1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Imidazoline Receptor

Imidazoline Receptor

Imidazoline receptors are the primary receptors on which clonidine and other imidazolines act. There are three classes of imidazoline receptors: I1 receptor – mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure, (NISCH or IRAS, imidazoline receptor antisera selected), I2 receptor - an allosteric binding site of monoamine oxidase and is involved in pain modulation and neuroprotection, I3 receptor - regulates insulin secretion from pancreatic beta cells. Activated I1-imidazoline receptors trigger the hydrolysis of phosphatidylcholine into DAG. Elevated DAG levels in turn trigger the synthesis of second messengers arachidonic acid and downstreameicosanoids. In addition, the sodium-hydrogen antiporter is inhibited, and enzymes of catecholamine synthesis are induced. The I1-imidazoline receptor may belong to the neurocytokine receptorfamily, since its signaling pathways are similar to those of interleukins.

Imidazoline Receptor Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-N0543
    Allantoin
    Agonist 99.85%
    Allantoin is a skin conditioning agent that promotes healthy skin, stimulates new and healthy tissue growth.
  • HY-101238
    Agmatine sulfate
    Agonist ≥98.0%
    Agmatine sulfate 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.
  • HY-14561A
    Idazoxan hydrochloride
    Antagonist 98.21%
    Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like drugs (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism.
  • HY-100490A
    Rilmenidine hemifumarate
    Inhibitor ≥98.0%
    Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
  • HY-101392
    Harmane
    Inhibitor 99.81%
    Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect.
  • HY-101392S
    Harmane-d1
    Inhibitor
    Harmane-d1 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively).
  • HY-101392S1
    Harmane-d2
    Inhibitor
    Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively).
  • HY-B0374
    Moxonidine
    Agonist 99.72%
    Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
  • HY-100490B
    Rilmenidine phosphate
    Agonist ≥98.0%
    Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
  • HY-B1416A
    Efaroxan hydrochloride
    Antagonist
    Efaroxan hydrochloride is a potent, selective and orally active α2-adrenoceptor antagonist, with antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist. Efaroxan hydrochloride can be used for the research of cardiovascular disease.
  • HY-100490
    Rilmenidine
    Agonist
    Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
  • HY-B0374A
    Moxonidine hydrochloride
    Agonist
    Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
  • HY-B0374S
    Moxonidine-d4
    Agonist
    Moxonidine-d4 (BDF5895-d4) is the deuterium labeled Moxonidine. Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
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