol on post- and prejunctional beta adrenoceptors. Verbeuren, T.J., Laekeman, G., Majchrowicz, B.B., Jordaens, F.H., Zonnekeyn, L.L., Herman, A.G. J. Pharmacol. Exp. Ther. (1985) [Pubmed]
  16. Effects of chronic beta-blocker treatment on catecholamine levels in spontaneously hypertensive rats. Heimburger, M., Denoroy, L., Renaud, B., Sassard, J., Cohen, Y., Wepierre, J. Biochem. Pharmacol. (1983) [Pubmed]
  17. Tertatolol, a new beta-blocker, is a serotonin (5-hydroxytryptamine1A) receptor antagonist in rat brain. Prisco, S., Cagnotto, A., Talone, D., De Blasi, A., Mennini, T., Esposito, E. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  18. Discriminative stimulus effects of 8-hydroxy-2-(di-n-propylamino)tetralin in pigeons and rats: species similarities and differences. Kleven, M.S., Koek, W. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  19. Atrial natriuretic peptide contributes to physiological control of lipid mobilization in humans. Moro, C., Crampes, F., Sengenes, C., De Glisezinski, I., Galitzky, J., Thalamas, C., Lafontan, M., Berlan, M. FASEB J. (2004) [Pubmed]
  20. Up-regulation of a thermogenesis-related gene (UCP1) and down-regulation of PPARgamma and aP2 genes in adipose tissue: possible features of the antiobesity effects of a beta3-adrenergic agonist. Margareto, J., Larrarte, E., Marti, A., Martinez, J.A. Biochem. Pharmacol. (2001) [Pubmed]
  21. Preserved renal perfusion during beta blockade by tertatolol with and without cyclooxygenase inhibition in normal humans. Reuse, C., Leeman, M., Degaute, J.P., Abramowicz, M., Prost, J.F., Naeije, R. Journal of clinical pharmacology. (1988) [Pubmed]
  22. Chronic effects of tertatolol on renal function in hypertensive patients with mild chronic renal failure. Hannedouche, T., Brouard, R., Godin, M., Kleinknecht, D., Paillard, F., Grünfeld, J.P. Nephrol. Dial. Transplant. (1991) [Pubmed]
  23. Tertatolol increases glomerular filtration and urinary sodium in anesthetized rats. Plante, G.E., Prévost, C., Sirois, P., Rochat, C., Prost, J.F. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  24. The Tertatolol International Multicenter Study (T.I.M.S.). Predicting factors of an efficient therapy. Agnes, E., Vandermercken, C., Prost, J.F., Safar, M.E. Am. J. Hypertens. (1989) [Pubmed]
  25. Selective infusion of tertatolol into the renal artery induces a local vasodilator effect in humans. Demonstration by the continuous thermodilution method. Nitenberg, A., Prost, J.F., Joussen, J.M., Blanchet, F., Dutray-Dupagne, C. Am. J. Hypertens. (1989) [Pubmed]
  26. Determination of tertatolol enantiomers in biological fluids by high-performance liquid chromatography. Lave, T., Efthymiopoulos, C., Koffel, J.C., Jung, L. J. Chromatogr. (1991) [Pubmed]
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