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Chemical Compound Review

Guanoxabenz     2-[(2,6-dichlorophenyl) methylideneamino]-1...

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Disease relevance of Guanoxabenz

  • Compared with yohimbine, these analogues were, respectively, 36 and 18 times more potent intravenously and 5 and 7.5 times more potent orally in their antagonism of guanoxabenz-induced mydriasis in the pentobarbitone-anaesthetized rat [1].

High impact information on Guanoxabenz

  • Moreover, when the spleen membranes were extensively washed for 30 min with buffers at 25 degrees, the guanoxabenz high-affinity binding disappeared [2].
  • The mechanism for formation of high affinity binding of guanoxabenz (1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine) to alpha2-adrenoceptors by the rat spleen cytosol was studied [3].
  • The formation of guanoxabenz high-affinity binding was also inhibited in a time- and concentration-dependent fashion by preincubating the membranes with the LW03 N-hydroxyguanidine analogue of guanoxabenz [2].
  • Neither corynanthine nor prazosin reversed the guanoxabenz-induced mydriasis [4].
  • The action of the enzyme on guanoxabenz resulted in the formation of guanabenz [1-(2,6-dichlorobenzylidene-amino)-3-guanidine]; the product formation could be monitored by HPLC and its identity was confirmed by NMR analysis [5].

Anatomical context of Guanoxabenz

  • Similarly, antagonist potency in the vas deferens was highly correlated with antagonist activity in reversing the centrally-mediated mydriasis induced by the selective alpha 2-adrenoceptor agonist, guanoxabenz, in pentobarbitone-anaesthetized rats [6].
  • However, by contrast to the results with the spleen, the guanoxabenz competition curves for the spinal cord and cerebral cortex were monophasic and resolved only into one site fits, the Kd of guanoxabenz being about 4000 nmol/l for both tissues [7].
  • We conclude that the rat cerebral cortex contains an enzymatic activity that may activate guanoxabenz leading to formation of a metabolite showing high affinity for alpha 2-adrenoceptors [8].
  • Moreover, when the rat RNG alpha 2B-adrenoceptor was expressed in COS-7 cells and its binding properties tested using [3H]-MK 912 binding, guanoxabenz, LT 11 as well as a number of other drugs inhibited the ligand binding at a single alpha 2-adrenoceptor site; the drug Kds being practically the same as those found for the neonatal rat lung [9].

Associations of Guanoxabenz with other chemical compounds


Gene context of Guanoxabenz

  • Formation of guanoxabenz from guanabenz in human liver. A new metabolic marker for CYP1A2 [10].
  • However, the competition curves for guanoxabenz were definitely biphasic and resolved into two site fits, indicating that guanoxabenz was binding to both high affinity (Kd = 35 nmol/l) and low affinity (Kd = 8900 nmol/l) alpha 2A-adrenoceptor sites in the proportions 57% and 43%, respectively [7].

Analytical, diagnostic and therapeutic context of Guanoxabenz

  • The alpha 2-adrenoceptor antagonists yohimbine and mianserin were also effective in blocking guanoxabenz-induced EEG synchronisation but had a lower potency than did RX 781094 [11].


  1. 2-Alkyl analogue of idazoxan (RX 781094) with enhanced antagonist potency and selectivity at central alpha 2-adrenoceptors in the rat. Gadie, B., Lane, A.C., McCarthy, P.S., Tulloch, I.F., Walter, D.S. Br. J. Pharmacol. (1984) [Pubmed]
  2. Characterization of the enzymatic activity for biphasic competition by guanoxabenz (1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine) at alpha2-adrenoceptors. I. Description of an enzymatic activity in spleen membranes. Uhlén, S., Dambrova, M., Tiger, G., Oliver, D.W., Wikberg, J.E. Biochem. Pharmacol. (1998) [Pubmed]
  3. Characterization of the enzymatic activity for biphasic competition by guanoxabenz (1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine) at alpha2-adrenoceptors. II. Description of a xanthine-dependent enzymatic activity in spleen cytosol. Dambrova, M., Uhlén, S., Welch, C.J., Prusis, P., Wikberg, J.E. Biochem. Pharmacol. (1998) [Pubmed]
  4. alpha 2-Adrenoceptor agonists induced mydriasis in the rat by an action within the central nervous system. Berridge, T.L., Gadie, B., Roach, A.G., Tulloch, I.F. Br. J. Pharmacol. (1983) [Pubmed]
  5. Identification of an N-hydroxyguanidine reducing activity of xanthine oxidase. Dambrova, M., Uhlén, S., Welch, C.J., Wikberg, J.E. Eur. J. Biochem. (1998) [Pubmed]
  6. Evidence for pharmacological similarity between alpha 2-adrenoceptors in the vas deferens and central nervous system of the rat. Doxey, J.C., Gadie, B., Lane, A.C., Tulloch, I.F. Br. J. Pharmacol. (1983) [Pubmed]
  7. Evidence for the existence of two forms of alpha 2A-adrenoceptors in the rat. Uhlén, S., Xia, Y., Chhajlani, V., Lien, E.J., Wikberg, J.E. Naunyn Schmiedebergs Arch. Pharmacol. (1993) [Pubmed]
  8. Characterization of guanoxabenz reducing activity in rat brain. Dambrova, M., Uhlén, S., Wikberg, J.E. Pharmacol. Toxicol. (1998) [Pubmed]
  9. Further evidence for the existence of two forms of alpha 2B-adrenoceptors in rat. Xia, Y., Uhlén, S., Chhajlani, V., Lien, E.J., Wikberg, J.E. Pharmacol. Toxicol. (1993) [Pubmed]
  10. Formation of guanoxabenz from guanabenz in human liver. A new metabolic marker for CYP1A2. Clement, B., Demesmaeker, M. Drug Metab. Dispos. (1997) [Pubmed]
  11. Neuropharmacological studies in rodents on the action of RX 781094, a new selective alpha 2-adrenoceptor antagonist. Dettmar, P.W., Lynn, A.G., Tulloch, I.F. Neuropharmacology (1983) [Pubmed]
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