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Chemical Compound Review

Lopac-I-127     (2S,3S)-1-[(7-methyl-2,3- dihydro-1H-inden...

Synonyms: Tocris-0821, AC1NUNSO, CHEMBL198059, SureCN8027938, CHEBI:73289, ...
 
 
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Disease relevance of Tocris-0821

 

High impact information on Tocris-0821

  • Furthermore, ICI 118551 selective beta 2-adrenergic blockade offers portal blood flow and portal pressure reduction independent of reduction in cardiac output, which could be uniquely advantageous in situations where impairment of cardiac compensatory mechanisms might prove deleterious [6].
  • We document the molecular properties of the more efficacious ICI 118551; (i) it shows higher affinity for the inactive form of the receptor and (ii) it inhibits the spontaneous formation of a beta-adrenergic receptor kinase substrate by the receptor [7].
  • To examine the possibility that beta 2-blockade may contribute to the antihypertensive action of beta-blocker therapy, we studied the cardiovascular effects of compound ICI 118551, a beta 2-selective blocker [8].
  • Intracerebroventricular, but not intravenous, administration of the beta 2-adrenergic receptor antagonist ICI 118551 (30 micrograms) prevented the increased renal sympathetic nerve activity and antinatriuretic responses to air stress [9].
  • METHODS: Slide-mounted sections of human and rat inferior vagal ganglia were incubated with [125I]-pindolol in the absence or presence of propranolol (10 mumol/l) to define non-specific binding, atenolol (10 mumol/l) to inhibit binding to beta 1-adrenoceptors, or ICI 118551 (3 nmol/l) to inhibit binding to beta 2-adrenoceptors [10].
 

Chemical compound and disease context of Tocris-0821

 

Biological context of Tocris-0821

  • The reduced noradrenaline release in the presence of ICI 118551 was not accompanied by a reduction in blood pressure [11].
  • Furthermore, the beta 2-selective antagonist ICI 118551 was much less potent in the C6 cell line (IC50 = 0.2 +/- 0.05 microM; N = 3) than in the B50 cells [12].
  • These CGP-induced responses were antagonized by the beta(2)-selective antagonist ICI 118551 (apparent log K(D) values of -8.84+/-0.15 and -9.51+/-0.02 for the cyclic AMP and reporter gene responses respectively) [13].
  • In the presence of the beta(2)-adrenoceptor antagonist ICI-118551 (ICI, 10 microM), Iso caused an increase in [(14)C]phenylalanine incorporation, protein and RNA mass, cell volume, and cross-sectional area [14].
  • Antagonism of (-)-isoprenaline-stimulated cyclic AMP production by low concentrations of ICI 118551, yielded pseudo pA2 values in muscle and adipose tissue of 7.6 and 8.7 respectively, confirming that beta 2-adrenoceptors in these tissues are linked to the production of the second-messenger [15].
 

Anatomical context of Tocris-0821

  • This may be because ICI 118551 also blocked vasodilatory beta 2-adrenoceptors on vascular smooth muscle [11].
  • Soleus muscle membranes were found to host a population of beta 2-adrenoceptors, characterized by a high affinity for ICI 118551 (pK 9.1), but beta 1-adrenoceptors could not be detected in this preparation [16].
  • 3. Using ICI-118551, we determined the ratio of beta 1:beta 2-adrenoceptors in the trachea and heart to be approximately 29:71 and 56:44, respectively [17].
  • In the uterus, ICI 118551 (3 X 10(-9) M, 3 X 10(-8) M, 3 X 10(-7) M) blocked the pindolol effect with a pKB of 9.28 [18].
  • These effects were not modified by the incubation of myocytes with CGP-20712A (3 x 10(-7) M), a beta1-AR antagonist, but were abolished by pretreatment of myocytes with ICI-118551 (10(-7) M), a beta2-AR antagonist [19].
 

Associations of Tocris-0821 with other chemical compounds

 

Gene context of Tocris-0821

 

Analytical, diagnostic and therapeutic context of Tocris-0821

References

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