imidazoline receptor

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.

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

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.

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.

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

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

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.

Efaroxan is a potent, selective α2-adrenoceptor antagonist with oral activity and exhibits antidiabetic properties. It is also a selective antagonist for the I1-imidazoline receptor, making it useful in cardiovascular disease research.

Moxonidine Hydrochloride serves as a selective agonist for the imidazoline receptor subtype 1 and functions as an antihypertensive agent. It primarily acts within the central nervous system and demonstrates a significant preference for I1 imidazoline receptors over α2-adrenoceptors, with a 40-fold higher affinity. This compound effectively reduces stimulated norepinephrine overflow, indicating its potent efficacy. Despite similar agents like AGN192403 targeting the same receptor, moxonidine's dose-response efficacy remains unaffected. Its ability to lower blood pressure and reduce heart rate is distinctly mediated through imidazoline receptors, reliant on well-preserved noradrenergic pathways within the rostral ventrolateral medulla (RVLM). This interaction is potentially linked to a specific 42 kDa imidazoline receptor protein, emphasizing its unique mechanism of action compared to other drugs like clonidine.

Harmane-D is the deuterated form of Harmane. Harmane, a β-carboline alkaloid (BCA), acts as a potent neurotoxin, inducing marked tremors and psychiatric symptoms. It exhibits a high affinity for the I1 imidazoline receptor (IC50=30 nM), showing 1000 times more selectivity than for the α2-adrenergic receptor (IC50=18 μM). Additionally, Harmane (T3158) is an efficient and selective monoamine oxidase inhibitor, with IC50 values of 0.5 μM and 5 μM for MAO A and B, respectively.

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.

AGN 192403 is an imidazoline compound with affinity for imidazoline-1 receptors (imidazoline-1 receptors). It also exhibits neuroprotective properties.

Efaroxan hydrochloride is the salt form of Efaroxan, a selective, orally available α2-adrenoceptor antagonist that raises resting plasma insulin levels and significantly potentiates adrenaline-induced increases in insulin levels.

Allantoin-13C2,15N4 is a variant of Allantoin (T0925) labeled with 13C and 15N. Known as a skin conditioning agent, Allantoin (T0925) promotes skin health and stimulates the growth of new, healthy tissue.

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.

Highly selective I2 imidazoline receptor ligand

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

Cirazoline (free base) is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, and a nonselective antagonist to the α₂ adrenergic receptor. It is believed that this combination of properties could make cirazoline an effective vasoconstricting agent.