i1-imidazoline receptor

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

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.

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

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

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.

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