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 (30):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-101374A
    AGN 192403 hydrochloride
    Antagonist
    AGN 192403 (BRD4780) hydrochloride is an I1-Imidazoline receptor antagonist for cardiovascular and neurological research.
    AGN 192403 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-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>