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Chemical Compound Review:

Ethoxyidazoxan 2-(9-ethoxy-7,10- dioxabicyclo[4.4.0]deca-1...

Synonyms: SureCN10804432, AC1L2PKE, CTK8D7107, AR-1C6697, PDSP1_001655, ...

Schmidt, M.E. et al., Pauwels, P.J. et al., Doxey, J.C. et al., Pauwels, P.J. et al.

Schmidt, Oshinsky, Kim, Schouten, Folley, Potter, Pauwels, Wurch, Tardif, Finana, Colpaert,

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

High impact information on RX 811059

Activation of the wild-type alpha2B AR-Galpha15 fusion protein in CHO-K1 cells by (-)-adrenaline induced a time- and concentration-dependent (pEC50 = 7.37+/-0.13) increase in the intracellular Ca2+ concentration, which could be antagonized by RX 811059 (pK(B) = 7.55+/-0.15) [1].
Objective: To test whether these effects on brain metabolic rate could have been mediated by imidazoline binding sites, single dose challenges of 9 or 12 mcg/kg ethoxyidazoxan (ETX; an alpha(2)-adrenoceptor antagonist which does not bind to imidazoline sites) were given to healthy male volunteers [2].
Although idazoxan produced contractions of the anococcygeus muscle and increased blood pressure in pithed rats, three of the analogues (RX 811005, RX 801079 and RX 811033) were inactive [3].
RX 811059 (10 microM) was the only compound to be completely silent at both the wt and mutant alpha2 AR subtypes [4].

References

Ligand-receptor interactions as controlled by wild-type and mutant Thr(370)Lys alpha2B-adrenoceptor-Galpha15 fusion proteins. Pauwels, P.J., Tardif, S., Finana, F., Wurch, T., Colpaert, F.C. J. Neurochem. (2000) [Pubmed]
Cerebral glucose metabolic and plasma catecholamine responses to the alpha(2) adrenoceptor antagonist ethoxyidazoxan given to healthy volunteers. Schmidt, M.E., Oshinsky, R.J., Kim, H.G., Schouten, J.L., Folley, B.S., Potter, W.Z. Psychopharmacology (Berl.) (1999) [Pubmed]
Selectivity and potency of 2-alkyl analogues of the alpha 2-adrenoceptor antagonist idazoxan (RX 781094) in peripheral systems. Doxey, J.C., Roach, A.G., Strachan, D.A., Virdee, N.K. Br. J. Pharmacol. (1984) [Pubmed]
Analysis of ligand activation of alpha 2-adrenoceptor subtypes under conditions of equal G alpha protein stoichiometry. Pauwels, P.J., Wurch, T., Tardif, S., Finana, F., Colpaert, F.C. Naunyn Schmiedebergs Arch. Pharmacol. (2001) [Pubmed]

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