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Chemical Compound Review

ICI118551     (2R,3R)-1-[(7-methyl-2,3- dihydro-1H-inden...

Synonyms: AC1O44IA
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Disease relevance of ICI118551


High impact information on ICI118551

  • The role of beta-arrestin was further confirmed by showing that transfection of beta-arrestin 2 in these knockout cells restored ICI118551 promoted ERK1/2 activation [3].
  • Displacement with ICI118551 in the bladder base and urethra best fitted a 2-site model with 20% and 28% high affinity sites (beta2), respectively [4].
  • (-)-Isoprenaline mediated relaxation of ileum was antagonized weakly by ICI118551 (100 nM) (beta(2)-AR antagonist) [5].
  • A beta2 antagonist, ICI118551, impaired the PRL but not the VP or OT response to fear or novel environmental stimuli [6].
  • Neither the phasic nature nor the EC50 of the norepinephrine-induced vasoconstrictions was altered in the presence of the beta2-adrenergic receptor antagonist 10(-5) M ICI118551 or the nitric oxide synthase inhibitor 10(-4) M NOARG [7].

Biological context of ICI118551

  • For both rat strains, only half of the displaceable [125I]CYP binding sites displayed high affinity for CGP12177 (IC50 = 6.8 to 7.5 nM), and competition binding studies with CGP20712 and ICI118551 indicated that they represent beta 1- and beta 2-adrenoceptors [8].
  • On calf adipocyte membranes, competition binding curves with CGP12177 displayed one high affinity binding site (IC50 = 4.7 nM), whereas the curves for CGP20712 (beta 1-selective antagonist) and ICI118551 (beta 2-selective antagonist) were biphasic [8].

Anatomical context of ICI118551


Associations of ICI118551 with other chemical compounds


Gene context of ICI118551

  • The affinity of ICI118551, a ligand selective for beta2-AR in other species, was uncharacteristically low in porcine LM (Kd = 441 nM), but was consistent with a value reported for the cloned porcine beta2-AR [9].


  1. Effects of clenbuterol, ICI118551 and sotalol on the growth of cardiac and skeletal muscle and on beta 2-adrenoceptor density in female rats. Sillence, M.N., Matthews, M.L., Spiers, W.G., Pegg, G.G., Lindsay, D.B. Naunyn Schmiedebergs Arch. Pharmacol. (1991) [Pubmed]
  2. Beta1-adrenergic receptors maintain fetal heart rate and survival. Chandra, R., Portbury, A.L., Ray, A., Ream, M., Groelle, M., Chikaraishi, D.M. Biol. Neonate (2006) [Pubmed]
  3. Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors. Azzi, M., Charest, P.G., Angers, S., Rousseau, G., Kohout, T., Bouvier, M., Piñeyro, G. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  4. Identification of beta-adrenoceptor subtypes in lower urinary tract of the female pig. Yamanishi, T., Chapple, C.R., Yasuda, K., Yoshida, K., Chess-Williams, R. J. Urol. (2002) [Pubmed]
  5. 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]
  6. Role of adrenoceptors in vasopressin, oxytocin and prolactin responses to conditioned fear stimuli in the rat. Zou, C.J., Onaka, T., Yagi, K. J. Neuroendocrinol. (1998) [Pubmed]
  7. Alpha1A-adrenergic receptors mediate vasoconstriction of the isolated spiral modiolar artery in vitro. Gruber, D.D., Dang, H., Shimozono, M., Scofield, M.A., Wangemann, P. Hear. Res. (1998) [Pubmed]
  8. Species and strain-related differences in the expression and functionality of beta-adrenoceptor subtypes in adipose tissue. Van Liefde, I., Van Ermen, A., van Witzenburg, A., Fraeyman, N., Vauquelin, G. Archives internationales de pharmacodynamie et de thérapie. (1994) [Pubmed]
  9. Characterization of porcine beta1- and beta2-adrenergic receptors in heart, skeletal muscle, and adipose tissue, and the identification of an atypical beta-adrenergic binding site. Sillence, M.N., Hooper, J., Zhou, G.H., Liu, Q., Munn, K.J. J. Anim. Sci. (2005) [Pubmed]
  10. Adrenaline stimulates acid production in isolated pig and human parietal cells. Song, Y.H., Mårdh, S., Nyrén, O., Lööf, L. Scand. J. Gastroenterol. (1988) [Pubmed]
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