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Imidazoline I₂ receptor density increases with the malignancy of human gliomas

¹ Department of Pharmacology, University of the Basque Country, E-48940 Leioa, Spain
² Neurosurgery Service, Cruces Hospital, Brakaldo, Bizkaia, Spain

Correspondence to:
Correspondence to:
Dr L F Callado
Department of Pharmacology, University of the Basque Country, E-48940 Leioa, Bizkaia, Spain; kfbcahel{at}lg.ehu.es

ABSTRACT
Background: Current glioma grading schemes are limited by subjective histological criteria. Imidazoline I₂ receptors are principally expressed on glial cells.

Objective: To investigate the feasibility of using the measurement of imidazoline I₂ receptor expression to differentiate glial tumours from other types of brain tumours and for grading the different gliomas.

Methods: The specific binding of [³H]idazoxan to imidazoline I₂ receptors was measured in homogenates from human gliomas of different grades.

Results: The density of imidazoline I₂ receptors was significantly greater in the three types of malignant glial tumours than in postmortem control brain or non-glial tumours. The increase in density correlated with the malignancy grade of the gliomas. No significant differences in affinity values were observed.

Conclusion: These results suggest that the density of imidazoline I₂ receptors may be a useful radioligand parameter for the differentiation of glial tumours from other types of brain tumours and for grading the different gliomas.

Keywords: imidazoline I2 receptors; human brain; gliomas

Abbreviations: GFAP, glial fibrillary acidic protein; I₂-IR, I₂ imidazoline receptor; i.p., intraperitoneally; PET, positron emission tomography