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
0 ImagesCat. No.: HY-100904ACAS No.: 72583-92-7Synonyms: 2 BFI free baseRX 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).
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Efaroxan
0 ImagesCat. No.: HY-B1416CAS No.: 89197-32-0Efaroxan is a potent, selective and orally active α2-adrenoceptor antagonist, with antidiabetic activity. Efaroxan is a selective I1-Imidazoline receptor antagonist. Efaroxan can be used for the research of cardiovascular disease.
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Moxonidine-133
0 ImagesCat. No.: HY-W767936Synonyms: BDF5895-133Moxonidine-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.
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RX 801077 hydrochloride (Standard)
0 ImagesSynonyms: 2 BFI (Standard)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).
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Metrazoline
0 ImagesCat. No.: HY-W714108CAS No.: 221225-04-3Synonyms: o-Methyl-tracizolineMetrazoline (o-Methyl-tracizoline) is the ligand for adrenergic receptor (low affinity) and imidazoline I2 receptor.
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RS 45041-190 hydrochloride
0 ImagesCat. No.: HY-101301ACAS No.: 204274-74-8RS 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).
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Efaroxan hydrochloride (Standard)
0 ImagesEfaroxan (hydrochloride) (Standard) is the analytical standard of Efaroxan (hydrochloride). This product is intended for research and analytical applications. Efaroxan hydrochloride is a potent, selective and orally active α2-adrenoceptor antagonist, with antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist. Efaroxan hydrochloride can be used for the research of cardiovascular disease.
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LNP 509
0 ImagesCat. No.: HY-188065CAS No.: 773839-36-4LNP 509 is a selective I1 imidazoline receptor ligand with a bovine pKi value of 6.27. LNP 509 exists mainly in the form of a more stable imine tautomer. Intracisternal administration of LNP 509 in anesthetized rabbits induces a dose-dependent decrease in mean arterial blood pressure. LNP 509 can be used in hypertension-related research.
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Lofexidine hydrochloride (Standard)
0 ImagesSynonyms: Baq-168 (Standard); MDL-14042 (Standard)Lofexidine (Baq-168) hydrochloride Standard is the analytical standard of Lofexidine hydrochloride (HY-B1052). This product is intended for research and analytical applications. 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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Moxonidine-d4
0 ImagesCat. No.: HY-B0374SCAS No.: 1794811-52-1Moxonidine-d4 (BDF5895-d4) is the deuterium 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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Moxonidine (Standard)
0 ImagesCat. No.: HY-B0374RCAS No.: 75438-57-2Synonyms: BDF5895 (Standard)Moxonidine (Standard) is the analytical standard of Moxonidine (HY-B0374). This product is intended for research and analytical applications. 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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Harmane-d4
0 ImagesCat. No.: HY-101392S2CAS No.: 2012598-89-7
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Rilmenidine hemifumarate (Standard)
0 ImagesCat. No.: HY-100490ARCAS No.: 207572-68-7Rilmenidine (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 .
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BU224 hydrochloride (Standard)
0 ImagesCat. No.: HY-101170RCAS No.: 205437-64-5BU224 (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.
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Cirazoline
0 ImagesCat. No.: HY-113985CAS No.: 59939-16-1Synonyms: LD 3098Cirazoline (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.
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Moxonidine hydrochloride (Standard)
0 ImagesSynonyms: BDF5895 hydrochloride (Standard)Moxonidine hydrochloride (Standard) is the analytical standard of Moxonidine hydrochloride (HY-B0374A). This product is intended for research and analytical applications. 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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Aganodine
0 ImagesCat. No.: HY-106504CAS No.: 86696-87-9Aganodine is a guanidine that activates presynaptic imidazoline receptors and can inhibit electrically evoked [3H]-norepinephrine release.
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Moxonidine-d3
0 ImagesCat. No.: HY-B0374S2Synonyms: BDF5895-d3Moxonidine-d3 (BDF5895-d3) is deuterium 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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S23757
0 ImagesCat. No.: HY-124926CAS No.: 208718-14-3S23757 is a selective imidazoline receptor antagonist that can prevent the hypotensive effect of imidazolines.
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Rilmenidine (Standard)
0 ImagesCat. No.: HY-100490RCAS No.: 54187-04-1Rilmenidine (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.
