1. Signaling Pathways
  2. 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 (54):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W714108
    Metrazoline
    Ligand
    Metrazoline (o-Methyl-tracizoline) is the ligand for adrenergic receptor (low affinity) and imidazoline I2 receptor.
    Metrazoline
  • HY-101301A
    RS 45041-190 hydrochloride
    RS 45041-190 hydrochloride is a high-affinity ligand for I2 imidazoline receptors, with the pKis of 8.66, 9.37, 9.32, and 8.85 in rat, rabbit, dog and baboon kidney, respectively. RS 45041-190 hydrochloride shows moderate potency for the inhibition of monoamine oxidase A in vitro (pIC50= 6.12), but had much lower potency for monoamine oxidase B (pIC50 = 4.47).
    RS 45041-190 hydrochloride
  • HY-B1416AR
    Efaroxan hydrochloride (Standard)
    Antagonist
    Efaroxan (hydrochloride) (Standard) is the analytical standard of Efaroxan (hydrochloride). This product is intended for research and analytical applications. 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.
    Efaroxan hydrochloride (Standard)
  • HY-B0374S
    Moxonidine-d4
    Agonist
    Moxonidine-d4 (BDF5895-d4) is the deuterium labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis.
    Moxonidine-d<sub>4</sub>
  • HY-B0374R
    Moxonidine (Standard)
    Agonist
    Moxonidine (Standard) is the analytical standard of Moxonidine (HY-B0374). This product is intended for research and analytical applications. Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis.
    Moxonidine (Standard)
  • HY-101392S2
    Harmane-d4
    Inhibitor
    Harmane-d4 is deuterium-labeled Harmane (HY-101392).
    Harmane-d<sub>4</sub>
  • HY-100490AR
    Rilmenidine hemifumarate (Standard)
    Inhibitor
    Rilmenidine (hemifumarate) (Standard) is the analytical standard of Rilmenidine (hemifumarate). This product is intended for research and analytical applications. 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 .
    Rilmenidine hemifumarate (Standard)
  • HY-101170R
    BU224 hydrochloride (Standard)
    Antagonist
    BU224 (hydrochloride) (Standard) is the analytical standard of BU224 (hydrochloride). This product is intended for research and analytical applications. BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research.
    BU224 hydrochloride (Standard)
  • HY-113985
    Cirazoline
    Agonist
    Cirazoline (LD 3098) is a doul agonist of Presynaptic imidazoline receptors (R(i-pre)) and α-adrenoceptor (R(α)). Cirazoline (30 μM) suppresses M current in SCG neurons cultured overnight.
    Cirazoline
  • HY-B0374AR
    Moxonidine hydrochloride (Standard)
    Agonist
    Moxonidine hydrochloride (Standard) is the analytical standard of Moxonidine hydrochloride (HY-B0374A). This product is intended for research and analytical applications. Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis.
    Moxonidine hydrochloride (Standard)
  • HY-106504
    Aganodine
    Activator
    Aganodine is a guanidine that activates presynaptic imidazoline receptors and can inhibit electrically evoked [3H]-norepinephrine release.
    Aganodine
  • HY-B0374S2
    Moxonidine-d3
    Agonist
    Moxonidine-d3 (BDF5895-d3) is deuterium labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis.
    Moxonidine-d<sub>3</sub>
  • HY-100490R
    Rilmenidine (Standard)
    Agonist
    Rilmenidine (Standard) is the analytical standard of Rilmenidine. This product is intended for research and analytical applications. 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.
    Rilmenidine (Standard)
  • HY-14561AR
    Idazoxan hydrochloride (Standard)
    Antagonist
    Idazoxan (hydrochloride) (Standard) is the analytical standard of Idazoxan (hydrochloride). This product is intended for research and analytical applications. 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 agents (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism.
    Idazoxan hydrochloride (Standard)