Imidazoline Receptor

Allantoin (Glyoxyldiureide), a urea hydantoin found in urine and plants, is used in dermatological preparations.

CR4056 (6-(1H-imidazol-1-yl)-2-phenylquinazoline) is a selective inhibitor of MAO-A with IC50 of 202.7 nM and a ligand of I2-imidazoline receptor with IC50 of 596 nM.

Harmane (Loturine) is a bio-active β-Carboline and monoamine oxidase inhibitor found in coffee and tobacco smoke.

BU 226 hydrochloride demonstrates affinity for imidazoline (I) receptors, in particular the I2 binding site with a Ki of 1.4 nM. BU 226 hydrochloride showed low (microM) affinity for alpha 2-adrenoceptors.

BU 224 hydrochloride is a selective imidazoline I(2) binding site ligand and has antinociceptive and antidepressant-like activities.

Rilmenidine hemifumarate (S-3341 hemifumarate) is a novel, orally active and selective I1 imidazoline receptor and α2-adrenoceptor agonist that induces autophagy, regulates the proliferation of leukaemia cells, stimulates the pro-apoptotic protein Bax, and induces autophagy in human leukaemia K5 cells. induces disruption of the mitochondrial pathway and apoptosis in human leukaemia K562 cells.

Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist, used to treat hypertension.

Idazoxan hydrochloride (RX 781094) is a benzodioxane-linked imidazole. It has alpha-2 adrenoceptor antagonist activity.

Moxonidine (BDF5895) is a selective agonist at the imidazoline receptor subtype 1, acting as an antihypertensive drug.

Agmatine sulfate (Agmatine sulfate salt) is a bioactive metabolite of the arginine amino acid. It exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.

2-BFI hydrochloride is a high-affinity agonist of I2-imidazoline receptor. 2-BFI hydrochloride can be used in studies about protection against stroke and acute inflammatory immune disease.