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.

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.

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.

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

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

1-(3-Fluorophenyl)imidazoline-2-thione ,with CAS No. 17452-26-5, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. 1-(3-Fluorophenyl)imidazoline-2-thione provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

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

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

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

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.

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.

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.

RX 801077 (2 BFI free base), a selective imidazoline I2 receptor (I2R) agonist with a K_i value of 70.1 nM, demonstrates anti-inflammatory and neuroprotective properties, making it a potential research candidate for traumatic brain injury (TBI).

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.

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

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.

RS-79948-197 hemihydrate is a non-imidazoline α2-adrenoceptor antagonist. It exhibits Kd values of 0.42 nM, 0.18 nM, and 0.19 nM for rat α2A, α2B, and α2C receptors, respectively, and 0.60 nM, 0.46 nM, and 0.77 nM for human α2A, α2B, and α2C receptors.

Highly selective I2 imidazoline receptor ligand