Tritium labelling and characterization of the potent imidazoline I1 receptor antagonist [5,7-3H] (+/-)-efaroxan at high specific activity.
(+/-)-Efaroxan 1 is a selective antagonist at the imidazoline I1 receptor. [3H] (+/-)-Efaroxan was required to explore its mechanism of action via receptor binding assay, and the radioligand was prepared by means of catalytic dehalogenation of a dibrominated precursor with tritium.
Egan
Judith A
JA
PerkinElmer Life and Analytical Sciences, Inc., 549 Albany St., Boston MA 02118, USA.
Filer
Crist N
CN
D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry*; D054755:Imidazoline Receptors; D007553:Isotope Labeling / Q000379:methods*; D009682:Magnetic Resonance Spectroscopy / Q000379:methods*; D011522:Protons; D011869:Radioligand Assay / Q000379:methods*; D011955:Receptors, Drug / Q000037:antagonists & inhibitors / Q000737:chemistry*; D014316:Tritium / Q000737:chemistry*
D001572:Benzofurans; D007093:Imidazoles; D054755:Imidazoline Receptors; D011522:Protons; D011955:Receptors, Drug; C410887:imidazoline I1 receptors; D014316:Tritium; C062597:efaroxan