Imidazoline Receptor

Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist.

Rilmenidine is a second-generation imidazoline-α2 adrenergic agonist.

Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). Moxonidine causes a decrease in sympathetic nervous system activity and, therefore, a decrease in blood pressure.

Idazoxan hydrochloride is an α2-AR adrenoceptor antagonist and potential I2 imidazoline receptor agonist. Also displays I1 imidazoline receptor antagonist activity. (pKi values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I1, I2, α 2A, α2B, and α 2C receptors respectively).

Moxonidine hydrochloride is a centrally acting antihypertensive agent.

Guanabenz acetate is an a2A-AR adrenergic agonist and IGRS (imidazoline I2 binding site) selective ligand.

KU14R is an antagonist of the pancreatic β-cell atypical imidazoline binding site (putative I3 receptor). KU14R has also been shown to selectively block efaroxan-induced insulin secretion.

Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist.