imidazoline

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

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

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.

Tetrahydrozoline hydrochloride (Murine Plus) is an imidazoline derivative with alpha receptor agonist activity.

Harman hydrochloride can directly induce CYP1A1 gene expression in an AhR-dependent manner and may represent a novel mechanism by which harman promotes mutagenicity, co-mutagenicity and carcinogenicity.

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

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.

Tolonidine is orally active and has been shown to possess hypotensive. Tolonidine is a derivative of imidazoline.

Idazoxan is an alpha2 receptor antagonist that also exhibits activity at imidazoline [I1] and [I2] receptors, playing a role in modulating dopamine release.

Metrazoline (o-Methyl-tracizoline) acts as a ligand for adrenergic receptors (low affinity) and imidazoline I2 receptors.

I2-IRs ligand-1 (Compound 12d) is an orally active compound capable of crossing the blood-brain barrier. It exhibits high affinity for imidazoline I2 receptors (I2-IRs) with a pKi of 9.98. This compound can enhance cognitive deficits in aging mice and possesses analgesic, anti-inflammatory, and neuroprotective properties. I2-IRs ligand-1 is applicable for research in Alzheimer's disease and related pain disorders.

Lysidine (2-Methyl-2-iMidazoline) is a nucleoside rarely seen outside of tRNA. Lysidine has better translation fidelity.

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.

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.

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.

Highly selective I2 imidazoline receptor ligand

L-Albizziin (2-Methoxyidazoxan monohydrochloride) is a highly potent selective antagonist of the alpha 2r adrenergic receptor, with little or no antagonistic effect on imidazoline. It has a significantly higher affinity for the alpha 2D adrenergic receptor (pKd9.7) in guinea pigs than for the alpha 2A adrenergic receptor (pKd8.2) in rabbits.

Aganodine is a guanidine that activates presynaptic imidazoline receptors. Aganodine inhibits the presynaptic release of norepinephrine through its agonism at imidazoline receptors.

S23757 is an imidazoline 1 receptor (I1R) selective ligand.

Dexisometheptene is an antimigraine drug candidate. Dexisometheptene significantly increases the pain threshold of acute pain response, and potently and selectively binds to receptors in the central nervous system known as imidazoline type-1 (I1) receptor

RX821002 is a potent and selective antagonist of α2-adrenoceptor with low affinity for imidazoline sites. RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively).

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

S 9871, also known as RX 801080, is an imidazoline derivative reported to antagonize imidazoline-stimulated insulin secretion.