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Chemical Compound Review

HEAT     2-[[2-(4-hydroxyphenyl) ethylamino]methyl]...

Synonyms: AG-F-41777, SureCN6413372, BE-2254, Ibe 2254, CTK4I2425, ...
 
 
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Disease relevance of BE-2254

 

Psychiatry related information on BE-2254

  • A lack of spatial working memory deficits in BE 2254 or saline-injected animals was also observed in two other conditions of the behavioral protocol [4].
 

High impact information on BE-2254

  • Phentolamine and the aqueous soluble alpha 1-adrenergic antagonist BE-2254 administered as late as 2 min before reperfusion similarly attenuated the increase in tissue calcium [5].
  • Epinephrine at a concentration of 10(-6) M also initiated triggered activity in Purkinje fibers exposed to LPC (75 microM), a response blocked by l-propranolol (2 X 10(-7) M and 10(-6) M) but not by the alpha 1-adrenergic blocking agent BE-2254 (10(-6) M) [6].
  • Rauwolscine (10(-9), 10(-8), and 10(-7) mol/liter) and BE 2254 (10(-7) but not 10(-8) mol/liter) significantly enhanced stimulation-induced tritium efflux in arteries and veins [7].
  • Heart rate, arterial pressure, femoral flow, and femoral resistance responses elicited from efferent spinal pathways were significantly attenuated following superfusion of the spinal cord with the alpha-antagonists BE-2254 (HEAT) and phentolamine [8].
  • 125I-Labeled BE 2254 (125IBE) was found to bind rapidly and reversibly to a single class of high-affinity binding sites in homogenates of rat vas deferens [9].
 

Biological context of BE-2254

 

Anatomical context of BE-2254

  • The effects of 2-[beta-(4-hydroxyphenyl)-ethyl-aminomethyl]-tetralone (BE 2254) on pre- and postsynaptic alpha-adrenoceptors were studies in isolated rabbit hearts and strips of rabbit pulmonary arteries [13].
  • In particular, alpha 1-adrenoceptor-selective antagonists (prazosin, WB 4101, BE 2254...) displaced with nanomolar affinity about 15 and 40% of the specific [3H]ketanserin binding in human and pig frontal cortex membranes, respectively [14].
  • To this end, C57Bl/6 mice were infused bilaterally into the lateral septal nuclei with 500 ng/0.2 microliter of BE 2254, a selective alpha 1 postsynaptic adrenoceptor antagonist [4].
  • (2) Heat shock and hyperosmolarity increase expression of differentiation markers in K562, HT29, HL60 and in K562, PANC1, and HT29 cells, respectively [15].
  • Dopamine (5.3 X 10(-6) to 5.3 X 10(-5) M) decreased the force of spontaneous myogenic contractions of the rat portal vein in a concentration-dependent manner in the presence of the alpha-adrenoreceptor antagonist BE-2254 [16].
 

Associations of BE-2254 with other chemical compounds

 

Gene context of BE-2254

  • Contribution of heat transfer to turbine blades and vanes for high temperature industrial gas turbines. Part 2: Heat transfer on serpentine flow passage [17].
 

Analytical, diagnostic and therapeutic context of BE-2254

  • Transmural electrical stimulation of BIAA segments resulted in activation of ERK, which was inhibited by the alpha(1)-AR-selective antagonist BE 2254 (2-[[beta-(4-hydroxyphenyl)ethyl]aminomethyl]-1-tetralone) [18].
  • Rapid and simple purification of the 125I-labeled alpha-1 adrenergic radioligand 2-[beta-(4-hydroxylphenylethyl)aminomethyl] tetralone (BE 2254) using reversed-phase high-performance liquid chromatography [19].
  • In these conditions, the BE 2254, as well as the saline-injected control group, showed an elevation of the anxiety level that may be the indirect expression of a nonspecific septal dysfunction induced by the vehicle injection rather than the normal behavioral response produced by the decrease of septal NA activity [4].
  • 2. Heat treatment of the partial denture alloys tested resulted in reductions in strength, while the elongations varied [20].

References

  1. Catecholamines can induce adenosine receptor-mediated protection of the myocardium but do not participate in ischemic preconditioning in the rabbit. Thornton, J.D., Daly, J.F., Cohen, M.V., Yang, X.M., Downey, J.M. Circ. Res. (1993) [Pubmed]
  2. The effect of dietary protein and energy restriction on heat production and growth costs in the young rat. Coyer, P.A., Rivers, J.P., Millward, D.J. Br. J. Nutr. (1987) [Pubmed]
  3. Effect of acute heat exposure on triglyceride transfer to the preovulatory follicles of the laying fowl (Gallus domesticus). Arad, Z., el-Sayed, M.S., Brackenbury, J.H. Br. Poult. Sci. (1993) [Pubmed]
  4. Consequences of selective blockade of septal noradrenergic afferents on anxiety and spatial working memory performance in mice. Belotti, M., Galey, D. Pharmacol. Biochem. Behav. (1996) [Pubmed]
  5. Alpha adrenergic-mediated accumulation of calcium in reperfused myocardium. Sharma, A.D., Saffitz, J.E., Lee, B.I., Sobel, B.E., Corr, P.B. J. Clin. Invest. (1983) [Pubmed]
  6. Induction of delayed afterdepolarizations and triggered activity in canine Purkinje fibers by lysophosphoglycerides. Pogwizd, S.M., Onufer, J.R., Kramer, J.B., Sobel, B.E., Corr, P.B. Circ. Res. (1986) [Pubmed]
  7. Neuronally released norepinephrine does not preferentially activate postjunctional alpha 1-adrenoceptors in human blood vessels in vitro. Stevens, M.J., Moulds, R.F. Circ. Res. (1985) [Pubmed]
  8. Spinal adrenergic mechanisms regulating sympathetic outflow to blood vessels. Taylor, D.G., Brody, M.J. Circ. Res. (1976) [Pubmed]
  9. Occupancy of alpha 1-adrenergic receptors and contraction of rat vas deferens. Minneman, K.P., Fox, A.W., Abel, P.W. Mol. Pharmacol. (1983) [Pubmed]
  10. Effect of carbonated water on arterial pH, PCO2 and plasma lactate in heat-stressed broilers. Raup, T.J., Bottje, W.G. Br. Poult. Sci. (1990) [Pubmed]
  11. Effects of environmental temperature and heat production due to food intake on abdominal temperature, shank skin temperature and respiration rate of broilers. Zhou, W.T., Yamamoto, S. Br. Poult. Sci. (1997) [Pubmed]
  12. Antagonism of pre and postsynaptic alpha-adrenoreceptors by BE 2254 (HEAT) and prazosin. Hicks, P.E. Journal of autonomic pharmacology. (1981) [Pubmed]
  13. Preferential blockade of postsynaptic alpha-adrenoceptors by BE 2254. Göthert, M., Nolte, J., Weinheimer, G. Eur. J. Pharmacol. (1981) [Pubmed]
  14. [3H]ketanserin labels 5-HT2 receptors and alpha 1-adrenoceptors in human and pig brain membranes. Hoyer, D., Vos, P., Closse, A., Pazos, A., Palacios, J.M., Davies, H. Naunyn Schmiedebergs Arch. Pharmacol. (1987) [Pubmed]
  15. Tumor cell differentiation by butyrate and environmental stress. Witt, O., Schulze, S., Kanbach, K., Roth, C., Pekrun, A. Cancer Lett. (2001) [Pubmed]
  16. No evidence of vascular dopamine receptors in the rat portal vein. Vidal-Beretervide, K., Decker, N., Schmidt, M. Fundamental & clinical pharmacology. (1988) [Pubmed]
  17. Contribution of heat transfer to turbine blades and vanes for high temperature industrial gas turbines. Part 2: Heat transfer on serpentine flow passage. Takeishi, K., Aoki, S. Ann. N. Y. Acad. Sci. (2001) [Pubmed]
  18. Relationship between alpha(1)-adrenergic receptor-induced contraction and extracellular signal-regulated kinase activation in the bovine inferior alveolar artery. Hague, C., Gonzalez-Cabrera, P.J., Jeffries, W.B., Abel, P.W. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  19. Rapid and simple purification of the 125I-labeled alpha-1 adrenergic radioligand 2-[beta-(4-hydroxylphenylethyl)aminomethyl] tetralone (BE 2254) using reversed-phase high-performance liquid chromatography. Riemer, R.K., Kuhn, R.W. J. Chromatogr. (1985) [Pubmed]
  20. The influence of heat treatments on several types of base-metal removable partial denture alloys. Morris, H.F., Asgar, K., Rowe, A.P., Nasjleti, C.E. The Journal of prosthetic dentistry. (1979) [Pubmed]
 
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