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.
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Imidazoline Receptor Related Products (61)
Related Products (61)
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RX 801077 hydrochloride
0 ImagesSynonyms: 2 BFIRX 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).
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Harmane-d1
0 ImagesHarmane-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).
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Lofexidine-d4 hydrochloride
0 ImagesCat. No.: HY-B1052SCAS No.: 1206845-57-9Synonyms: Baq-168-d4; MDL-14042-d4Lofexidine-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.
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Harman-13C2,15N
0 ImagesCat. No.: HY-W777360CAS No.: 1189461-56-0Harman-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).
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Idazoxan
0 ImagesCat. No.: HY-14561CAS No.: 79944-58-4Synonyms: RX 781094Idazoxan (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.
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Harmane-d2
0 ImagesCat. No.: HY-101392S1Harmane-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).
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I2-IRs ligand-1
0 ImagesCat. No.: HY-170994I2-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.
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5-((2-Bromophenoxy)methyl)-4,5-dihydrooxazol-2-amine
0 ImagesCat. No.: HY-188066CAS No.: 359715-57-4S23515 is a highly selective I1 imidazoline receptor (I1R) agonist with a Ki value of 6.4 nM. S23515 modulates central cardiovascular functions, induces hypotension and bradycardia, shows no affinity for α-adrenergic receptors, and cannot cross the blood-brain barrier. S23515 inhibits oxidosqualene-lanosterol cyclase (OSC) and cholesterol synthesis, induces the production of (24S,25)-Epoxycholesterol (HY-W040150), and upregulates the expression of ABCA1 and ABCG1 in human macrophages. S23515 is applicable to research related to dyslipidemia and hypertension.
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Moxonidine-13C,d3 hydrochloride
0 ImagesCat. No.: HY-B0374ASSynonyms: BDF5895-13C,d3 hydrochlorideMoxonidine-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.
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BU226 hydrochloride
0 ImagesBU226 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.
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Agmatine-d8 hydrochloride
0 ImagesCat. No.: HY-101238SAAgmatine-d8 hydrochloride is the deuterated-labeled Agmatine-d8 hydrochloride. Agmatine hydrochloride 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.
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Agmatine-d8 sulfate
0 ImagesCat. No.: HY-101238SCAS No.: 909556-32-7Agmatine-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.
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N-(2-Chloro-4-iodophenyl)-2-methyl-3,4-dihydro-2H-pyrrol-5-amine
0 ImagesCat. No.: HY-188067CAS No.: 497180-72-0LNP-911 is a ligand for the I1 imidazoline receptor. LNP-911 allosterically modulates I1Rs and enhances the effect of agonists on Forskolin (HY-15371)-stimulated cAMP accumulation. LNP-911 exists mainly as a stable imine tautomer. After radioiodination, LNP-911 serves as a selective high-affinity radioligand for characterization studies of I1Rs in membrane preparations. LNP-911 can be used in hypertension-related research.
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Tracizoline
0 ImagesCat. No.: HY-182597CAS No.: 65248-90-0Tracizoline is an orally active I2-imidazoline receptor agonist. Tracizoline functionally modulates I2-imidazoline receptors, regulates hippocampal FADD cell fate adaptor, attenuates mechanical and thermal hyperalgesia, activates α2A-adrenergic receptors with very weak partial agonism, and induces antidepressant-like activity via 5-HT1A receptor activation. Tracizoline can be used for the research of inflammatory pain, neuropathic pain, and depression.
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Rilmenidine-d4
0 ImagesCat. No.: HY-100490SCAS No.: 85047-14-9Rilmenidine-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.
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Harmane (Standard)
0 ImagesHarmane (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.
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Moxonidine-d7
0 ImagesCat. No.: HY-B0374S1Synonyms: BDF5895-d7Moxonidine-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.
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Lofexidine-d4
0 ImagesCat. No.: HY-B1052S1CAS No.: 78302-26-8Synonyms: Baq-168 free base-d4; MDL-14042 free base-d4Lofexidine-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.
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AGN 192403
0 ImagesCat. No.: HY-101374CAS No.: 175521-95-6Synonyms: (+)-BRD4780 free baseAGN 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.
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Rilmenidine phosphate (Standard)
0 ImagesCat. No.: HY-100490BRCAS No.: 85409-38-7Rilmenidine (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 .
