• Agonists 4-NEMD 7-Me-marsanidine (also I1 agonist) Agmatine (also I agonist, NMDA, 5-HT3, nicotinic antagonist and NOS inhibitor) Apraclonidine Brimonidine Cannabigerol (also acts as a moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist). (wikipedia.org)
  • Saw palmetto extract (SPE), used widely for the treatment of benign prostatic hyperplasia (BPH) has been shown to bind alpha(1)-adrenergic, muscarinic and 1,4-dihydropyridine (1,4-DHP) calcium channel antagonist receptors. (nih.gov)
  • The results suggest that lauric acid and oleic acid bind noncompetitively to alpha(1)-adrenergic, muscarinic and 1,4-DHP calcium channel antagonist receptors. (nih.gov)
  • Indoramin is an alpha-1 selective antagonist of adrenergic receptor, sold under trade names Baratol and Doralese, and now available as a generic. (ncats.io)
  • Prokinetic effect of indoramin, an alpha-adrenergic antagonist, on human gall-bladder. (ncats.io)
  • Chemistry/Storage/Stability/Compatibility - An alpha 2 -adrenergic antagonist, atipamezole HCl injection should be stored at room temperature (15°-30°C) and protected from light. (elephantcare.org)
  • Cirazoline is a full agonist at the α 1A adrenergic receptor , a partial agonist at both the α 1B and α 1D adrenergic receptors, [1] and a nonselective antagonist to the α 2 adrenergic receptor . (wikipedia.org)
  • The phenylephrine studies were repeated in seven hypertensive patients during treatment with prazosin, an alpha 1 adrenergic antagonist. (ox.ac.uk)
  • It is in a class of medications called centrally acting alpha 2A -adrenergic receptor agonists. (medlineplus.gov)
  • The H2 antagonists are highly selective, do not affect the H1 receptors, and are not anticholinergic agents. (medscape.com)
  • Synthesis and in vitro characterisation of N -[5-(4,5-dihydro-1 H -imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective α 1A receptor agonist. (rndsystems.com)
  • A-61603, a potent α 1 -adrenergic receptor agonist, selective for the α 1A receptor subtype. (rndsystems.com)
  • Scholars@Duke publication: Fetal terbutaline exposure causes selective postnatal increases in cerebellar alpha-adrenergic receptor binding. (duke.edu)
  • Despite the absence of body or brain growth impairment, selective increases were seen postnatally in cerebellar alpha 1- and alpha 2-receptor subtypes, whereas the same receptor populations were decreased by small amounts in cerebral cortex and midbrain + brainstem. (duke.edu)
  • The α1B mediates cardiac hypertrophy induced by non-selective α1-AR agonists like phenylephrine. (unc.edu)
  • We recently showed that an oral selective α1A agonist drug, dabuzalgron, preserves ATP content and mitochondrial function in mouse HF models. (unc.edu)
  • Guanabenz, an alpha2-selective adrenergic agonist and GADD34 functional inhibitor, was identified to enhance the efficacy of sunitinib by targeting GADD34-induced protective autophagy in glioblastoma cells, TMZ-resistant cells, hypoxic cultured cells, sphere-forming cells, and colony formation abilities. (tmu.edu.tw)
  • Midodrine, a selective alpha1 adrenergic agonist, exerts its actions by activating the alpha-adrenergic receptors of the arteriolar and venous vasculature, thus producing an increase in vascular tone and blood pressure. (scireproject.com)
  • beta-Adrenergic receptors showed little or no change in any region. (duke.edu)
  • Stuckey et al19 evaluated whether an 8-week and central alpha 2-1 and beta-adrenergic receptors. (bvsalud.org)
  • Pharmacology - Atipamezole competitively inhibits alpha 2 -adrenergic receptors, thereby acting as a reversal agent for alpha 2 -adrenergic agonists ( e.g. , medetomidine). (elephantcare.org)
  • Agmatine acts as an agonist at imidazoline and alpha-2-adrenergic receptors, also modulating NMDA receptor activity. (psicothema.com)
  • It is classified as a centrally acting alpha 2 adrenergic agonist and imidazoline receptor agonist and has been in clinical use since 1966. (uspharmacist.com)
  • The methylenedioxy amphetamine derivatives exhibited an inverse stereospecificity with respect to serotonin uptake sites versus postsynaptic 5-HT receptors with the S(+) isomer being more potent at the presynaptic recognition site, while the R(-) isomer was more potent at the postsynaptic recognition sites. (erowid.org)
  • These results show no evidence for a generalized change in alpha adrenergic responsiveness in hypertension and support the concept that increased blood pressure responses to alpha adrenergic stimulation in hypertensives are due to structural and geometric changes in the arterial wall rather than to an increased responsiveness of postsynaptic alpha adrenergic receptors. (ox.ac.uk)
  • Pretreatment with chlorethylclonidine, which selectively alkylates the alpha-1B subtype, did not affect the Emax value of phenylephrine-induced contractions, but significantly shifted the curve to the right. (aspetjournals.org)
  • phenylephrine decreases effects of iobenguane I 123 by receptor binding competition. (medscape.com)
  • Phenylephrine Hydrochloride Injection, USP is an alpha-1 adrenergic receptor agonist indicated for the treatment of clinically important low blood pressure resulting primarily from the dilation of blood vessels, which decreases blood pressure in the setting of anesthesia. (outsourcing-pharma.com)
  • Using the dorsal hand vein compliance technique we compared the changes in diameter of superficial veins in response to phenylephrine, an alpha 1 adrenergic receptor agonist, and to nitroglycerin, a venorelaxant, in patients with essential hypertension and in normotensive subjects. (ox.ac.uk)
  • Cooling augmented contractions evoked by the alpha 2-adrenergic agonists B-HT 920 and UK 14304 but did not affect responses to the full alpha 1-adrenergic agonist phenylephrine. (johnshopkins.edu)
  • Moreover, following partial irreversible blockade of the alpha 1-adrenoceptors with phenoxybenzamine, cooling also reduced the contractions evoked by phenylephrine. (johnshopkins.edu)
  • Therefore, cooling reduces alpha 1-adrenergic responsiveness in canine cutaneous veins, but in the case of full alpha 1-adrenergic agonists such as norepinephrine and phenylephrine the inhibitory effect of cooling is buffered by an alpha 1-adrenoceptor reserve. (johnshopkins.edu)
  • Antagonists of DA 1 receptors are SCH23390 and clozapine. (biopsychiatry.com)
  • Alpha antagonists and intraoperative floppy iris syndrome: A spectrum. (ncats.io)
  • The dorsal hand vein compliance technique is useful in detecting systemic effects of alpha adrenergic antagonists. (ox.ac.uk)
  • 1987, Interaction between morphine, an opioid agonist, and clonidine, an alpha-adrenergic agonist, on the regulation of anterior pituitary hormone secretion in normal male subjects. (wustl.edu)
  • Note that the two centrally-acting alpha-2 adrenergic receptor agonists, Intuniv (guanfacine, 2009) and Kapvay (clonidine, 2009), were previously approved for use in Hypertension in the late 1980's and early 1970's, as Tenex and Catapres, respectively. (tri-institute.org)
  • For example, the alpha-2A adrenergic receptor subtype is post-synaptic in the prefrontal cortex and these receptors strengthen cognitive and executive functions by inhibiting cAMP opening of potassium channels, thus enhancing prefrontal connections and neuronal firing. (wikipedia.org)
  • Receptor subtype involved in α 1A -adrenergic receptor-mediated Ca 2+ signaling in cardiomyocytes. (rndsystems.com)
  • The α-1D Is the predominant α-1-adrenergic receptor subtype in human epicardial coronary arteries. (rndsystems.com)
  • Knockout of the alpha 1A/C-adrenergic receptor subtype: the alpha 1A/C is expressed in resistance arteries and is required to maintain arterial blood pressure. (rndsystems.com)
  • The regional and subtype selectivity are compatible with primary deficits in the development of noradrenergic projections to the cerebellum identified in previous studies and provide further evidence that therapeutic use of beta-adrenergic agonists may produce neurobehavioral teratology. (duke.edu)
  • The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. (ncats.io)
  • Binding of indoramin to alpha1 receptors was studied using rat cerebral cortex membranes with [3H]prazosin to label alpha1 adrenoreceptors. (ncats.io)
  • Alpha adrenergic blockade during prazosin therapy. (ox.ac.uk)
  • This indicates that small doses of prazosin (1-2 mg) cause significant in vivo shifts in the dose-response relationship of alpha adrenergic agonists. (ox.ac.uk)
  • Cooling (from 37 to 24 degrees C) augmented contractions to norepinephrine under control conditions and after alpha 1-adrenergic blockade (prazosin) but not following alpha 2-adrenergic blockade (rauwolscine). (johnshopkins.edu)
  • The α2A-adrenergic agonist, guanfacine, is now used to treat prefrontal cortical cognitive disorders such as Attention Deficit Hyperactivity Disorder. (wikipedia.org)
  • Guanfacine extended-release tablets are a central alpha 2A -adrenergic receptor agonist indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) as monotherapy and as adjunctive therapy to stimulant medications (1, 14). (nih.gov)
  • A pharmacological profile of the methylenedioxy-substituted amphetamine derivatives indicates that MDMA and MDA exhibited highest affinity for serotonin uptake sites, 5-HT2 serotonin, alpha 2-adrenergic and M-1 muscarinic receptors. (erowid.org)
  • Salivary seromucous glands are regulated predominantly by parasympathetic activation of muscarinic receptors, resulting in exocrine secretion of mucins and macroglobulin responsible by lubrication and protection of oral mucosa 3-4 . (bvsalud.org)
  • A 61603 hydrobromide is a potent α -adrenoceptor agonist that is at least 35-fold more potent at α 1A than at α 1B or α 1D sites. (rndsystems.com)
  • The NBOMe compounds are highly potent 5HT2A receptor agonists and are also agonists at alpha-adrenergic receptors, which likely account for their serotonergic and sympathomimetic symptoms. (erowid.org)
  • Furthermore, 2,5-DMA derivatives exhibited agonist-like binding characteristics at 5-HT2 serotonin receptors with the R(-) isomer being the more potent isomer. (erowid.org)
  • Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α2-adrenergic receptor in the central and peripheral nervous systems. (wikipedia.org)
  • Activation of these receptors decreases peripheral resistance, inducing lowering of arterial blood pressure and increases in heart rate, sympathetic tone, and activity of the renin aldosterone system. (biopsychiatry.com)
  • Other behavioral, cardiovascular, and toxic effects of MDMA and related derivatives may be mediated by actions at other central and/or peripheral recognition sites, including muscarinic cholinergic receptors and alpha 2-adrenergic receptors, for which these compounds exhibit relatively high affinity. (erowid.org)
  • Dr. Beak discovered that the orphan nuclear receptor, RORα, is expressed in the mouse and human heart and mediates cardiac hypertrophy in response to angiotensin II. (unc.edu)
  • These agents are reversible competitive blockers of histamine at the H2 receptors, particularly those in the gastric parietal cells where they inhibit acid secretion. (medscape.com)
  • Except in special conditions, vasodilators and alpha- and beta-blockers are 3rd-line drugs, which if needed should be used after consultation with a specialist. (msdmanuals.com)
  • Kratom is an unscheduled opioid receptor agonist that comes in the form of dietary supplements currently being abused by chronic pain patients on prescription opioids. (erowid.org)
  • Active alkaloids isolated from kratom such as mitragynine and 7-hydroxymitragynine are thought to act on mu- and delta-opioid receptors as well as alpha-2 adrenergic and 5-HT2A receptors. (erowid.org)
  • Many pain physicians are not familiar with kratom and as providers who take care of high-risk chronic pain patients using prescribed opioids, knowledge of current unregulated opioid receptor agonists with abuse potential is of paramount importance. (erowid.org)
  • An agent that selectively binds to and activates alpha -adrenergic receptors. (ebi.ac.uk)
  • Isoproterenol acts as a biased agonist of the α-1A-adrenoceptor that selectively activates the MAPK/ERK pathway. (rndsystems.com)
  • It is also located on the vascular smooth muscle cells of certain blood vessels, such as those found in skin arterioles or on veins, where it sits alongside the more plentiful α1-adrenergic receptor. (wikipedia.org)
  • It is unclear whether this is caused by structural changes in the arterial wall or by hyperresponsiveness of vascular smooth muscle to endogenous alpha adrenergic agonists. (ox.ac.uk)
  • In the current study, pregnant rats were given 10 mg/kg of terbutaline on gestational days 17, 18 and 19 and adrenergic receptor binding capabilities examined in brain regions of the offspring. (duke.edu)
  • [3] Administration of cirazoline also seemed to present impairment in the spatial memory of monkeys through the activation of the same receptors that showed decreased food intake in rats. (wikipedia.org)
  • For this purpose, WIN 55,212-2 was injected in pregnant wistar rats from gestation day 5 to 20 and a detailed analysis of the levels of the neurotrophin brain-derived neurotrophic factor (BDNF) as well as of the signaling molecules extracellular signal-regulated kinase (ERK)1/2 and alpha-calcium/calmodulin-dependent protein kinase II (alpha-CaMKII) was carried out in adult offspring. (researchgate.net)
  • Furthermore, a robust reduction of total and phospho-alpha-CaMKII was found in the hippocampus of rats prenatally exposed to WIN 55,212-2. (researchgate.net)
  • The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. (wikipedia.org)
  • p90 ribosomal S6 kinases play a significant role in early gene regulation in the cardiomyocyte response to G(q)-protein-coupled receptor stimuli, endothelin-1 and α(1)-adrenergic receptor agonists. (rndsystems.com)
  • 2005, Molecular basis of inverse agonism in a G protein-coupled receptor. (wustl.edu)
  • Heart failure (HF) is characterized by markedly elevated levels of catecholamines that bind to adrenergic receptors (ARs) in the heart. (unc.edu)
  • It has been widely established that dopamine and its agonists play an important role in cardiovascular, renal, hormonal, and central nervous system regulation through stimulation of alpha and beta adrenergic and dopaminergic receptors. (biopsychiatry.com)
  • Bronchial epithelial cells were cultured with the short-acting β2-agonist salbutamol or the long-acting β2-agonist salmeterol prior to stimulation with HDE. (cdc.gov)
  • Cooling and alpha 1- and alpha 2-adrenergic responses in cutaneous veins: role of receptor reserve. (johnshopkins.edu)
  • Experiments were designed to determine the effects of cooling on alpha 1- and alpha 2-adrenergic responses in isolated canine cutaneous veins. (johnshopkins.edu)
  • By binding to specific receptor-sites these agents appear to potentiate the effects of gamma-aminobutyric acid (GABA) and facilitate inhibitory GABA neurotransmission and other inhibitory transmitters. (medscape.com)
  • Included in this class are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters. (ebi.ac.uk)
  • These experiments suggest that cooling augments alpha 2-adrenergic responsiveness without affecting alpha 1-adrenergic responsiveness. (johnshopkins.edu)
  • Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS. (rush.edu)
  • Derivatives of 2,5-DMA exhibited preferential high affinity at 5-HT2 serotonin receptors when compared to their relative affinities at 5-HT1 serotonin receptors. (erowid.org)
  • There were significant correlations between the in vitro affinities of 2,5-DMA derivatives at 5-HT2 serotonin receptors and their human hallucinogenic potencies as well as with their potencies in behavioral generalization studies, suggesting the importance of 5-HT2 serotonin receptors in mediating the hallucinogenic effects of the various 2,5-DMA derivatives. (erowid.org)
  • Similar to the 2,5-DMA derivatives, MDMA and MDA exhibited agonist-like binding characteristics at 5-HT2 serotonin receptors. (erowid.org)
  • The relatively weak hallucinogenic effects of the methylenedioxy-substituted amphetamine derivatives (when compared to the 2,5-DMA derivatives) may be mediated through actions at 5-HT2 serotonin receptors. (erowid.org)
  • In addition, the neurotoxic, psychotomimetic, analgesic, temperature regulation, and mood-altering effects of MDMA and other methylenedioxy-substituted derivatives may be mediated, in part, through their actions at other serotonin recognition sites in brain, including serotonin uptake sites and 5-HT1A serotonin receptors. (erowid.org)
  • Epinephrine belongs to a class of drugs called alpha-adrenergic and beta-adrenergic receptor agonists. (medicalnewstoday.com)
  • Also, in keeping with our convention, included are newly approved drugs for this indication, although they may have been previously approved for another indication, i.e ., the two alpha-2 adrenergic receptor agonists. (tri-institute.org)
  • A drug that mimics the effects of stimulating postganglionic adrenergic sympathetic nerves. (ebi.ac.uk)
  • However, the contractions evoked by the partial alpha 1-adrenergic agonist St 587 were virtually abolished by cooling. (johnshopkins.edu)
  • These agents stimulate alpha-adrenoreceptors in brain stem, activating an inhibitory neuron, which in turn results in reduced sympathetic outflow. (medscape.com)
  • This effect was associated with decreased activation of pathways linked to neurotrophin and glutamate receptor signaling. (researchgate.net)
  • β2-Agonist treatment significantly increased PKA activation and significantly decreased HDE-stimulated IL-6 and IL-8 production in a concentration- and time-dependent manner. (cdc.gov)
  • Brimonidine is an alpha adrenergic receptor agonist (primarily alpha-2). (aksci.com)
  • Brimonidine Tartrate Ophthalmic Solution is an alpha-adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. (biopharminternational.com)
  • Functional alpha-1B adrenergic receptors on human epicardial coronary artery endothelial cells. (rndsystems.com)
  • Functional characterisation of alpha(1)-adrenoceptors in denervated rat vas deferens. (ncats.io)
  • Using an established intranasal inhalation exposure model, we found that salbutamol pretreatment reduced airway neutrophil influx and IL-6, TNF-alpha, CXCL1, and CXCL2 release in bronchoalveolar lavage fluid following a one-time exposure to HDE. (cdc.gov)
  • Comment: Tricyclic antidepressants increase or decrease effects of sympathomimetics, by blocking reuptake of NE, or blocking uptake of indirect sympathomimetics into the adrenergic neuron. (medscape.com)
  • It has several general functions in common with the α1-adrenergic receptor, but also has specific effects of its own. (wikipedia.org)
  • Agonists (activators) of the α2-adrenergic receptor are frequently used in anaesthesia where they affect sedation, muscle relaxation and analgesia through effects on the central nervous system (CNS). (wikipedia.org)
  • Net pharmacologic effects are to reduce sedation, decrease blood pressure, increase heart and respiratory rates, and re-duce the analgesic effects of alpha 2 -adrenergic agonists. (elephantcare.org)
  • It has recently been demonstrated that prenatal exposure to the cannabinoid receptor 1 agonist (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinyl-methyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenylmethanone (WIN 55,212-2) produces memory deficit in adulthood, an effect associated with a reduced functionality of the glutamatergic system. (researchgate.net)
  • In summary, the present data suggest that deficits of BDNF levels and signaling through ERK1/2 and alpha-CaMKII might contribute to cognitive and neuroplastic defects associated with prenatal exposure to cannabinoids. (researchgate.net)
  • Together, these results support the need for future clinical investigations to evaluate the utility of ß2-agonist therapies in the treatment of airway inflammation associated with CAFO dust exposure. (cdc.gov)
  • Sunitinib, a multitargeted receptor tyrosine kinase inhibitor, is currently being tested as therapy for glioblastomas. (tmu.edu.tw)
  • The affinity of oleic acid, myristic acid and linoleic acid for each receptor was greater than the affinity of SPE. (nih.gov)
  • The pharmacological characteristics of alpha-1 and alpha-2 adrenergic receptors in young (6 month) and old (4.5-5 year) female rabbit urethra were studied using isolated muscle bath techniques. (aspetjournals.org)
  • Some species other than humans express a fourth α2D-adrenergic receptor as well. (wikipedia.org)
  • From a therapeutic point of view, the above-mentioned agonists are used for treating Parkinson's disease, acting over DA 2 dopaminergic receptors of the nigrostriatal system. (biopsychiatry.com)
  • Cardiac alpha (α)1-ARs have received less attention, however data from cell and animal studies indicate that they protect against the development of HF. (unc.edu)
  • Adrenergic alpha-2 Receptor Agonists" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (rush.edu)
  • Pharmacological characterization of alpha adrenergic receptors in the young and old female rabbit urethra. (aspetjournals.org)
  • Unlike 2,5-DMA derivatives, MDMA and MDA demonstrated little selectivity for 5-HT2 versus 5-HT1 subtypes of receptors. (erowid.org)