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Imidazoline receptor ligands act on the I1, I2 and I3 binding sites for imidazoline compounds. Imidazoline receptors were proposed when clonidine-like compounds were found to lower blood pressure through brainstem sites distinct from α2-adrenergic receptors. I1 sites take part in central blood pressure control, and I2 sites are linked to monoamine oxidase. I3 sites in pancreatic β cells are involved in the regulation of insulin secretion. Moxonidine hydrochloride and rilmenidine phosphate are listed as I1 agonists, and AGN 192403 as an I1 antagonist. Idazoxan hydrochloride blocks α2-adrenergic receptors and binds I2 sites, as does BU226 hydrochloride, while KU14R is an I3 antagonist. Clonidine hydrochloride and guanabenz acetate act mainly at α2-adrenergic receptors and are also listed under Adrenergic Receptors.
Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist.
Synonyms: Tenaxum; HYPERIUM
Rilmenidine is a second-generation imidazoline-α2 adrenergic agonist.
Synonyms: (+/-)-Idazoxan Monohydrochloride; RX 781094; RX 781094A
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).
Synonyms: Moxonidine hydrochloride CP; Moxonidine HCL; BDF-5895 HCL
Moxonidine hydrochloride is a centrally acting antihypertensive agent.
Guanabenz acetate is an a2A-AR adrenergic agonist and IGRS (imidazoline I2 binding site) selective ligand.
Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist.
