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 (54):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-100904
    RX 801077 hydrochloride
    		Agonist 99.20%
    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-101392S
    Harmane-d1
    		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).
    Harmane-d<sub>1</sub>
  • HY-B1052S
    Lofexidine-d4 hydrochloride
    		Agonist
    Lofexidine-d4 hydrochloride (Baq-168-d4) is the deuterium labeled Lofexidine hydrochloride (HY-B1052). Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal.
    Lofexidine-d<sub>4</sub> hydrochloride
  • 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).
    Harmane-d<sub>2</sub>
  • HY-170994
    I2-IRs ligand-1
    		Ligand
    I2-IRs ligand-1 (Compound 12d) is an orally active and BBB-penetrable compound. I2-IRs ligand-1 has a high affinity for imidazoline I2 receptors (I2-IRs) (pKi: 9.98). I2-IRs ligand-1 can improve cognitive impairment in senescent mice and exhibits analgesic, anti-inflammatory, and neuroprotective activities. I2-IRs ligand-1 can be used for the research of Alzheimer's disease and related pain disorders.
    I2-IRs ligand-1
  • HY-W777360
    Harman-13C2,15N
    		Inhibitor
    Harman-13C2,15N is 13C and 15N labeled Harmane. Harmane 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 also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harman-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-B0374AS
    Moxonidine-13C,d3 hydrochloride
    		Agonist
    Moxonidine-13C,d3 hydrochloride is 13C and deuterated labeled Moxonidine hydrochloride (HY-B0374A). 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-<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-101238S
    Agmatine-d8 sulfate
    Agmatine-d8 sulfate is a deuterium labeled Agmatine sulfate (HY-101238). 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-d<sub>8</sub> sulfate
  • 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.
    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 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>7</sub>
  • HY-B1052S1
    Lofexidine-d4
    		Agonist
    Lofexidine-d4 (Baq-168 free base-d4) is deuterium labeled Lofexidine (HY-B1052A). Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal.
    Lofexidine-d<sub>4</sub>
  • HY-101374
    AGN 192403
    		Antagonist
    AGN 192403 (BRD4780) is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 is also a TMED9 inhibitor. AGN 192403 shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 can be used for glioma tumor and neurological diseases research.
    AGN 192403
  • 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-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-W767936
    Moxonidine-133
    Moxonidine-13C,d3 (BDF5895-13C,d3) is the 13C-labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
    Moxonidine-<sup>13</supC,d<sub>3</sub>
  • HY-100904R
    RX 801077 hydrochloride (Standard)
    		Agonist
    RX 801077 (hydrochloride) (Standard) is the analytical standard of RX 801077 (hydrochloride) (HY-100904). This product is intended for research and analytical applications. 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 (Standard)