Rilmenidine hemifumarate is an imidazoline I1 binding site (I1BS)-selective ligand (Ki = 7.1 nM), with much weaker affinity for I2BS (Ki = 5.2 μM). Rilmenidine hemifumarate also acts as an α2-adrenoceptor (α2-AR) agonist. Unlike clonidine (sc-203002), rilmenidine hemifumarate has greater selectivity for I1BS relative to α2-AR.
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