Ethyl-3H]RS-79948-197 alpha2-adrenoceptor autoradiography validation in alpha2-adrenoceptor knockout mice

European Journal of Pharmacology
Veronica FagerholmMika Scheinin

Abstract

[Ethyl-(3)H][8aR,12aS,13aS]-5,8,8a,9,10,11,12,12a,13,13a-decahydro-3-methoxy-12-(ethylsulfonyl)-6H-isoquino[2,1-g][1,6]naphthyridine ([ethyl-(3)H]RS-79948-197) was evaluated for alpha(2)-adrenoceptor autoradiography in brain sections from wild-type mice and alpha(2A)- and alpha(2ABC)-adrenoceptor knockout mice. Receptor numbers were 83% lower in cortex and 28% lower in caudate putamen of alpha(2A)-knockout mice than in wild-type mice. No specific binding was seen in alpha(2ABC)-knockout mice. [Ethyl-(3)H]RS-79948-197 saturation binding parameters were compared to those of [(3)H]2-(2,3-dihydro-2-methoxy-1,4-benzodioxan-2-yl)-4,5-dihydro-1H-imidazoline ([(3)H]RX821002) and [methyl-(3)H]17alpha-hydroxy-20alpha-yohimban-16beta-carboxylic acid methyl ester ([methyl-(3)H]rauwolscine). [Ethyl-(3)H-]RS-79948-197 detected a larger number of both alpha(2A)- and alpha(2B/C)-adrenoceptors than [(3)H]RX821002, while [methyl-(3)H]rauwolscine only underestimated the number of alpha(2A)-adrenoceptors. Oxymetazoline and prazosin competed for [ethyl-(3)H]RS-79948-197 binding with the expected rank order of affinities. Higher than necessary [ethyl-(3)H]RS-79948-197 concentrations resulted in a rapid increase in non-specific binding. Slow dissocia...Continue Reading

References

Feb 1, 1992·Pharmacology, Biochemistry, and Behavior·J K WamsleyD B Bylund
Aug 11, 1989·European Journal of Pharmacology·D LanginH Paris
May 30, 1997·Annals of the New York Academy of Sciences·C M MilliganP Towers

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Citations

May 20, 2003·European Journal of Pharmacology·Janne LähdesmäkiHeikki Mansikka
Apr 1, 2010·Basic & Clinical Pharmacology & Toxicology·Shawquia YoungMałgorzata Dukat
Nov 24, 2004·European Journal of Pharmacology·Veronica FagerholmMerja Haaparanta

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