2. Signaling Pathways
  3. Neuronal Signaling
  4. Imidazoline Receptor

Imidazoline Receptor

Imidazoline Receptor

Related Products

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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 (32):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0543
    Allantoin
    		Agonist 99.75%
    Allantoin is a skin conditioning agent that promotes healthy skin, stimulates new and healthy tissue growth.
    Allantoin
  • 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.
    Agmatine sulfate
  • HY-14561A
    Idazoxan hydrochloride
    		Antagonist 99.32%
    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
  • HY-101392
    Harmane
    		Inhibitor 99.91%
    Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) .
    Harmane
  • HY-100490A
    Rilmenidine hemifumarate
    		Inhibitor 99.82%
    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
  • HY-N0543R
    Allantoin (Standard)
    		Agonist
    Allantoin (Standard) is the analytical standard of Allantoin. This product is intended for research and analytical applications. Allantoin is a skin conditioning agent that promotes healthy skin, stimulates new and healthy tissue growth.
    Allantoin (Standard)
  • HY-100490BR
    Rilmenidine (phosphate) (Standard)
    		Agonist
    Rilmenidine (phosphate) (Standard) is the analytical standard of Rilmenidine (phosphate). This product is intended for research and analytical applications. 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 .
    Rilmenidine (phosphate) (Standard)
  • 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-B0374A
    Moxonidine hydrochloride
    		Agonist 99.83%
    Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
    Moxonidine hydrochloride
  • HY-B1416A
    Efaroxan hydrochloride
    		Antagonist 99.94%
    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
  • HY-N0543S
    Allantoin-13C2,15N4
    		99.90%
    Allantoin-13C2,15N4 is the 13C and 15N labeled Allantoin[1]. Allantoin is a skin conditioning agent that promotes healthy skin, stimulates new and healthy tissue growth[2].
    Allantoin-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N<sub>4</sub>
  • HY-B0374
    Moxonidine
    		Agonist 99.72%
    Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
    Moxonidine
  • 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 .
    Rilmenidine phosphate
  • HY-101392S
    Harmane-d
    		Inhibitor 98.01%
    Harmane-d 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)[1][2][3][4].
    Harmane-d
  • HY-101170
    BU224 hydrochloride
    		Antagonist
    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
  • HY-100490
    Rilmenidine
    		Agonist ≥99.0%
    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
  • HY-14561
    Idazoxan
    		Agonist
    Idazoxan (RX 781094) is a potent antagonist of α2 adrenergic receptor (α2AR) and potential I2 imidazoline receptor agonist. Idazoxan can be used in the research of antidepression and schizophrenia. Idazoxan has oral bioactivity.
    Idazoxan
  • 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)[1][2][3][4].
    Harmane-d<sub>2</sub>
  • HY-B0374AS
    Moxonidine-13C,d3 hydrochloride
    		Agonist
    Moxonidine-13C,d3 hydrochloride is 13C and deuterated labeled Moxonidine hydrochloride (HY-B0374A). Moxonidine (BDF5895) hydrochloride is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
    Moxonidine-<sup>13</sup>C,d<sub>3</sub> hydrochloride
  • HY-101380A
    BU226 hydrochloride
    		98.93%
    BU226 hydrochloride is a selective imidazoline 2 (I2) receptors ligand with an Ki of 1.4 nM for I2 and an IC50 of 534.5 nM for I1. BU226 hydrochloride can be used for researching antidepressant.
    BU226 hydrochloride