Imidazoline Receptors
Imidazoles
Receptors, Drug
Receptors, Adrenergic, alpha-2
A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.
Adrenergic alpha-Antagonists
Rhinovirus-induced oxidative stress and interleukin-8 elaboration involves p47-phox but is independent of attachment to intercellular adhesion molecule-1 and viral replication. (1/68)
Virus-induced elaboration of proinflammatory cytokines is mediated by virus-induced oxidative stress. The purpose of these studies was to determine the source of the virus-induced oxidative stress. Inhibition of viral replication with antibody to intercellular adhesion molecule-1 had no effect on virus-induced oxidative stress or interleukin-8 (IL-8) response (597+/-88 vs. 668+/-78 pg/mL in control cells). Treatment of cells with diphenylene iodonium inhibited virus-induced oxidative stress and IL-8 elaboration, but allopurinol, ibuprofen, and rotenone had no effect. Studies in cell lines produced from a patient with gp91-phox deficiency revealed normal responses. In contrast, the oxidative response was decreased and the IL-8 concentration was 227+/-36 pg/mL in cells from a patient with p47-phox deficiency, compared with 664+/-48 pg/mL in control cells. These studies suggest that the stimulation of reactive oxygen species by viral challenge occurs at the cell surface even in the absence of viral replication and involves a flavoprotein that may act in concert with p47-phox. (+info)The binding of oxidized low density lipoprotein (ox-LDL) to ox-LDL receptor-1 reduces the intracellular concentration of nitric oxide in endothelial cells through an increased production of superoxide. (2/68)
Oxidized low density lipoprotein (ox-LDL) has been suggested to affect endothelium-dependent vascular tone through a decreased biological activity of endothelium-derived nitric oxide (NO). Oxidative inactivation of NO is regarded as an important cause of its decreased biological activity, and in this context superoxide (O(2)) is known to inactivate NO in a chemical reaction during which peroxynitrite is formed. In this study we examined the effect of ox-LDL on the intracellular NO concentration in bovine aortic endothelial cells and whether this effect is influenced by ox-LDL binding to the endothelial receptor lectin-like ox-LDL receptor-1 (LOX-1) through the formation of reactive oxygen species and in particular of O(2). ox-LDL induced a significant dose-dependent decrease in intracellular NO concentration both in basal and stimulated conditions after less than 1 min of incubation with bovine aortic endothelial cells (p < 0.01). In the same experimental conditions ox-LDL also induced O(2) generation (p < 0.001). In the presence of radical scavengers and anti-LOX-1 monoclonal antibody, O(2) formation induced by ox-LDL was reduced (p < 0.001) with a contemporary rise in intracellular NO concentration (p < 0.001). ox-LDL did not significantly modify the ability of endothelial nitric oxide synthase to metabolize l-arginine to l-citrulline. The results of this study show that one of the pathophysiological consequences of ox-LDL binding to LOX-1 may be the inactivation of NO through an increased cellular production of O(2). (+info)Reactive oxygen species production in association with suberization: evidence for an NADPH-dependent oxidase. (3/68)
In response to wounding, potato tubers generate reactive oxygen species (ROS) in association with suberization. Immediately following wounding, an initial burst of ROS occurs, reaching a maximum within 30 to 60 min. In addition to this initial oxidative burst, at least three other massive bursts occur at 42, 63 and 100 h post-wounding. These latter bursts are associated with wound healing and are probably involved in the oxidative cross-linking of suberin poly(phenolics). The source of ROS is likely to be a plasma membrane NADPH-dependent oxidase immunorelated to the human phagocyte plasma membrane oxidase. The initial oxidative burst does not appear to be dependent on new protein synthesis, but the subsequent bursts are associated with an increase in oxidase protein components. Oxidase activity is enhanced in vitro by hydroxycinnamic acids and conjugates associated with the wound healing response in potato. (+info)A new vasoconstrictor, a preliminary report. (4/68)
Otrivin,(R) a compound of the hydrochloride salt of phenyl-aminomethylimidazoline, was administered to 74 patients for varying periods as a nasal vasoconstrictor. Seventy-three had relief of nasal congestion for from five to six hours-longer periods than had been obtained with other vasoconstrictors they had used. No pressor effect was noted. (+info)Induction of defence gene expression by oligogalacturonic acid requires increases in both cytosolic calcium and hydrogen peroxide in Arabidopsis thaliana. (5/68)
Responses to oligogalacturonic acid (OGA) were determined in transgenic Arabidopsis thaliana seedlings expressing the calcium reporter protein aequorin. OGA stimulated a rapid, substantial and transient increase in the concentration of cytosolic calcium ([Ca2+]cyt) that peaked after ca. 15 s. This increase was dose-dependent, saturating at ca. 50 ug Gal equiv/ml of OGA. OGA also stimulated a rapid generation of H2O2. A small, rapid increase in H2O2 content was followed by a much larger oxidative burst, with H2O2 content peaking after ca. 60 min and declining thereafter. Induction of the oxidative burst by OGA was also dose-dependent, with a maximum response again being achieved at ca. 50 ug Gal equiv/mL. Inhibitors of calcium fluxes inhibited both increases in [Ca2+]cyt and [H2O2], whereas inhibitors of NADPH oxidase blocked only the oxidative burst. OGA increased strongly the expression of the defence-related genes CHS, GST, PAL and PR-1. This induction was suppressed by inhibitors of calcium flux or NADPH oxidase, indicating that increases in both cytosolic calcium and H2O2 are required for OGA-induced gene expression. (+info)Sensitization of tumor cells toward chemotherapy: enhancing the efficacy of camptothecin with imidazolines. (6/68)
Activation of nuclear transcription factor kappaB (NF-kappaB) by chemotherapeutic agents was found to protect cells from apoptosis. In light of its central role in regulating the cellular resistance to apoptotic agents, inhibition of NF-kappaB-mediated gene transcription may sensitize tumor cells to chemotherapeutic agents and enhance their efficacy. We describe herein a noncytotoxic imidazoline scaffold that sensitizes leukemia T cells to the chemotherapeutic agent camptothecin. No significant induction of apoptosis was found when cells were treated with the imidazoline; however, pretreatment of cells with this agent resulted in a drastic enhancement in efficacy of camptothecin (approximately 75-fold). Elucidation of the potential cellular mechanism revealed that the imidazoline prevents nuclear translocation of NF-kappaB. These findings indicate that inhibition of NF-kappaB by this imidazoline may present improved strategies in the chemotherapeutic treatment of cancer. (+info)Voltage- and NADPH-dependence of electron currents generated by the phagocytic NADPH oxidase. (7/68)
The phagocytic NADPH oxidase generates superoxide by transferring electrons from cytosolic NADPH to extracellular O2. The activity of the oxidase at the plasma membrane can be measured as electron current (I(e)), and the voltage dependence of I(e) was recently reported to exhibit a strong rectification in human eosinophils, with the currents being nearly voltage independent at negative potentials. To investigate the underlying mechanism, we performed voltage-clamp experiments on inside-out patches from human eosinophils activated with PMA. Electron current was evoked by bath application of different concentrations of NADPH, whereas slow voltage ramps (0.8 mV/ms), ranging from -120 to 200 mV, were applied to obtain 'steady-state' current-voltage relationships (I-V). The amplitude of I(e) recorded at -40 mV was minimal at 8 microM NADPH and saturated above 1 mM, with half-maximal activity (K(m)) observed at approx. 110 microM NADPH. Comparison of I-V values obtained at different NADPH concentrations revealed that the voltage-dependence of I(e) is strongly influenced by the substrate concentration. Above 0.1 mM NADPH, I(e) was markedly voltage-dependent and steeply decreased with depolarization within the physiological membrane potential range (-60 to 60 mV), the I-V curve strongly rectifying only below -100 mV. At lower NADPH concentrations the I-V curve was progressively shifted to more positive potentials and I(e) became voltage-independent also within the physiological range. Consequently, the K(m) of the oxidase decreased by approx. 40% (from 100 to 60 microM) when the membrane potential increased from -60 to 60 mV. We concluded that the oxidase activity depends on both membrane potential and [NADPH], and that the shape of the I(e)-V curve is influenced by the concentration of NADPH in the submillimolar range. The surprising voltage-independence of I(e) reported in whole-cell perforated patch recordings was most likely due to substrate limitation and is not an intrinsic property of the oxidase. (+info)Endothelin-1, superoxide and adeninediphosphate ribose cyclase in shark vascular smooth muscle. (8/68)
In vascular smooth muscle (VSM) of Squalus acanthias, endothelin-1 (ET-1) signals via the ET(B) receptor. In both shark and mammalian VSM, ET-1 induces a rise in cytosolic Ca(2+) concentration ([Ca(2+)](i)) via activation of the inositol trisphosphate (IP(3)) receptor (IP(3)R) and subsequent release of Ca(2+) from the sarcoplasmic reticulum (SR). IP(3)R-mediated release of SR Ca(2+) causes calcium-induced calcium release (CICR) via the ryanodine receptor (RyR), which can be sensitized by cyclic adeninediphosphate ribose (cADPR). cADPR is synthesized from NAD(+) by a membrane-bound bifunctional enzyme, ADPR cyclase. We have previously shown that the antagonists of the RyR, Ruthenium Red, high concentrations of ryanodine and 8-Br cADPR, diminish the [Ca(2+)](i) response to ET-1 in shark VSM. To investigate how ET-1 might influence the activity of the ADPR cyclase, we employed inhibitors of the cyclase. To explore the possibility that ET-1-induced production of superoxide (O(2)*-) might activate the cyclase, we used an inhibitor of NAD(P)H oxidase (NOX), DPI and a scavenger of O(2)*-, TEMPOL. Anterior mesenteric artery VSM was loaded with fura-2AM to measure [Ca(2+)](i). In Ca(2+)-free shark Ringers, ET-1 increased [Ca(2+)](i) by 104+/-8 nmol l(-1). The VSM ADPR cyclase inhibitors, nicotinamide and Zn(2+), diminished the response by 62% and 72%, respectively. Both DPI and TEMPOL reduced the response by 63%. The combination of the IP(3)R antagonists, 2-APB or TMB-8, with DPI or TEMPOL further reduced the response by 83%. We show for the first time that in shark VSM, inhibition of the ADPR cyclase reduces the [Ca(2+)](i) response to ET-1 and that superoxide may be involved in the activation of the cyclase. (+info)Imidazolines are a class of compounds with a heterocyclic imidazole ring, used in medical treatments for their vasoconstrictive, sedative, and anti-inflammatory properties, often found in decongestants, anesthetic adjuvants, and as antihistamine agents.
Imidazolines are a class of compounds with a heterocyclic ring containing two nitrogen atoms, one of which is part of an imidazole ring. In the context of medicine and pharmacology, imidazolines are commonly used as decongestants, vasoconstrictors, and as ingredients in some over-the-counter and prescription medications for the treatment of conditions such as allergic rhinitis, nasal congestion, and redness of the eyes.
Imidazoline compounds work by stimulating alpha-adrenergic receptors, which leads to vasoconstriction and decreased blood flow in the affected area. This can help to relieve symptoms such as nasal congestion and red, swollen eyes. However, it is important to note that imidazoline compounds can also have systemic effects when absorbed into the bloodstream, and may cause side effects such as dizziness, dry mouth, and sedation.
Some examples of imidazoline compounds used in medicine include tetrahydrozoline, oxymetazoline, and naphazoline. These compounds are available in various forms, including nasal sprays, eye drops, and oral medications. It is important to follow the instructions for use carefully and to talk to a healthcare provider if you have any questions or concerns about using imidazoline-containing products.
Imidazoline receptors are a type of G-protein coupled receptor that bind imidazoline compounds and play a role in various physiological functions, including blood pressure regulation, sleep regulation, and neuroprotection.
Imidazoline receptors are a type of G-protein coupled receptor (GPCR) that are widely distributed throughout the central and peripheral nervous system. They were initially identified through their ability to bind imidazoline compounds, but it is now known that they also bind a variety of other structurally diverse ligands.
There are three subtypes of imidazoline receptors: I1, I2, and I3. The I1 receptor is found in the brain and has been shown to play a role in regulating blood pressure, nociception (pain perception), and neuroprotection. The I2 receptor is also found in the brain and has been implicated in the regulation of dopamine release and the sleep-wake cycle. The I3 receptor is primarily located in the peripheral nervous system and has been shown to play a role in regulating insulin secretion and glucose metabolism.
Imidazoline receptors have attracted interest as potential therapeutic targets for a variety of conditions, including hypertension, pain, neurodegenerative disorders, and metabolic diseases. However, further research is needed to fully understand their functions and therapeutic potential.
Idazoxan is a nonselective alpha-2 adrenergic antagonist, which was previously used in research to study the role of alpha-2 receptors in various biological processes, but it is not commonly used in clinical practice due to its lack of specificity and side effects.
Idazoxan is not a medication that is commonly used in clinical practice, so it may not have a widely accepted "medical definition." However, I can provide some information about what idazoxan is and how it's been studied.
Idazoxan is an investigational drug that belongs to a class of medications called alpha-2 adrenergic receptor antagonists. These drugs work by blocking the action of certain chemicals in the brain called neurotransmitters, which can affect mood, behavior, and various physiological functions.
Idazoxan has been studied for its potential use in treating a variety of conditions, including depression, anxiety, and substance abuse disorders. It has also been investigated as a tool for studying certain aspects of brain function and neurotransmitter systems. However, it has not been approved by regulatory agencies such as the U.S. Food and Drug Administration (FDA) for any specific medical use.
It's worth noting that while idazoxan may have potential therapeutic uses, it is not without risks and side effects. Like many medications, it can interact with other drugs and may cause adverse reactions in some people. As such, it should only be used under the close supervision of a qualified healthcare provider.
'Benzofurans' are a class of organic compounds that consist of a furan ring (a five-membered aromatic heterocycle containing one oxygen atom) fused to a benzene ring.
Benzofurans are a class of organic compounds that consist of a benzene ring fused to a furan ring. The furan ring is a five-membered aromatic heterocycle containing one oxygen atom and four carbon atoms. Benzofurans can be found in various natural and synthetic substances. Some benzofuran derivatives have biological activity and are used in medicinal chemistry, while others are used as flavorings or fragrances. However, some benzofuran compounds are also known to have psychoactive effects and can be abused as recreational drugs.
Imidazoles are a class of heterocyclic organic compounds containing a 5-membered ring made up of two nitrogen atoms and three carbon atoms, which have significant therapeutic applications as antifungal agents, antibacterial agents, and in various other medical and industrial uses.
Imidazoles are a class of heterocyclic organic compounds that contain a double-bonded nitrogen atom and two additional nitrogen atoms in the ring. They have the chemical formula C3H4N2. In a medical context, imidazoles are commonly used as antifungal agents. Some examples of imidazole-derived antifungals include clotrimazole, miconazole, and ketoconazole. These medications work by inhibiting the synthesis of ergosterol, a key component of fungal cell membranes, leading to increased permeability and death of the fungal cells. Imidazoles may also have anti-inflammatory, antibacterial, and anticancer properties.
"Drug receptors are specialized proteins found on the surface of cells, to which drug molecules can bind, leading to a change in cell function and ultimately producing a pharmacological response."
Drug receptors are specific protein molecules found on the surface of cells, to which drugs can bind. These receptors are part of the cell's communication system and are responsible for responding to neurotransmitters, hormones, and other signaling molecules in the body. When a drug binds to its corresponding receptor, it can alter the receptor's function and trigger a cascade of intracellular events that ultimately lead to a biological response.
Drug receptors can be classified into several types based on their function, including:
1. G protein-coupled receptors (GPCRs): These are the largest family of drug receptors and are involved in various physiological processes such as vision, olfaction, neurotransmission, and hormone signaling. They activate intracellular signaling pathways through heterotrimeric G proteins.
2. Ion channel receptors: These receptors form ion channels that allow the flow of ions across the cell membrane when activated. They are involved in rapid signal transduction and can be directly gated by ligands or indirectly through G protein-coupled receptors.
3. Enzyme-linked receptors: These receptors have an intracellular domain that functions as an enzyme, activating intracellular signaling pathways when bound to a ligand. Examples include receptor tyrosine kinases and receptor serine/threonine kinases.
4. Nuclear receptors: These receptors are located in the nucleus and function as transcription factors, regulating gene expression upon binding to their ligands.
Understanding drug receptors is crucial for developing new drugs and predicting their potential therapeutic and adverse effects. By targeting specific receptors, drugs can modulate cellular responses and produce desired pharmacological actions.
Alpha-2 adrenergic receptors are G protein-coupled receptors that, when activated by catecholamines like norepinephrine and epinephrine, primarily mediate inhibitory responses, such as reducing the release of neurotransmitters or decreasing heart rate, via the activation of Gi/o proteins and subsequent inhibition of adenylyl cyclase.
Alpha-2 adrenergic receptors are a type of G protein-coupled receptor that binds catecholamines, such as norepinephrine and epinephrine. These receptors are widely distributed in the central and peripheral nervous system, as well as in various organs and tissues throughout the body.
Activation of alpha-2 adrenergic receptors leads to a variety of physiological responses, including inhibition of neurotransmitter release, vasoconstriction, and reduced heart rate. These receptors play important roles in regulating blood pressure, pain perception, and various cognitive and emotional processes.
There are several subtypes of alpha-2 adrenergic receptors, including alpha-2A, alpha-2B, and alpha-2C, which may have distinct physiological functions and be targeted by different drugs. For example, certain medications used to treat hypertension or opioid withdrawal target alpha-2 adrenergic receptors to produce their therapeutic effects.
Adrenergic alpha-antagonists, also known as alpha-blockers, are a class of medications that block the effects of adrenaline and noradrenaline at the alpha-adrenergic receptors, leading to vasodilation, decreased blood pressure, and a variety of other effects depending on the specific subtype of alpha receptor blocked.
Adrenergic alpha-antagonists, also known as alpha-blockers, are a class of medications that block the effects of adrenaline and noradrenaline at alpha-adrenergic receptors. These receptors are found in various tissues throughout the body, including the smooth muscle of blood vessels, the heart, the genitourinary system, and the eyes.
When alpha-blockers bind to these receptors, they prevent the activation of the sympathetic nervous system, which is responsible for the "fight or flight" response. This results in a relaxation of the smooth muscle, leading to vasodilation (widening of blood vessels), decreased blood pressure, and increased blood flow.
Alpha-blockers are used to treat various medical conditions, such as hypertension (high blood pressure), benign prostatic hyperplasia (enlarged prostate), pheochromocytoma (a rare tumor of the adrenal gland), and certain types of glaucoma.
Examples of alpha-blockers include doxazosin, prazosin, terazosin, and tamsulosin. Side effects of alpha-blockers may include dizziness, lightheadedness, headache, weakness, and orthostatic hypotension (a sudden drop in blood pressure upon standing).
Imidazoline
Three isomers are known, 2-imidazolines, 3-imidazolines, and 4-imidazolines. The 2- and 3-imidazolines contain an imine center ... whereas the 4-imidazolines contain an alkene group. The 2-Imidazoline group occurs in several drugs. Liu, H. and Du, D.-M. ( ... Imidazoline is a class of heterocycles formally derived from imidazoles by the reduction of one of the two double bonds. ... 2009), Recent Advances in the Synthesis of 2-Imidazolines and Their Applications in Homogeneous Catalysis. Adv. Synth. Catal., ...
2-Imidazoline
The 2-imidazolines are the most common imidazolines commercially, as the ring exists in some natural products and some ... Imidazoline receptor Imidazolidine Liu H, Du DM (March 2009). "Recent Advances in the Synthesis of 2-Imidazolines and Their ... 2-Imidazolines Clonidine Biimidazoline ligands and a complex. Second generation Grubbs' catalyst Spongotine B Cis-imidazolines ... Imidazoles can be prepared from dehydrogenation of imidazolines. As a structural analogue of 2-oxazolines, 2-imidazolines have ...
Imidazoline receptor
Imidazoline+Receptors at the U.S. National Library of Medicine Medical Subject Headings (MeSH) imidazoline receptor 2 at the U. ... Imidazoline receptors are the primary receptors on which clonidine and other imidazolines act. There are three main classes of ... imidazoline NISCH Head GA, Mayorov DN (January 2006). "Imidazoline receptors, novel agents and therapeutic potential". ... As of 2017, there are three known subtypes of imidazoline receptors: I1, I2, and I3. The I1 receptor appears to be a G protein- ...
Alpha-adrenergic agonist
Ruffolo, R. R. Jr.; Waddell, J. E. (1982). "Receptor interactions of imidazolines. IX. Cirazoline is an α1 adrenergic agonist ... Retrieved 2015-01-24.. Horie, K; Obika, K; Foglar, R (1995). "Selectivity of the imidazoline α-adrenoceptor agonists ( ... most selective agonist for alpha2-adrenergic as opposed to imidazoline-I1) Guanoxabenz (metabolite of guanabenz) Guanethidine ( ... mixed alpha2-adrenergic and imidazoline-I1 receptor agonist) Dexmedetomidine Fadolmidine Guanfacine, (preference for alpha2A- ...
Cirazoline
Ruffolo, R. R. Jr.; Waddell, J. E. (1982). "Receptor interactions of imidazolines. IX. Cirazoline is an α1 adrenergic agonist ... Horie, K; Obika, K; Foglar, R. (1995). "Selectivity of the imidazoline α-adrenoceptor agonists (oxymetazoline and cirazoline) ... Imidazolines, Phenol ethers, All stub articles, Biochemistry stubs). ...
Amidine
Imidazolines contain a cyclic amidine. A. W. Dox (1928). "Acetamidine Hydrochloride". Organic Syntheses. 8: 1. doi:10.15227/ ...
Muzafer Mujić
Mujić, M.; van Rossum, J. M. (June 1965). "Comparative pharmacodynamics of sympathomimetic imidazolines; studies on intestinal ... known for his contributions to classification of sympathomimetic drugs and comparative pharmacodynamics of imidazolines. He is ... interests included basic research in classification of sympathomimetic drugs and comparative pharmacodynamics of imidazolines. ...
Aganodine
... is a guanidine that activates presynaptic imidazoline receptors. Through its agonism at imidazoline receptors, ... Göthert, M.; Brüss, M.; Bönisch, H.; Molderings, G.J. (1999). "Presynaptic Imidazoline Receptors". Annals of the New York ... Molderings, GJ; Likungu, J; Jakschik, J; Göthert, M (1997). "Presynaptic imidazoline receptors and non-adrenoceptor 3H-idazoxan ...
Oxymetazoline
It can reduce nasal airway resistance (NAR) up to 35.7% and reduce nasal mucosal blood flow up to 50%. Since imidazolines are ... Like other imidazolines, Oxymetazoline is readily absorbed orally. Effects on α receptors from systemically absorbed ... DE 1117588, Fruhstorfer W, Müller-Calgan H, "2-(2,6-dimethyl-3-hydroxy-4-tert-butyl-benzyl)-2-imidazoline,and acid addition ... Imidazolines, Merck & Co. brands, Phenols, Schering-Plough brands, Tert-butyl compounds, Topical decongestants, ...
6-MeO-THH
October 2001). "beta-carboline binding to imidazoline receptors". Drug and Alcohol Dependence. 64 (2): 203-8. doi:10.1016/S0376 ... and imidazoline receptors. Beta-carboline Harmala alkaloid Tryptamine Shulgin A, Shulgin A (September 1997). TiHKAL: The ...
Alpha-2 adrenergic receptor
Imidazoline receptors occur in the nucleus tractus solitarii and also the centrolateral medulla. Clonidine is now thought to ... However, it is now known that clonidine binds to imidazoline receptors with a much greater affinity than α2 receptors, which ... Khan, ZP; Ferguson, CN; Jones, RM (February 1999). "alpha-2 and imidazoline receptor agonists. Their pharmacology and ...
Raymond P. Ahlquist
Ahlquist RP, Huggins RA, Woodbury RA (March 1947). "The pharmacology of benzyl-imidazoline (Priscol)". The Journal of ...
Tetryzoline
There is no antidote for tetryzoline or other similar imidazoline analogue poisoning, but the symptoms can be alleviated and ... Chemically, tetryzoline is a derivative of imidazoline. It has two enantiomers. Tetryzoline is the INN. An urban legend ... US 2731471, Synerholm M, Jules LH, Sahyun M, "Imidazoline Derivatives", issued 17 January 1956, assigned to Sahyun Laboratories ...
Lysidine (chemical)
Lysidine is a derivative of 2-imidazoline. It is a colorless solid with basic properties and soluble in organic solvents. It is ...
Idazoxan
"Participation of imidazoline receptors and alpha(2-)-adrenoceptors in the central hypotensive effects of imidazoline-like drugs ... Imidazoline antagonists, Benzodioxans, Imidazolines, All stub articles, Nervous system drug stubs). ... It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor. Idazoxan has ... US 2979511, Krapcho J, Lott WA, "Certain 1, 4-benzodioxanyl imidazolines and corresponding pyrimidines and process", issued 11 ...
Neosaxitoxin
All of them are related imidazoline guanidinium derivatives. NSTX, and other PSTs, are produced by several species of marine ...
Ethylenediamine
Some imidazoline-containing fungicides are derived from ethylenediamine. Ethylenediamine is an ingredient in the common ...
Secondary hypertension
Schäfer SG, Kaan EC, Christen MO, Löw-Kröger A, Mest HJ, Molderings GJ (July 1995). "Why imidazoline receptor modulator in the ...
NISCH
"Relationship between platelet imidazoline receptor-binding peptides and candidate imidazoline-1 receptor, IRAS". Annals of the ... June 2000). "Imidazoline receptor antisera-selected (IRAS) cDNA: cloning and characterization". DNA and Cell Biology. 19 (6): ... This gene encodes a nonadrenergic imidazoline-1 receptor protein that localizes to the inner layer of the plasma membrane as ... Imidazoline receptor GRCh38: Ensembl release 89: ENSG00000010322 - Ensembl, May 2017 "Human PubMed Reference:". National Center ...
Nutlin
... s are cis-imidazoline analogs which inhibit the interaction between mdm2 and tumor suppressor p53, and which were ... Imidazoline core based on the methoxyphenyl substituents also stabilizes p53. Vassilev LT, Vu BT, Graves B, Carvajal D, ... imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological ... "Synthetic Design and Biological Evaluation of New p53-MDM2 Interaction Inhibitors Based on Imidazoline Core". Pharmaceuticals. ...
Imidazolidinone
Imidazolones (also called imidazolinones) are oxo derivatives of imidazoline (dihydroimidazoles). Examples include imidazol-4- ...
Agmatine
Nicotinic, imidazoline I1 and I2, α2-adrenergic (no intrinsic activity-neither agonist nor antagonist), glutamate NMDAr, and ... Agmatine binds to α2-adrenergic receptor and imidazoline receptor binding sites, and blocks NMDA receptors and other cation ... imidazoline receptors subtypes, norepinephrine release and NO production. Agmatine hypoglycemic effects are the result of ... an endogenous ligand at imidazoline binding sites". British Journal of Pharmacology. 133 (6): 755-80. doi:10.1038/sj.bjp. ...
Clorgiline
ISBN 978-0-12-376350-1. Piletz JE, Halaris A, Ernsberger PR (1994). "Psychopharmacology of imidazoline and alpha 2-adrenergic ... and with very high affinity to the I2 imidazoline receptor (Ki = 40 pM). Clorgiline is also a multidrug efflux pump inhibitor. ...
Moxonidine
... is a selective agonist at the imidazoline receptor subtype 1 (I1). This receptor subtype is found in both the ... Moxonidine (INN) is a new-generation alpha-2/imidazoline receptor agonist antihypertensive drug licensed for the treatment of ... Compared to the older central-acting antihypertensives, moxonidine binds with much greater affinity to the imidazoline I1- ... Fairbanks CA, Wilcox GL (July 1999). "Moxonidine, a selective alpha2-adrenergic and imidazoline receptor agonist, produces ...
Lofexidine
Both contain an imidazoline ring and a 2,6-dichlorinated phenyl ring. The differences in structure are shown in red, while the ...
Mdm2
Inhibitors of the MDM2-p53 interaction include the cis-imidazoline analog nutlin. Levels and stability of Mdm2 are also ...
Oxazoline
Ishihara, Midori; Togo, Hideo (2007). "Direct oxidative conversion of aldehydes and alcohols to 2-imidazolines and 2-oxazolines ...
Efaroxan
... is an α2-adrenergic receptor antagonist and antagonist of the imidazoline receptor. The Darzens reaction between 2- ... Imidazolines, Alpha-2 blockers, All stub articles, Pharmacology stubs). ...
Imidazolidine
ISBN 978-0-85404-182-4. Ferm, R. J.; Riebsomer, J. L. From "The chemistry of the 2-imidazolines and imidazolidines" Chemical ... The intermediate, resulting from the addition of only two hydrogen atoms is called imidazoline (dihydroimidazole). The ...
Sharon Hammes-Schiffer
Additionally, her study of PCET in Iron Bi-imidazoline complexes has refined common comprehension of PCET, having proven her ... and Proton-Coupled Electron Transfer in Iron Bi-imidazoline Complexes". Journal of the American Chemical Society. 123 (16): ...
Imidazoline - Wikipedia
Three isomers are known, 2-imidazolines, 3-imidazolines, and 4-imidazolines. The 2- and 3-imidazolines contain an imine center ... whereas the 4-imidazolines contain an alkene group. The 2-Imidazoline group occurs in several drugs. Liu, H. and Du, D.-M. ( ... Imidazoline is a class of heterocycles formally derived from imidazoles by the reduction of one of the two double bonds. ... 2009), Recent Advances in the Synthesis of 2-Imidazolines and Their Applications in Homogeneous Catalysis. Adv. Synth. Catal., ...
2-Imidazoline, 2-(o-chlorobenzyl)-, hydrochloride
Chemical Database: 2-Imidazoline, 2-benzyl-, monohydrochloride (EnvironmentalChemistry.com)
This page contains information on the chemical 2-Imidazoline, 2-benzyl-, monohydrochloride including: 22 synonyms/identifiers. ... 2-Benzyl-2-imidazoline monohydrochloride*2-Imidazoline, 2-benzyl-, hydrochloride*2-Imidazoline, 2-benzyl-, monohydrochloride*4, ... 2-Imidazoline, 2-benzyl-, monohydrochloride. Identifications. *CAS Number: 59-97-2*Synonyms/Related:*1H-Imidazole, 4,5-dihydro- ... Chemical Database - 2-Imidazoline, 2-benzyl-, monohydrochloride. EnvironmentalChemistry.com. 1995 - 2023. Accessed on-line: 11/ ...
Characterization of Imidazoline Receptors in Blood Vessels for the Development of Antihypertensive Agents
The expression of imidazoline receptor on rat aorta was identified. However, guanidinium derivatives for detection of aortic ... Western blot analysis was used for detecting the expression of imidazoline receptor in tissues of Wistar rats. The isometric ... Meanwhile, only agmatine-induced relaxation was abolished by BU224, a selective antagonist of imidazoline I,sub,2,/sub,- ... Taken together, we suggest that agmatine can induce vascular relaxation through activation of peripheral imidazoline I,sub,2,/ ...
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Imidazoline (I3) Receptors. The signal peptide region is shown in purple The signal peptide region is shown in purple. ... Imidazoline (I3) Receptors. Of those, 18 and 39 patients were females and adult males, respectively Of those, 18 and 39 ... Imidazoline (I3) Receptors. The co-crystal structure of CCT251545 bound to CDK8/cyclin C revealed a loop region in the C- ... Imidazoline (I3) Receptors. The legislative history of the Bayh-Dole Act and the plain language of the statute establish that ...
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Oleyl Hydroxyethyl Imidazoline
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Imidazoline Corrosion Inhibitor Chemical for Oil & Gas Industry
Imidazoline corrosion inhibitor for use in oil & gas industry with strong annular heterocyclic structures as an efficient ... Chemistry behind Imidazoline. Imidazoline adherents to heterocyclic group of compounds which has five membered rings with two ... This Imidazoline chemistry is the basis for one of the dominating types of film-forming organic corrosion inhibitors in oil ... The other Imidazoline derivatives act as cationic surfactants, determined by the nature of hydrocarbon or substituent groups ...
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Homer-3 and mGluR1 (metabotropic glutamate receptor) are indicated predominantly about Purkinje cell dendritic spines (6). Antibodies had been screened by cell-based assays. The indirect immunofluorescence technique outcomes exposed anti-Homer-3 antibody titers of just one 1:3.2 in the CSF and 1:100 in the serum. The girl was certainly improved after antiviral and immunosuppression (immunoglobin, methylprednisolone and…. ...
Pyrromelletic Acid Diphenyl Imidazoline Salt 1:2 | CAS: 54553-91-2 | Vicura
We supply Pyrromelletic Acid Diphenyl Imidazoline Salt 1:2 (Vicura MC-55 / CAS: 54553-91-2) to manufacturers of powder coatings ... Vicura MC-55 (Pyrromelletic Acid Diphenyl Imidazoline Salt 1:2) is an off-white powder with the following chemical formula: C10 ... Vicura MC-55 (Pyromellitic Acid Diphenyl Imidazoline Salt) is an organic salt of polycarboxylic acid and cyclic amidine. It is ... Pyrromelletic Acid Diphenyl Imidazoline Salt , CAS: 54553-91-2 , Disclaimer. This information is supplied solely for ...
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Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
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Characterization of imidazoline receptors in blood vessels for the development of antihypertensive agents<...
Characterization of imidazoline receptors in blood vessels for the development of antihypertensive agents. / Chen, Mei Fen; ... Characterization of imidazoline receptors in blood vessels for the development of antihypertensive agents. In: BioMed Research ... Characterization of imidazoline receptors in blood vessels for the development of antihypertensive agents. BioMed Research ... The expression of imidazoline receptor on rat aorta was identified. However, guanidinium derivatives for detection of aortic ...
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Recently, imidazolines and oxazolines have shown great promise in proteosome inhibition. Previous research has led to the ... Furthermore, the mechanism can be easily modified to produce imidazolines, which have already been shown to regulate the ... It is anticipated that the oxazolines will function similar to imidazolines, and deregulate the proteosome, resulting in cancer ... Recently, imidazolines and oxazolines have shown great promise in proteosome inhibition. Previous research has led to the ...
Xylometazoline was the most potent imidazoline agonist, which was between 10- and 100-fold more potent than l-erythro...
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Alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role. Anaesthesia 1999;54:146-165. ... Alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role. Anaesthesia 1999;54:146-165. ... Alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role. . Anaesthesia. 1999. ;. 54. :. 146. -. 165 ... Alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role. . Anaesthesia. 1999. ;. 54. :. 146. -. 165 ...
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Irving PE[au] - Search Results - PubMed
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2-heteroaryl and 2-oxime ether series. Navas F 3rd, ... 2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2-heteroaryl compounds. Speake ... 2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2- ... 2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2- ...
ReceptorsAgonistDerivativesHydrochlorideSynthesisAgonistsDecongestantAdrenergicAdsorptionInhibitorsImidazolesCorrosion inhibitorOrganicCompoundsCompoundInhibitionMechanismDropsNeutralBlood pressureApplicationsProductGroupFunctionReceptorsLigandsClonidineMolecularAbstractBinding siteEffectsSystemPropertiesDataGoodProductsAlphaRecentChemicalModel
Receptors9
- Also, guanidinium derivatives show the ability to activate imidazoline receptors. (hindawi.com)
- Meanwhile, only agmatine-induced relaxation was abolished by BU224, a selective antagonist of imidazoline I 2 -receptors. (hindawi.com)
- Imidazoline receptors are introduced to play a role in cardiovascular regulation [ 2 , 3 ]. (hindawi.com)
- The clinical used antihypertensive agent rilmenidine may reduce blood pressure via an activation of imidazoline I 1 -receptors in brain to lower sympathetic tone [ 8 , 9 ]. (hindawi.com)
- It has been documented that compounds with guanidine-like structures may bind to imidazoline receptors [ 11 ]. (hindawi.com)
- As with other therapeutically used alpha2-agonists such as moxonidine and rilmenidine, clonidine possesses an imidazoline structure and is believed to lower blood pressure not only via central and peripheral alpha2-receptors, but perhaps even more so by acting on central "imidazoline I1 receptors" in the brain stem. (uni-wuerzburg.de)
- The molecular structure of these hypothetical "imidazoline I1 receptors" has not yet been identified. (uni-wuerzburg.de)
- In order to test whether ligands with an imidazoline structure elicit pharmacological effects via alpha2-adrenergic receptors or via "imidazoline receptors", mice were generated with a targeted deletion of all three alpha2-adrenergic receptor subtypes (alpha2ABC-KO). (uni-wuerzburg.de)
- Agmatine acts as an agonist at imidazoline and alpha-2-adrenergic receptors, also modulating NMDA receptor activity. (psicothema.com)
Agonist3
- Moxonidine is an I 1 ‐imidazoline receptor agonist that reduces blood pressure by inhibition of central sympathetic activity. (bps.ac.uk)
- Reverse the signs caused by the a2-adrenergic agonist imidazoline decongestant in the eye drops with a single dose of atipamezole and send the pet home. (aspcapro.org)
- Reverse the signs caused by the a2-adrenergic agonist imidazoline decongestant in the eye drops with atipamezole and keep Missy in hospital on fluids. (aspcapro.org)
Derivatives1
- The other Imidazoline derivatives act as cationic surfactants, determined by the nature of hydrocarbon or substituent groups attached to carbon or nitrogen atom of the heterocyclic ring. (chemtexltd.com)
Hydrochloride2
Synthesis1
- Liu, H. and Du, D.-M. (2009), Recent Advances in the Synthesis of 2-Imidazolines and Their Applications in Homogeneous Catalysis. (wikipedia.org)
Agonists3
- alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines. (nih.gov)
- 2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds. (nih.gov)
- The resulting templates 6 and 7 were particulary interesting as they lacked the N-H of most imidazole or imidazoline alpha-agonists. (acs.org)
Decongestant1
- The signs are very consistent with Oxymetazoline, which is an imidazoline decongestant. (aspcapro.org)
Adrenergic1
- The non-adrenergic imidazoline-1 receptor protein nischarin is a key regulator of astrocyte glutamate uptake. (neurotree.org)
Adsorption1
- Imidazoline corrosion inhibitor, an effective organic corrosion inhibitor used in acidic and aggressive environment, can form an adsorption film on the surface of metal, slowing down the diffusion of ions and inhibiting the occurrence of metal corrosion. (chemtexltd.com)
Inhibitors1
- This 'Imidazoline' chemistry is the basis for one of the dominating types of film-forming organic corrosion inhibitors in oil and gas installations globally. (chemtexltd.com)
Imidazoles2
- Imidazoline is a class of heterocycles formally derived from imidazoles by the reduction of one of the two double bonds. (wikipedia.org)
- Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. (nih.gov)
Corrosion inhibitor1
- 1）. Schercozoline O imidazoline is a water-in-oil emulsifier and corrosion inhibitor with an oleic fatty acid source. (fandachem.com)
Organic1
- Vicura MC-55 (Pyromellitic Acid Diphenyl Imidazoline Salt) is an organic salt of polycarboxylic acid and cyclic amidine. (vestachem.com)
Compounds1
- Imidazoline adherents to heterocyclic group of compounds which has five membered rings with two nitrogen atoms. (chemtexltd.com)
Compound2
- Benzene-1,2,4,5-tetracarboxylic acid, compound with 4,5-dihydro-2-phenyl-1H-imidazole (1:2) is also known as Pyromellitic acid di(2-phenyl-2-imidazoline) salt (1:2). (vestachem.com)
- The effects of an imidazoline compound (BL11282) on protein expression in rat pancreatic islets were investigated with a proteomic approach. (researchgate.net)
Inhibition1
- Recently, imidazolines and oxazolines have shown great promise in proteosome inhibition. (mnsu.edu)
Mechanism2
- The curing mechanism between Vicura MC-55 (Pyrromelletic Acid Diphenyl Imidazoline Salt 1:2) and the epoxy resin is complex. (vestachem.com)
- Furthermore, the mechanism can be easily modified to produce imidazolines, which have already been shown to regulate the proteosome and cause cancer cell death. (mnsu.edu)
Drops1
- Tetrahydrozoline is a form of a medicine called imidazoline, which is found in over-the-counter eye drops and nasal sprays. (medlineplus.gov)
Neutral1
- 2). Schercozoline O imidazoline is chemically described as 1-hydroxyethyl 2-alkyl imidazoline and is classified as a neutral agent that can easily be converted to a cationic agent. (fandachem.com)
Blood pressure1
- It has been indicated that activation of peripheral imidazoline I 2 -receptor (I-2R) may reduce the blood pressure in spontaneously hypertensive rats (SHRs). (hindawi.com)
Applications1
- These properties make Imidazolines one of the key intermediates for a variety of industrial applications. (chemtexltd.com)
Product1
- This month's survey of recent patent and research literature describes money-making ideas for personal care product development, including silicone resin waxes to modify texture and rheology, imidazoline for hair conditioning, gallnut and Eclipta prostrat a to minimize hair dye damage, renewable propanediol, and an in vitro measurement for SPF, among others. (cosmeticsandtoiletries.com)
Group4
- The 2- and 3-imidazolines contain an imine center, whereas the 4-imidazolines contain an alkene group. (wikipedia.org)
- The 2-Imidazoline group occurs in several drugs. (wikipedia.org)
- The nitrogen atom in the structure tends to provide some particular attributes like enhanced functional derivation, allowing the study of various functional group of Imidazoline radicals without effecting its paramagnetic properties. (chemtexltd.com)
- direct reaction between the imidazoline and the epoxy group and homopolymerization of the epoxy resin that is catalyzed by Vicura MC- 55. (vestachem.com)
Function1
- It is anticipated that the oxazolines will function similar to imidazolines, and deregulate the proteosome, resulting in cancer cell death. (mnsu.edu)
Receptors11
- Imidazoline receptors are orphan proteins and their biological function has primarily been established by binding of selective ligands, although their protein identity has yet to be determined. (tocris.com)
- Imidazoline receptors have a physiological role in the central regulation of blood pressure. (tocris.com)
- Despite the elusive nature of their molecular identities, recent progress on drug discovery targeting imidazoline receptors (I 1 and I 2 ) demonstrates the exciting potential of these compounds to elicit neuroprotection and to treat various disorders such as hypertension, metabolic syndrome, and chronic pain. (axonmedchem.com)
- The centrally acting muscle relaxant tizanidine has an imidazoline structure and binds not only to alpha(2)-adrenoceptors but also to imidazoline receptors. (nih.gov)
- The role of imidazoline receptors in the muscle-relaxant effect of tizanidine was studied using the alpha(2)-adrenoceptor/imidazoline receptor antagonist idazoxan and the alpha(2)-adrenoceptor antagonist yohimbine. (nih.gov)
- From these results, it is suggested that imidazoline receptors, but not alpha(2)-adrenoceptors, are involved in the supraspinal inhibitory effects of tizanidine on spinal reflexes, and at the spinal level, alpha(2)-adrenoceptors and imidazoline receptors are involved in the inhibitory effects of tizanidine. (nih.gov)
- Imidazoline I2 receptors are not well characterized. (nih.gov)
- Dexmedetomidine puts a bad chronotropic activity upon sinoatrial node cells through the initial regarding imidazoline receptors. (cd31-signal.com)
- Neuroprotective Effects of Dexmedetomidine against Thapsigargin-induced ER-stress via Activity of α2-adrenoceptors and Imidazoline Receptors[J]. AIMS Neuroscience, 2016, 3(2): 237-252. (aimspress.com)
- Significance of the imidazoline receptors in toxicology. (nih.gov)
- Receptors of CLONIDINE and other IMIDAZOLINES . (bvsalud.org)
Ligands2
Clonidine2
- Imidazoline binding sites were originally classified into I 1 sites (labeled by clonidine) and I 2 sites (labeled by idazoxan). (tocris.com)
- The ability of the α 2 -adrenoceptor agonist clonidine and the antagonist idazoxan to label a subpopulation of binding sites that was not displaceable by the endogenous ligand noradrenaline led to the discovery of the imidazoline binding sites some 25 y ago ( 1 ). (snmjournals.org)
Molecular1
- 4 Innopharma Screening Platform, BioFarma Research Group, Centro de Investigación en Medicina Molecular y Enfermedades Crónica (CIMUS), Universidad de Santiago de Compostela, E-15782, Santiago de Compostela, Spain. (nih.gov)
Abstract1
- abstract = "Imidazoline derivates have been synthesized from soybean oil fatty acids and some amines (diethylenetriamine (A), triethylenetetramine (B) and tetraethylenepentamine (C)) by condensation polymerization method. (ui.ac.id)
Binding site1
- The imidazoline 2 binding site (I 2 BS) is thought to be expressed in glia and implicated in the regulation of glial fibrillary acidic protein. (snmjournals.org)
Effects1
- FLIP down-regulation as well as caspase-8 activation and apoptosis induced by FasL were all inhibited by the NO-liberating agent sodium nitroprusside and dipropylenetriamine NONOate, whereas the NO synthase inhibitor aminoguanidine and NO scavenger 2-(4-carboxyphenyl)-4,4,5,5-tetramethyl-imidazoline-1-oxyl-3-oxide (PTIO) had opposite effects, indicating an anti-apoptotic role of NO in the Fas signaling process. (cdc.gov)
System1
- Imidazoline Receptor System: The Past, the Present, and the Future. (axonmedchem.com)
Properties1
- Dexmedetomidine is a potent and highly selective α 2 -adrenoceptor agonist with sedative, analgesic, and sympatholytic properties, though it also exhibits some affinity for imidazoline binding sites. (aimspress.com)
Data1
- Data of FT- IR shows several peaks with a ring imidazoline already formed. (ui.ac.id)
Good1
- Moderate concentration of SOFA/TEPA Imidazoline (IM C2) has good long terms corrosion inhibitor for mild steel at 5 wt. (ui.ac.id)
Products1
- It can be concluded that imidazoline derivatives products can be used as alternative corrosion inhibitor on mild steel. (ui.ac.id)
Alpha1
- The resulting templates 6 and 7 were particulary interesting as they lacked the N-H of most imidazole or imidazoline alpha-agonists. (acs.org)
Recent1
- Liu, H. and Du, D.-M. (2009), Recent Advances in the Synthesis of 2-Imidazolines and Their Applications in Homogeneous Catalysis. (wikipedia.org)
Chemical1
- Imidazoline Amphoteric Surfactant--Shanghai Fine Chemical Co., Ltd. (shfinechem.com)
Model1
- In this study, our aim was to determine the therapeutic potential of the powerful analgesic I2-imidazoline ligand CR4056 in the 5xFAD model of AD, since this ligand has been proven to be safely tolerated in humans. (nih.gov)
