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 (40):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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
  • HY-100490S
    Rilmenidine-d4
    		Agonist
    Rilmenidine-d4 is the deuterium labeled Rilmenidine. 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[1][2][3].
    Rilmenidine-d<sub>4</sub>
  • HY-101392R
    Harmane (Standard)
    		Inhibitor
    Harmane (Standard) is the analytical standard of Harmane. This product is intended for research and analytical applications. 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.
    Harmane (Standard)
  • HY-B0374S1
    Moxonidine-d7
    		Agonist
    Moxonidine-d7 is deuterated labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
    Moxonidine-d<sub>7</sub>
  • HY-100904A
    RX 801077
    		Agonist
    RX 801077 (2 BFI free base) is a selective imidazoline I2 receptor (I2R) agonist with a Ki value of 70.1 nM. RX 801077 shows anti-inflammation and neuroprotection. RX 801077 has the potential for the research of traumatic brain injury (TBI).
    RX 801077
  • 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-B0374R
    Moxonidine (Standard)
    		Agonist
    Moxonidine (Standard) is the analytical standard of Moxonidine. This product is intended for research and analytical applications. Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
    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 [1][2][3].
    Rilmenidine hemifumarate (Standard)
  • HY-101238R
    Agmatine sulfate (Standard)
    		Agonist
    Agmatine (sulfate) (Standard) is the analytical standard of Agmatine (sulfate). This product is intended for research and analytical applications. 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 (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[1][2][3].
    BU224 hydrochloride (Standard)
  • 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-101392A
    Harmane hydrochloride
    		Inhibitor
    Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harmane hydrochloride
  • 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-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. Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
    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[1][2][3].
    Rilmenidine (Standard)
  • 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[1][2].
    Moxonidine-d<sub>4</sub>