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Apraclonidine is an α2-adrenergic receptor (α2-AR) agonist and structural analog of clonidine (Item No. 15949).1 It binds to α2-ARs in calf cortex, rat kidney, and rat spleen with IC50 values of 0.9, 4.3, and 4.2 nM, respectively. Apraclonidine also binds to α2-ARs in rat cerebral cortex, pig submandibular gland and lung tissue, and in dog kidney membrane (Kds = 0.87, 5.28, 1.30, and 5.25 nM, respectively).2,3 It inhibits noradrenaline-stimulated contraction in guinea pig ileum and rabbit vas deferens (EC50s = 7.59 and 6.76 nM, respectively).4 Opthalmic formulations containing apraclonidine have been used to treat elevated intraocular pressure.
WARNING This product is not for human or veterinary use.
1. [3H]Para-
2. Comparison of alpha-
3. Characterization of binding sites for [3H]-
4. Receptor interactions of a series of imidazolines: Comparison of the alpha 2-