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 (35):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-100904
    RX 801077 hydrochloride
    		Agonist 99.82%
    RX 801077 hydrochloride (2 BFI) is a selective imidazoline I2 receptor (I2R) agonist with a Ki value of 70.1 nM. RX 801077 hydrochlorideshows anti-inflammation and neuroprotection. RX 801077 hydrochloride has the potential for the research of traumatic brain injury (TBI).
    RX 801077 hydrochloride
  • 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-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-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>