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Chemical Compound Review

Tbhpbo     4-[2-hydroxy-3-(tert- butylamino)propoxy]-1...

Synonyms: CHEMBL420746, SureCN2016211, KBioGR_001194, KBioSS_002444, CHEBI:73288, ...
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Disease relevance of Tbhpbo

  • Using a rat model of cardiac failure, induced by myocardial infarction (MI), we compared the desensitization and resensitization of responses to CGP 12177A with those to isoprenaline and RO 363 in left (LA) and right atria (RA) [1].

High impact information on Tbhpbo

  • Denopamine, procaterol, and CGP12177A stimulated oxygen consumption at a concentration of 100 mumol/L [2].
  • The presence of beta 3-ARs coupled to lipolysis was demonstrated by the activity of CGP12177A (EC50 = 1.6 mumol/L; intrinsic activity = 62%) [2].
  • Overexpression of beta 1-adrenoceptors in adult rat ventricular myocytes enhances CGP 12177A cardiostimulation: implications for 'putative' beta 4-adrenoceptor pharmacology [3].
  • 1. The alpha(1)-adrenoceptor antagonist properties of the beta-adrenoceptor nonconventional partial agonist, CGP 12177A, was investigated in functional assays in rat aorta and in radioligand binding assays in rat cerebral cortical membranes [4].
  • BRL37344A and also the other beta(3)-AR agonists, CGP12177A and SR58611A, caused p38 MAPK phosphorylation in dose-dependent manners [5].

Biological context of Tbhpbo

  • These data indicate that CGP-12177A is a novel agonist for BAT thermogenesis [6].
  • In young rats CGP-12177A increased the number of available BAT mitochondrial GDP binding sites at 20 and 60 min post-injection, but in senescent rats GCP-12177A was unable to increase GDP binding [6].

Anatomical context of Tbhpbo


Associations of Tbhpbo with other chemical compounds


Gene context of Tbhpbo


Analytical, diagnostic and therapeutic context of Tbhpbo


  1. Desensitization and resensitization of beta 1- and putative beta 4-adrenoceptor mediated responses occur in parallel in a rat model of cardiac failure. Kompa, A.R., Summers, R.J. Br. J. Pharmacol. (1999) [Pubmed]
  2. Beta 3-adrenergic receptor-mediated lipolysis and oxygen consumption in brown adipocytes from cynomolgus monkeys. Meyers, D.S., Skwish, S., Dickinson, K.E., Kienzle, B., Arbeeny, C.M. J. Clin. Endocrinol. Metab. (1997) [Pubmed]
  3. Overexpression of beta 1-adrenoceptors in adult rat ventricular myocytes enhances CGP 12177A cardiostimulation: implications for 'putative' beta 4-adrenoceptor pharmacology. Lewis, C.J., Gong, H., Brown, M.J., Harding, S.E. Br. J. Pharmacol. (2004) [Pubmed]
  4. ALpha1-adrenoceptor antagonist properties of CGP 12177A and other beta-adrenoceptor ligands: evidence against beta(3)- or atypical beta-adrenoceptors in rat aorta. Brahmadevara, N., Shaw, A.M., MacDonald, A. Br. J. Pharmacol. (2004) [Pubmed]
  5. Stimulation of beta(3)-adrenoceptors causes phosphorylation of p38 mitogen-activated protein kinase via a stimulatory G protein-dependent pathway in 3T3-L1 adipocytes. Mizuno, K., Kanda, Y., Kuroki, Y., Nishio, M., Watanabe, Y. Br. J. Pharmacol. (2002) [Pubmed]
  6. Thermogenesis and mitochondrial GDP binding with age in response to the novel agonist CGP-12177A. Scarpace, P.J., Matheny, M., Borst, S.E. Am. J. Physiol. (1992) [Pubmed]
  7. beta(1)-Adrenoceptors compensate for beta(3)-adrenoceptors in ileum from beta(3)-adrenoceptor knock-out mice. Hutchinson, D.S., Evans, B.A., Summers, R.J. Br. J. Pharmacol. (2001) [Pubmed]
  8. Beta-adrenoceptor subtypes in the ureteral smooth muscle of rats, rabbits and dogs. Tomiyama, Y., Hayakawa, K., Shinagawa, K., Akahane, M., Ajisawa, Y., Park, Y.C., Kurita, T. Eur. J. Pharmacol. (1998) [Pubmed]
  9. Effects of cafeteria diet feeding on beta3-adrenoceptor expression and lipolytic activity in white adipose tissue of male and female rats. Lladó, I., Estrany, M.E., Rodríguez, E., Amengual, B., Roca, P., Palou, A. Int. J. Obes. Relat. Metab. Disord. (2000) [Pubmed]
  10. Existence of a beta3-adrenoceptro and its functional role in the human ureter. Park, Y.C., Tomiyama, Y., Hayakawa, K., Akahane, M., Ajisawa, Y., Miyatake, R., Kiwamoto, H., Sugiyama, T., Kurita, T. J. Urol. (2000) [Pubmed]
  11. Mediation of most atypical effects by species homologues of the beta 3-adrenoceptor. Blin, N., Nahmias, C., Drumare, M.F., Strosberg, A.D. Br. J. Pharmacol. (1994) [Pubmed]
  12. Regulation of obese mRNA expression by hormonal factors in primary cultures of rat adipocytes. Yoshida, T., Hayashi, M., Monkawa, T., Saruta, T. Eur. J. Endocrinol. (1996) [Pubmed]
  13. Anomalous behavior of CGP 12177A on beta 1-adrenergic receptors. Pak, M.D., Fishman, P.H. J. Recept. Signal Transduct. Res. (1996) [Pubmed]
  14. Influence of cell type upon the desensitization of the beta 3-adrenergic receptor. Chaudhry, A., Granneman, J.G. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  15. G-protein-coupled receptor chromatographic stationary phases. 2. Ligand-induced conformational mobility in an immobilized beta2-adrenergic receptor. Beigi, F., Chakir, K., Xiao, R.P., Wainer, I.W. Anal. Chem. (2004) [Pubmed]
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