Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

Imiloxan 2-(7,10- dioxabicyclo[4.4.0]deca- 1,3,5...

Synonyms: Imiloxano, Imiloxanum, GNF-Pf-2156, Imiloxan [INN], CHEMBL347695, ...

Bohmann, C. et al., Gobbi, M. et al., Michel, A.D. et al., Takano, Y. et al., Timmermans, P.B. et al.

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High impact information on RS 21361

However, at a frequency of 100 Hz for 0.06 s the alpha-adrenoceptor antagonists, idazoxan (0.1, 1.0 microM), imiloxan (0.1, 1.0 microM), BRL 44408 (0.1, 1.0 microM), BRL 41992 (0.1, 1.0 microM) and prazosin (0.01 microM) failed to enhance S-I outflow of radioactivity [1].
The selectivity of imiloxan for the alpha 2B-adrenoceptor binding site, coupled with its specificity for alpha 2-adrenoceptors, should make it a valuable tool in the classification of alpha 2-adrenoceptor subtypes [2].
RS 21361 exhibited but minor actions on diastolic pressure and did not influence heart rate [3].
The effect of intrathecally administered imiloxan and WB4101: possible role of alpha 2-adrenoceptor subtypes in the spinal cord [4].
The rank order of potency in antagonizing the inhibitory effect of (-)-noradrenaline or clonidine on the K(+)-induced [3H]noradrenaline and [3H]5-hydroxytryptamine (5-HT) release from superfused synaptosomes was BRL-44408 > or = BRL-41992 >> imiloxan [5].

Associations of RS 21361 with other chemical compounds

2 At a frequency of 1 Hz for 30 s the alpha-adrenoceptor antagonists BRL 44408 (0.01, 0.1 microM) and imiloxan (0.1, 1.0 microM) enhanced S-I outflow of radioactivity [1].

References

Alpha 2-autoreceptor subclassification in rat isolated kidney by use of short trains of electrical stimulation. Bohmann, C., Schollmeyer, P., Rump, L.C. Br. J. Pharmacol. (1993) [Pubmed]
Assessment of imiloxan as a selective alpha 2B-adrenoceptor antagonist. Michel, A.D., Loury, D.N., Whiting, R.L. Br. J. Pharmacol. (1990) [Pubmed]
A study of the selectivity and potency of rauwolscine, RX 781094 and RS 21361 as antagonists of alpha-1 and alpha-2 adrenoceptors. Timmermans, P.B., Qian, J.Q., Ruffolo, R.R., van Zwieten, P.A. J. Pharmacol. Exp. Ther. (1984) [Pubmed]
The effect of intrathecally administered imiloxan and WB4101: possible role of alpha 2-adrenoceptor subtypes in the spinal cord. Takano, Y., Takano, M., Yaksh, T.L. Eur. J. Pharmacol. (1992) [Pubmed]
Further studies on alpha 2-adrenoceptor subtypes involved in the modulation of [3H]noradrenaline and [3H]5-hydroxytryptamine release from rat brain cortex synaptosomes. Gobbi, M., Frittoli, E., Mennini, T. J. Pharm. Pharmacol. (1993) [Pubmed]

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