A specific category of drugs that prevent sleepiness by specifically targeting sleep-mechanisms in the brain. They are used to treat DISORDERS OF EXCESSIVE SOMNOLENCE such as NARCOLEPSY. Note that this drug category does not include broadly-acting central nervous system stimulants such as AMPHETAMINES.
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.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.
Cell-surface proteins that bind epinephrine and/or norepinephrine with high affinity and trigger intracellular changes. The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. Adrenergic receptors may also be classified according to the subtypes of G-proteins with which they bind; this scheme does not respect the alpha-beta distinction.
One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. They are found in the HEART, juxtaglomerular cells, and in the central and peripheral nervous systems.
A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.
One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS.
Drugs that selectively bind to and activate alpha adrenergic receptors.
A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.
Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
Drugs that selectively bind to and activate beta-adrenergic receptors.
A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
Drugs that bind to and activate adrenergic receptors.
AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.
Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.
Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
Compounds that bind to and activate ADRENERGIC BETA-1 RECEPTORS.
Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.
A highly selective and specific beta antagonist that is used to characterize beta-adrenoceptors.
Hydrogenated alprenolol derivative where the extra hydrogens are often tritiated. This radiolabeled form of ALPRENOLOL, a beta-adrenergic blocker, is used to label the beta-adrenergic receptor for isolation and study.
The active sympathomimetic hormone from the ADRENAL MEDULLA. It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. It is used in ASTHMA and CARDIAC FAILURE and to delay absorption of local ANESTHETICS.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.
Drugs that bind to and block the activation of ADRENERGIC BETA-1 RECEPTORS.
Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.
Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.
A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)
Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.
An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
Hypoxia-inducible factor 1, alpha subunit is a basic helix-loop-helix transcription factor that is regulated by OXYGEN availability and is targeted for degradation by VHL TUMOR SUPPRESSOR PROTEIN.
A beta-2 selective adrenergic antagonist. It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS.
Drugs that bind to and block the activation of ADRENERGIC BETA-3 RECEPTORS.
G-protein-coupled receptor kinases that mediate agonist-dependent PHOSPHORYLATION and desensitization of BETA-ADRENERGIC RECEPTORS.
A family of heterotrimeric GTP-binding protein alpha subunits that activate ADENYLYL CYCLASES.
A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.
A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
The relationship between the dose of an administered drug and the response of the organism to the drug.
The rate dynamics in chemical or physical systems.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
Drugs that act on adrenergic receptors or affect the life cycle of adrenergic transmitters. Included here are adrenergic agonists and antagonists and agents that affect the synthesis, storage, uptake, metabolism, or release of adrenergic transmitters.
Established cell cultures that have the potential to propagate indefinitely.
One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
... dopamine mainly triggers dopamine receptors and β1-adrenergic receptors while at high doses it works via α-adrenergic receptors ... Alpha-1 adrenergic receptor stimulation on vascular smooth muscle, leads to vasoconstriction and results in an increase in ... and β2 adrenergic receptors. Cruickshank, Laura; Kennedy, Alan R.; Shankland, Norman (2013). "Tautomeric and ionisation forms ... Dopamine binds to alpha-1 and beta-1 adrenergic receptors. Mediated through myocardial beta-1 adrenergic receptors, dopamine ...
Administering a norepinephrine receptor agonist (a substance that initiates a cell response when it binds with a receptor) to ... The alpha-1 adrenergic receptor is specifically implicated. Although it has not yet been thoroughly investigated, there is ... these findings are based on the effects of other commonly prescribed drugs that happen to block noradrenergic receptors. ... 1-2 weeks - the injury is very severe, and recovery is likely to take many months. The patient is likely to experience long- ...
Elliott, J. (1997). "Alpha-adrenoceptors in equine digital veins: Evidence for the presence of both alpha1 and alpha2-receptors ... "Effects of 3-Adrenergic Receptor Activation on Rat Urinary Bladder Hyperactivity Induced by Ovariectomy". Journal of ... Sagrada, A; Fargeas, M J; Bueno, L (1987). "Involvement of alpha-1 and alpha-2 adrenoceptors in the postlaparotomy intestinal ... ISBN 978-0-7817-7311-9. Schmitz, JM; Graham, RM; Sagalowsky, A; Pettinger, WA (1981). "Renal alpha-1 and alpha-2 adrenergic ...
... is an antagonist of the 5-HT2 and α1-adrenergic receptors. Villalobos-Molina, R; Ibarra, M; Hong, E (1995). "The 5- ... HT2 receptor antagonist, pelanserin, inhibits alpha 1-adrenoceptor-mediated vasoconstriction in vitro". European Journal of ...
alpha-2 adrenergic receptor agonist Decreases blood pressure and sympathetic nerve traffic. Clonidine,[12] Methyldopa[12] ... "Serum Activity Against G Protein-Coupled Receptors and Severity of Orthostatic Symptoms in Postural Orthostatic Tachycardia ... Alpha-2 adrenergic antagonist Increase blood pressure Yohimbine[111] Prognosis[edit]. POTS has a favorable prognosis when ... Especially elevations of adrenergic α1 receptor is associated with symptoms severity in patients with POTS.[55] ...
See also receptor antagonist) alpha-2 receptors. Agonists of alpha-2 receptors in the vascular smooth muscle lead to ... alpha-2 and beta-2 adrenergic receptors,. The main endogenous agonist of these cell receptors is norepinephrine (NE). The ... adrenergic receptors exert opposite physiologic effects in the vascular smooth muscle under activation: alpha-1 receptors. ... However, in clinical practice drugs applied intravenously that are agonists of alpha-2 receptors such as clonidine lead to ...
... all of which act as receptor antagonists of muscarinic acetylcholine receptors) are effective for treating asthma and COPD- ... Both of these medications activate alpha-1 adrenergic receptors that result in smooth muscle constriction. Non-selective beta ... Beta2-adrenergic agonists are recommended for bronchospasm. Short acting (SABA) Terbutaline Salbutamol Levosalbutamol Long ... Beta blockers bind into the β2 receptors and block the action of epinephrine and norepinephrine from binding to its receptors, ...
They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers ... inhibiting the downstream cellular signaling pathways of adrenergic receptors. However, there are exceptions: clonidine is an ... preventing postsynaptic adrenergic receptor activation and downstream signaling. Another way to inhibit adrenergic receptor ... adrenergic agonist at the α2 receptor; since this receptor is located presynaptically, agonism at this receptor inhibits the ...
alpha-1 adrenergic receptor activation, by norepinephrine, decreases glutamatergic excitatory postsynaptic potentials at AMPA ... receptors. The auditory cortex is the most highly organized processing unit of sound in the brain. This cortex area is the ... Dinh, L; Nguyen T; Salgado H; Atzori M (2009). "Norepinephrine homogeneously inhibits alpha-amino-3-hydroxyl-5-methyl-4- ... 27 (1): 180-9. doi:10.1523/JNEUROSCI.3227-06.2007. PMC 6672294. PMID 17202485. Kulynych, J. J.; Vladar, K.; Jones, D. W.; ...
... due to its higher affinity for the 5HT2A receptor over the D2 receptor. Antagonizing H1 histamine receptors causes sedation and ... Additionally, it also exhibits a relatively low affinity for serotonin 5-HT1, GABAA, beta-adrenergic receptors, and ... histamine H1 and alpha 1-adrenergic receptors in vitro". Schizophr. Res. 37 (1): 107-22. doi:10.1016/s0920-9964(98)00146-7. ... Olanzapine has a higher affinity for 5-HT2A serotonin receptors than D2 dopamine receptors, which is a common property of most ...
Day HE, Campeau S, Watson SJ, Akil H (July 1997). "Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic receptor mRNA ... and syncope are associated with the body's poor ability to control blood pressure without active alpha-adrenergic receptors. ... and α1D-receptor subtypes. These receptors are found on vascular smooth muscle, where they are responsible for the ... "Functional α1-adrenergic receptors on leukocytes of patients with polyarticular juvenile rheumatoid arthritis". Journal of ...
It was found to be an active Alpha-1 adrenergic receptor agonist in rabbit ear arteries. It has binding affinity towards 5-HT2C ... and 5-HT2A receptors in rats. It features competitive antagonist activity at 5-HT serotonin receptor in Sprague-Dawley rat ... It exhibits binding affinity against rat 5-hydroxytryptamine 2C receptors using [3H]mesulergine as a radioligand. As of October ... 2C-H exhibits agonist activity in vitro at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells ...
The potency of synephrine at adrenergic receptors of the β-class (regardless of sub-type) is much lower than at α-receptors. ... Although clearly indicating a selectivity of synephrine for α1 receptors, its potency at this receptor sub-class is still ... differences in activity at alpha-1 and alpha-2 adrenergic receptors". The Journal of Pharmacology and Experimental Therapeutics ... An adrenergic antagonist selective for α1 receptors. Reversal of reserpine-induced hypothermia by a drug is a classical test ...
... is a compound which acts as an antagonist at the α1B-adrenergic receptor. It was one of the first selective antagonists ... developed for this receptor and was invented in 1969, but is still commonly used in research into adrenergic receptors, ... March 2000). "Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety". Pharmaceutica Acta Helvetiae ... Morrow AL, Creese I (April 1986). "Characterization of alpha 1-adrenergic receptor subtypes in rat brain: a reevaluation of [3H ...
Increased level of norepinephrine increases the basal activity of alpha-2 adrenergic receptors, which mediate an analgesic ... Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... the α1A-adrenergic, the histamine H1 and the M1-M5 muscarinic acetylcholine receptors (see the Table on the right). ... Jang SW, Liu X, Chan CB, Weinshenker D, Hall RA, Xiao G, Ye K (June 2009). "Amitriptyline is a TrkA and TrkB receptor agonist ...
... and alpha 2-adrenergic receptors". Journal of Medicinal Chemistry. 37 (15): 2328-33. doi:10.1021/jm00041a011. PMID 7914537. ... which may have selectivity for the different subtypes of the alpha-2 receptor. It has two isomers, with the (S) isomer being ... 4-NEMD is a potent sedative drug which acts as a selective alpha-2 adrenergic agonist. It is closely related to dexmedetomidine ... September 1997). "Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of ...
Especially elevations of adrenergic α1 receptor is associated with symptoms severity in patients with POTS. If POTS is caused ... A high number of patients has elevated levels of autoantibodies against the adrenergic alpha 1 receptor and against the ... August 2020). "Serum Activity Against G Protein-Coupled Receptors and Severity of Orthostatic Symptoms in Postural Orthostatic ... April 1999). "Abnormal norepinephrine clearance and adrenergic receptor sensitivity in idiopathic orthostatic intolerance". ...
It has mainly been used to investigate the role of α1B receptors in the regulation of blood pressure. The α1B receptor is also ... Hillman KL, Doze VA, Porter JE (June 2007). "Alpha1A-adrenergic receptors are functionally expressed by a subpopulation of ... alpha(1D)-, and alpha(2)-adrenoceptors". European Journal of Pharmacology. 613 (1-3): 86-92. doi:10.1016/j.ejphar.2009.04.011. ... a potent and selective alpha1b adrenergic receptor antagonist ". Journal of Medicinal Chemistry. 41 (8): 1205-8. doi:10.1021/ ...
Leibel's initial research was focused on adrenergic receptor-mediated effects on lipolysis, and on the control of fatty acid re ... Phi Beta Kappa Alpha Omega Alpha Austen-Colgate Scholar NIH Postdoctoral Fellowship Rockefeller Scholar in Clinical Science ... "Constitutive and impaired signaling of leptin receptors containing the Gln --> Pro extracellular domain fatty mutation". Proc ... February 1997). "Molecular genetic analysis of a human neuropeptide Y receptor. The human homolog of the murine "Y5" receptor ...
... alpha}2-Adrenergic Receptor Subtypes Archived 2011-03-05 at the Wayback Machine J. Pharmacol. Exp. Ther. 322: pp. 214-221 (July ... Ephedrine works by increasing the activity of the α and β adrenergic receptors. Ephedrine was first isolated in 1885 and came ... of the adrenergic receptor system by increasing the activity of norepinephrine at the postsynaptic α and β receptors. The ... on adrenergic receptors. It is most usually marketed as the hydrochloride or sulfate salt. Ephedrine exhibits optical isomerism ...
... adrenergic receptors), second messenger generators (adenylate cyclase, phospholipase C), G proteins (RhoA, G alpha), kinases ( ... The Notch receptor and cell-signaling pathway have been demonstrated to be essential to vasculogenesis and the formation of ... So there is a difference in the distribution of the various adrenergic receptors that explains the difference in why blood ... These invaginations in the sarcoplasm contain a host of receptors (prostacyclin, endothelin, serotonin, muscarinic receptors, ...
Increased alpha-adrenergic receptor activity in epicardial coronary arteries or the excessive release of the "flight or fight" ... of beta receptors such as propranolol which may theoretically worsen vasospasm by inhibiting beta-2 adrenergic receptor's ... "Prinzmetal's variant form of angina as a manifestation of alpha-adrenergic receptor-mediated coronary artery spasm: ... and blocker of alpha-1 adrenergic receptors such as prazosin (which when activated cause vasodilation) but studies are needed ...
However, the most common type of alpha blocker is usually an α1 blocker. Non-selective α-adrenergic receptor antagonists ... and alpha 2-adrenergic receptors". The FASEB Journal. 6 (3): 832-839. doi:10.1096/fasebj.6.3.1346768. PMID 1346768. S2CID ... are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha- ... This is done by binding to the alpha receptors in smooth muscle or blood vessels. α-blockers can bind both reversibly and ...
Angiotensin receptor blockers (ARB) and calcium channel blockers (CCB), alpha- and beta- adrenergic receptor blockers ... Silodosin shows high affinity and selectivity for alpha-1a adrenergic receptors found in the prostate which ensures that it ... DrugDigest - Alpha blockers RxList.com - Tamsulosin alpha-Adrenergic+Blockers at the US National Library of Medicine Medical ... Silodosin is the most selective for alpha-1a receptors. The affinity and selectivity for alpha-1 receptors seems to be ...
Giovannitti JA, Thoms SM, Crawford JJ (2015-03-01). "Alpha-2 adrenergic receptor agonists: a review of current clinical ... specifically at the 5-HT1A and 5-HT1B G-protein coupled receptors. Additionally, the effect of MDMA on alpha-2 receptors is ... Neurochemically, MDMA activates 5-hydroxytryptamine, or 5-HT serotonin receptors, ... 62 (1): 31-9. doi:10.2344/0003-3006-62.1.31. PMC 4389556. PMID 25849473. Lee N. "Weekly Dose: ecstasy, the party drug that ...
The potency of synephrine at adrenergic receptors of the β-class (regardless of sub-type) is much lower than at α-receptors. ... Another receptor-oriented study by Wikberg revealed that synephrine (stereochemistry unspecified) was a more potent agonist at ... differences in activity at alpha-1 and alpha-2 adrenergic receptors." J. Pharmacol. Exp. Ther. 224 559-566. ... J. E. S. Wikberg (1978). "Pharmacological classification of adrenergic α receptors in the guinea pig." Nat. 273 164-166. ...
Hillman KL, Doze VA, Porter JE (2007). „Alpha1A-adrenergic receptors are functionally expressed by a subpopulation of cornu ... Görnemann T, Villalón CM, Centurión D, Pertz HH (2009). „Phenylephrine contracts porcine pulmonary veins via alpha(1B)-, alpha( ... a potent and selective alpha1b adrenergic receptor antagonist ". Journal of Medicinal Chemistry. 41 (8): 1205-8. PMID 9548811. ... Yang XP, Chiba S (2002). „Effects of L-765,314, a selective and potent alpha 1B-adrenoceptor antagonist, on periarterial nerve ...
... has been found to bind with high to moderate affinity to the receptors alpha-1 and alpha-2 adrenergic, 5-HT7- and 5- ... Repinotan acts as a selective high-affinity full receptor agonist at the 5-HT1A receptor subtype.[12] It increases the activity ... Other drugs included zonampanel, which acts as an AMPA receptor antagonist instead of a 5-HT1A receptor agonist and DP-b99. DP- ... Repinotan HCI (BAYx3702) acts as a highly selective 5-HT1A receptor full agonist. It is blocked by the specific 5-HT1A receptor ...
Klein U, Ramirez MT, Kobilka BK, von Zastrow M (Aug 1997). "A novel interaction between adrenergic receptors and the alpha- ... "Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor ... The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic ... McClue SJ, Milligan G (Sep 1990). "The alpha 2B adrenergic receptor of undifferentiated neuroblastoma x glioma hybrid NG108-15 ...
1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ... adrenergic receptor activity. • protein binding. • alpha1-adrenergic receptor activity. Cellular component. • integral ...
Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ... In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more ... α1-Adrenergic receptors are members of the G protein-coupled receptor superfamily. Upon activation, a heterotrimeric G protein ...
Anti-alpha 1 Adrenergic Receptor/ADRA1 antibody (ab3462) has been cited in 10 publications. References for Human in ICC/IF, IHC ... Sloniecka M et al. Expression Profiles of Neuropeptides, Neurotransmitters, and Their Receptors in Human Keratocytes In Vitro ... Ives SJ et al. Heat and a1-adrenergic responsiveness in human skeletal muscle feed arteries: the role of nitric oxide. J Appl ... Novielli NM et al. Pre-diabetes augments neuropeptide Y1- and a1-receptor control of basal hindlimb vascular tone in young ZDF ...
alpha 1 Adrenergic Receptor ELISA Kits vergleichen und bestellen. ... alpha 1 Adrenergic Receptor ELISA Kits für viele Reaktivitäten ... and adrenergic receptors on stage of maturation in neonatal calves and emphasize the association of alpha1-adrenergic receptor ... alpha-1C adrenergic receptor , adrenergic alpha 1c receptor , adrenergic receptor alpha 1c subtype , adrenergic receptor, alpha ... adrenergic, alpha-1A-, receptor variant 5 , adrenergic, alpha-1A-, receptor variant 8 , alpha-1A adrenergic receptor , alpha-1A ...
Alpha-1 adrenergic receptor: binding and phosphoinositide breakdown in human myometrium.. M Breuiller-Fouche, F Doualla-Bell ... Alpha-1 adrenergic receptor: binding and phosphoinositide breakdown in human myometrium.. M Breuiller-Fouche, F Doualla-Bell ... Alpha-1 adrenergic receptor: binding and phosphoinositide breakdown in human myometrium.. M Breuiller-Fouche, F Doualla-Bell ... Alpha-1 adrenergic receptor: binding and phosphoinositide breakdown in human myometrium. Message Subject (Your Name) has ...
... expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c. Biochem Biophys Res Commun ... Knockout of the alpha 1A/C-adrenergic receptor subtype: the alpha 1A/C is expressed in resistance arteries and is required to ... The alpha(1A/C)- and alpha(1B)-adrenergic receptors are required for physiological cardiac hypertrophy in the double-knockout ... Transgenic mice with cardiac overexpression of alpha1B-adrenergic receptors. In vivo alpha1-adrenergic receptor-mediated ...
Despite the preponderance of alpha-2 receptors, the alpha receptor mediating renal vasoconstriction appears to be of the alpha- ... 3H]Dihydroergocryptine, a nonselective alpha adrenergic antagonist, the alpha-1 selective antagonist, [3H]prazosin and the ... the alpha receptor mediating renal arteriolar vasoconstriction appeared to be of the alpha-1 subtype as there was a close ... To establish a correlation between binding and a biological function, the ability of alpha adrenergic agents to stimulate or ...
BACKGROUND: Circulating agonistic autoantibodies acting at G protein-coupled receptors have been associated with numerous sever ... adrenergic receptor cause vascular impairments in rat brain as demonstrated by magnetic resonance angiography View in MDC ... adrenergig receptor either induced by immunization with a receptor peptide or applied by intravenous injection. The vasculature ... METHODOLOGY/PRINCIPAL FINDINGS: Using a rat model we studied the long-term action of antibodies against the alpha(1)- ...
Expression of alpha 1 adrenergic receptor subtype mRNAs in the rat cardiovascular system with aging. Mech Ageing Dev. 1996 Jun ... Expression of alpha 1 adrenergic receptor subtype mRNAs in the rat cardiovascular system with aging. ... Expression of alpha 1 adrenergic receptor subtype mRNAs in the rat cardiovascular system with aging. ...
Alpha-1B adrenergic receptor and Alpha-1D adrenergic receptor. Noradrenaline-activated alpha-1 adrenergic receptors participate ... Alpha-1B adrenergic receptor acts through G-protein beta/gamma of pertussis toxin-sensitive Alpha activating activity ... Moreover, Alpha-1A adrenergic receptor may participate in protein synthesis stimulation via Pyk2(FAK2)) / c-Src/ Phospholipase ... alpha(1A) adrenergic receptor induces eukaryotic initiation factor 4E-binding protein 1 phosphorylation via a Ca(2+)-dependent ...
As model systems we utilize the so called adrenergic receptors for adrenaline and related molecules. The goal is to learn the ... After phorbol ester treatment this increased to 3.6 mol of phosphate per mol of alpha 1 receptor. The effect of phorbol esters ... These phorbol ester-treated cells also displayed a decrease in binding affinity of cellular alpha 1 receptors for agonists with ... Phorbol esters promote alpha 1-adrenergic receptor phosphorylation and receptor uncoupling from inositol phospholipid ...
... alpha-adrenergic and muscarinic receptors in vivo was assessed by various neurochemical measurements in rat brain. Olanzapine ... alpha-adrenergic and muscarinic receptors in vivo, consistent with its high affinity for these receptor sites in vitro. ... alpha-adrenergic and muscarinic receptors in vivo was assessed by various neurochemical measurements in rat brain. Olanzapine ... Inactivation of dopamine D1 and D2 receptors by EEDQ was antagonized by olanzapine. The ex vivo binding of the 5HT2 radioligand ...
... binding at alpha-adrenergic receptor subtypes by guanyl nucleotides and Na+ is not limited to alpha 2-adrenergic receptors, as ... an alpha 2-adrenergic antagonist) to examine alpha-adrenergic receptors in rat renal cortical membranes. Under the conditions ... Characterization of alpha-adrenergic receptor subtypes in the rat renal cortex. Differential regulation of alpha 1- and alpha 2 ... Characterization of alpha-adrenergic receptor subtypes in the rat renal cortex. Differential regulation of alpha 1- and alpha 2 ...
... adrenergic receptor response, PLC-beta(1) and PLC-beta(3) were overexpressed in NCM using adenoviral infection (Ad-PLC-beta(1) ... Adrenergic receptor activation caused phosphorylation of PLC-beta(1) but not PLC-beta(3), whereas stimulation by ATP induced ... 275, 10845-10850). To examine the PLC subtype mediating the alpha(1)- ... showing that effects of the two PLC-beta isoforms were specific for particular receptor types. PLC-delta(1) overexpression ...
As model systems we utilize the so called adrenergic receptors for adrenaline and related molecules. The goal is to learn the ... A chimeric receptor consisting of the beta 2-adrenergic receptor (beta 2AR) into which the putative third cytoplasmic loop of ... activated phosphatidylinositol metabolism as effectively as the native alpha 1AR, as did a truncated alpha 1AR lacking the last ... Regions of the alpha 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of ...
Order alpha 1 Adrenergic Receptor Proteins from many different species. Find the right product on antibodies-online.com. ... and adrenergic receptors on stage of maturation in neonatal calves and emphasize the association of alpha1-adrenergic receptor ... alpha-1C adrenergic receptor , adrenergic alpha 1c receptor , adrenergic receptor alpha 1c subtype , adrenergic receptor, alpha ... adrenergic, alpha-1A-, receptor variant 5 , adrenergic, alpha-1A-, receptor variant 8 , alpha-1A adrenergic receptor , alpha-1A ...
Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison ... subtypes and characterized pharmacological properties of the expressed receptor protein. A number of significant sequence ... human and rat alpha-1a/d, human and hamster alpha-1b, human and bovine alpha-1c) stably expressed in rat-1 fibroblasts at ... All six alpha-1AR subtypes couple to phosphoinositide hydrolysis in a pertussis toxin-insensitive manner, including the cloned ...
... adrenergic receptors mediate LH-releasing hormone secretion through phospholipases C and A(2) in immortalized hypothalamic ... the remainder is made up of alpha(1A)-ARs. Receptor activation leads to stimulation of PLC. PLC beta 1 and PLC beta 3 are ... adrenergic receptors (alpha(1)-ARs). With the immortalized hypothalamic LHRH neurons, we have found that alpha(1)-adrenergic ... Ligand binding and RNA studies demonstrate that the GT1 cells contain both alpha(1A)- and alpha(1B)-ARs. Competition binding ...
... adrenergic receptor, is a ,G protein-coupled receptor, (GPCR... World Heritage Encyclopedia, the aggregation of the largest ... Adrenergic receptor References * ^ Piascik, M. T.; Perez, D. M. (2001). "Alpha1-adrenergic receptors: New insights and ... Norepinephrine, Alpha-2 adrenergic receptor, Amitriptyline, Serotonin antagonist and reuptake inhibitor, Dopamine receptor D3 ... allowing the β2-adrenergic receptors which mediate vasodilation to dominate.[13] In contrast to α2-adrenergic receptors, α1- ...
Klein U, Ramirez MT, Kobilka BK, von Zastrow M (Aug 1997). "A novel interaction between adrenergic receptors and the alpha- ... "Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor ... The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic ... McClue SJ, Milligan G (Sep 1990). "The alpha 2B adrenergic receptor of undifferentiated neuroblastoma x glioma hybrid NG108-15 ...
1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ... adrenergic receptor activity. • protein binding. • alpha1-adrenergic receptor activity. Cellular component. • integral ...
2014) Cardiac alpha1-adrenergic receptors: novel aspects of expression, signaling mechanisms, physiologic function, and ... 2017) An Oral Selective Alpha-1A Adrenergic Receptor Agonist Prevents Doxorubicin Cardiotoxicity. JACC Basic Transl Sci 2:39-53 ... Alpha-1-Adrenergic Receptor Subtypes in the Cells of the Human Heart Jensen, Brian C. University of North Carolina Chapel Hill ... Alpha-1-Adrenergic Receptor Subtypes in the Cells of the Human Heart. Jensen, Brian C. / University of North Carolina Chapel ...
... encodes a protein of 560 amino acids whose putative topology is similar to that of the family of G-protein-coupled receptors. ... Molecular cloning and expression of the cDNA for the alpha 1A-adrenergic receptor. The gene for which is located on human ... using the hamster alpha 1B-adrenergic receptor as a probe. The deduced amino acid sequence of clone RA42 ... Northern blot analysis of various rat tissues also shows the distribution expected of the alpha 1A receptor subtype with ...
Adrenergic Receptors in Myocardial Ischemia. * Front Matter Pages 79-79 PDF. * Alpha1- and Beta-Adrenergic Receptors in ... Uncoupling of the β-Adrenergic Receptor by Myocardial Ischemia D. E. Vatner ... Sensitization of the Adrenergic System in Early Myocardial Ischemia: Independent Regulation of β-Adrenergic Receptors and ... Mechanisms of Altered Adrenergic Responsiveness Contributing to Arrhythmogenesis During Myocardial Ischemia J. E. Saffitz, P. B ...
Adrenergic alpha-Antagonists) AND (Child* OR Adolescent). At LILACS, the following search strategy was used: strategy (alpha ... This review analyzed the outcome of alpha adrenergic antagonist in children with ureteral calculi. We conclude that it is the ... Key words: Ureterolithiasis; Adrenergic alpha-1 Receptor Antagonists; Child; Review Literature as Topic ... Adrenergic alpha antagonists) AND (Child). We further searched manually through the references of the primary studies. The ...
Adrenergic Receptors: Trafficking. Adrenergic receptor trafficking is an active physiological process where adrenergic ... 3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. (opens in new tab) ... and alpha 2-adrenergic receptors. Phenoxybenzamine was approximately 250-fold more potent at decreasing alpha 1-adrenergic ... receptor density than it was at decreasing alpha 2-adrenergic receptor density. ...
Phenoxybenzamine is a nonselective alpha-adrenergic receptor blocker that antagonizes both alpha-1 and alpha-2 receptors. This ... It inhibits postsynaptic alpha-adrenergic receptors, resulting in vasodilation of veins and arterioles and a decrease in total ... It inhibits postsynaptic alpha-adrenergic receptors, resulting in vasodilation of veins and arterioles and a decrease in total ... It is an alpha-adrenergic blocker specifically targeted to alpha-1 receptors. Tamsulosin has the advantage of producing ...
  • α1-adrenergic receptor subtypes increase inhibition in the olfactory system, suggesting a synaptic mechanism for noradrenergic modulation of olfactory driven behaviors. (wikipedia.org)
  • Ten commercial antibodies for alpha-1-adrenergic receptor subtypes are nonspecific. (abcam.com)
  • The alpha-AR -induced mydriasis in mice is mediated mainly by the alphaA-AR, with a smaller contribution of the alphaB-AR, matching the relative abundance of these subtypes at the mRNA level. (antikoerper-online.de)
  • 1 KO of the two main myocardial α1-AR subtypes, the α1A and α1B, impairs normal post-natal cardiac growth, and causes severe dilated cardiomyopathy and death after pressure overload. (pubmedcentralcanada.ca)
  • Characterization of alpha-adrenergic receptor subtypes in the rat renal cortex. (aspetjournals.org)
  • Guanyl nucleotides decreased the affinity of epinephrine at both receptor subtypes, but this effect was greater at the alpha 2-receptor and, according to computer analysis, occurred through different mechanisms at the two receptor subtypes. (aspetjournals.org)
  • Thus, separate alpha 1- and alpha 2-adrenergic receptors can be detected in the rat renal cortex and binding to both receptor subtypes can be regulated by guanyl nucleotides and Na+ X Na+ may directly interact with alpha 2- but not alpha 1-adrenergic receptors in the renal cortex. (aspetjournals.org)
  • Our findings with renal cortical membranes indicate that regulation of agonist binding at alpha-adrenergic receptor subtypes by guanyl nucleotides and Na+ is not limited to alpha 2-adrenergic receptors, as previously reported with other tissues. (aspetjournals.org)
  • We have cloned cDNAs encoding three human alpha-1 adrenergic receptor (AR) subtypes and characterized pharmacological properties of the expressed receptor protein. (duke.edu)
  • Pharmacological characterization was performed simultaneously using six cloned alpha-1AR subtypes (human and rat alpha-1a/d, human and hamster alpha-1b, human and bovine alpha-1c) stably expressed in rat-1 fibroblasts at approximately equal receptor concentrations (1-2 pmol/mg of total protein). (duke.edu)
  • In general, human alpha-1AR subtypes have similar pharmacology compared to their rat, hamster and bovine homologs, although a few minor species differences important for alpha-1AR classification are noted. (duke.edu)
  • All six alpha-1AR subtypes couple to phosphoinositide hydrolysis in a pertussis toxin-insensitive manner, including the cloned human alpha-1a/dAR which had not been expressed previously. (duke.edu)
  • In summary, these data represent the first side-by-side comparison of pharmacological properties between species homologs of alpha-1AR subtypes and should facilitate the development of alpha-1AR subtype selective drugs for clinical use. (duke.edu)
  • It consists of three highly homologous subtypes, including α 1A - , α 1B - , and α 1D -adrenergic . (gutenberg.org)
  • The research plan follows naturally from the applicant's recent novel work identifying the tissue distribution of the 3 alpha-1-AR subtypes in the human heart. (grantome.com)
  • Abundant data from animal studies, including knockout mouse models created by the mentor, show that the alpha-1 A and alpha-IB subtypes play beneficial roles in the heart and protect against HF. (grantome.com)
  • Surprisingly, the function of the human cardiac alpha-1-AR subtypes is unknown, and alpha-1-ARs have never been studied in human heart cells. (grantome.com)
  • III) Identify the functional alpha-1-AR subtypes in human coronary smooth muscle and endothelial cells. (grantome.com)
  • α2-adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. (wikipedia.org)
  • There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation. (wikipedia.org)
  • This study provides definitive evidence for the existence of three alpha 1-adrenergic receptor subtypes. (nih.gov)
  • Three distinct alpha-1 adrenergic receptor subtypes (alpha-1a, alpha-1b and alpha-1d) have been identified through molecular cloning. (elsevier.com)
  • The results of the present study indicate that alpha-1 adrenergic receptor subtypes are discretely distributed among rat tissues, suggesting independent functions. (elsevier.com)
  • There are three families of adrenergic receptors, alpha 1 , alpha 2 and beta, and each family contains three distinct subtypes. (thefreedictionary.com)
  • α 2 -adrenergic receptors include 3 highly homologous subtypes: α 2A , α 2B , and α 2C . (wikipedia.org)
  • Left ventricular hypertrophy (LVH) is associated with decreased responsiveness of renal α1-adrenoreceptors subtypes to adrenergic agonists. (bireme.br)
  • This study investigated the impact of nitric oxide (NO) and its potential interaction with the responsiveness of renal α1-adrenoreceptors subtypes to adrenergic stimulation in rats with left ventricular hypertrophy (LVH). (bireme.br)
  • Clonidine and other α-2 agonists used clinically (tizanidine, brimonidine and dexmedetomidine) activate to varying degrees three structurally distinct subtypes of the α-2 receptor: α-2A, α-2B, and α-2C. (asahq.org)
  • Further research to define the role of various alpha receptor subtypes is needed to identify strategies for separating the analgesic and sedative effects of α-2 agonists. (asahq.org)
  • Adrenergic alpha2 receptors are divided into three subtypes in humans: alpha2A, alpha2B and alpha2C. (genecards.org)
  • Other effects on smooth muscle are contraction in: Ureter Uterus (when pregnant): this is minor compared to the relaxing effects of the β2 receptor, agonists of which - notably albuterol/salbutamol - were formerly[citation needed] used to inhibit premature labor. (wikipedia.org)
  • Incubation of these cells with tumor-promoting phorbol esters, which stimulate calcium- and phospholipid-dependent protein kinase, leads to a marked attenuation of the ability of alpha 1-receptor agonists such as norepinephrine to stimulate the turnover of inositol phospholipids. (duke.edu)
  • These phorbol ester-treated cells also displayed a decrease in binding affinity of cellular alpha 1 receptors for agonists with no change in antagonist affinity. (duke.edu)
  • High affinity for the antagonist WB4101 and agonists phenylephrine and methoxamine suggests that cDNA RA42 encodes the alpha 1A receptor subtype. (nih.gov)
  • Shumay E, Gavi S, Wang HY and Malbon CC (2004) Trafficking of beta2‐adrenergic receptors: insulin and beta‐agonists regulate internalisation by distinct cytoskeletal pathways. (els.net)
  • The responsiveness of renal α1A, α1B and α1D-adrenoceptors in the low dose and high dose phases of 5-MeU, CEC and BMY7378 to adrenergic agonists was increased along with cGMP in the kidney of LVH-NO group. (bireme.br)
  • These findings suggest that exogenous NO precursor up-regulated the renal eNOS/NO/cGMP pathway in LVH rats and resulted in augmented α1A, α1B and α1D adrenoreceptors responsiveness to the adrenergic agonists. (bireme.br)
  • Although complete selectivity between receptor agonism is rarely achieved, phenylephrine is an α 1 agonist, while clonidine and methyldopa are α 2 partial agonists [1] . (wikidoc.org)
  • Alpha-adrenergic agonists are used in the treatment of glaucoma by decreasing the production of aqueous fluid by the ciliary bodies of the eye. (wikidoc.org)
  • α-2-ADRENOCEPTORS are known to mediate analgesia, and α-2-adrenoceptor agonists (such as clonidine) have proven effective in the treatment of pain, such as intractable cancer pain, 1,2 postsurgical pain, 3,4 and sympathetically maintained pain. (asahq.org)
  • The α-2A receptor was necessary for the analgesic activity of brimonidine, clonidine, and tizanidine, but a surprising difference identified in the activity of the α-2 agonists in α-2C knockout mice led to investigation of the roles of α-1 and α-2 receptor activation in pain modulation. (asahq.org)
  • Here we show that while the carazolol pocket captured in the β 2 AR crystal structure accommodates (-)-isoproterenol and other agonists without steric clashes, a finite movement of the flexible extracellular part of TM-V helix (TM-Ve) obtained by receptor optimization in the presence of docked ligand can further improve the calculated binding affinities for agonist compounds. (pubmedcentralcanada.ca)
  • Tilting of TM-Ve towards the receptor axis provides a more complete description of polar receptor/ligand interactions for full and partial agonists, by enabling optimal engagement of agonists with two experimentally identified anchor sites, formed by Asp113/Asn312 and Ser203/Ser204/Ser207 side chains. (pubmedcentralcanada.ca)
  • Further, receptor models incorporating a flexible TM-V backbone allow reliable prediction of binding affinities for a set of diverse ligands, suggesting potential utility of this approach to design of effective and subtype-specific agonists for adrenergic receptors. (pubmedcentralcanada.ca)
  • The responses mediated through the receptors that are activated by the partial agonists are resistant to myosin light chain kinase inhibitors, while the response through the activation of the other receptors are suppressed by the inhibitors. (nii.ac.jp)
  • To further elucidate the significance of NE- and Glu-evoked astrocytic [Ca2+]i signaling to neuron-astrocyte communication in the mature CNS, [Ca2+]i of astrocyte networks within hippocampal slices (P21-42) was measured during bath application of NE and Glu receptor agonists. (jneurosci.org)
  • In the mouse bleomycin model of right ventricular failure, the alpha1A -adrenergic receptor subtype agonist A61603 prevents right ventricular failure. (antikoerper-online.de)
  • alpha 2 Agonist binding (p-amino-clonidine) declined in both hypothalamus and brain stem, and the fall was greater in hypertensive than in normotensive rats. (ahajournals.org)
  • The down regulation of alpha 2-adrenergic receptors and the up regulation of alpha 1-adrenergic receptors are compatible with increased alpha 2-adrenergic agonist presynaptic inhibition of catecholamine release with resultant postsynaptic alpha 1-adrenergic receptor supersensitivity. (ahajournals.org)
  • Is the attenuation of beta-adrenergic agonist efficacy during labor caused by elevated prostaglandin E levels? (biomedsearch.com)
  • OBJECTIVE: Our purpose was to investigate whether attenuation of beta-adrenergic agonist efficacy during labor is due to elevated prostaglandin E levels. (biomedsearch.com)
  • STUDY DESIGN: beta-Receptor function (response to beta-agonist or forskolin) was tested in mononuclear leukocytes collected from women at term before or during labor. (biomedsearch.com)
  • An optical section of the fluorescent receptors is obtained by epifluorescence confocal microscopy from insulin‐treated (a), untreated (b) and β‐adrenergic agonist‐treated (c) cells. (els.net)
  • Hadcock JR and Malbon CC (1988) Down‐regulation of beta‐adrenergic receptors: agonist‐induced reduction in receptor mRNA levels. (els.net)
  • Kallal L, Gagnon AW, Penn RB and Benovic JL (1998) Visualization of agonist‐induced sequestration and down‐regulation of a green fluorescent protein‐tagged beta2‐adrenergic receptor. (els.net)
  • 2004) Characterization of agonist stimulation of cAMP‐dependent protein kinase and G protein‐coupled receptor kinase phosphorylation of the beta2‐adrenergic receptor using phosphoserine‐specific antibodies. (els.net)
  • An adrenergic alpha-agonist is a drug which selectively stimulates alpha adrenergic receptors . (wikidoc.org)
  • Functions in regulating agonist-mediated G-protein coupled receptor (GPCR) signaling by mediating both receptor desensitization and resensitization processes. (uniprot.org)
  • However, the extent of beta-arrestin involvement appears to vary significantly depending on the receptor, agonist and cell type. (uniprot.org)
  • The 2.4 Å crystal structure of the β 2 -adrenergic receptor (β 2 AR) in complex with the high-affinity inverse agonist (-)-carazolol provides a detailed structural framework for the analysis of ligand recognition by adrenergic receptors. (pubmedcentralcanada.ca)
  • Xylometazoline is a direct acting sympathomimetic adrenergic alpha-agonist used to induce systemic vasoconstriction, thereby decreasing nasal congestion. (hmdb.ca)
  • Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. (freepatentsonline.com)
  • The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. (freepatentsonline.com)
  • 1. A biodegradable intraocular implant for improving vision, the implant comprising an alpha-2 adrenergic receptor agonist and a biodegradable polymer, the implant capable of releasing the alpha-2 adrenergic receptor agonist from the polymer, upon intravitreal placement of the implant, in an amount effective to improve the vision of the eye in which the implant is placed. (freepatentsonline.com)
  • 2. The implant of claim 1, wherein the alpha-2 adrenergic receptor agonist is selected from the group consisting of quinoxalines, (2-imidozolin-2-ylamino) quinoxalines, 5-bromo-6-(2-imidozolin-2-ylamino) quinoxalines, derivatives thereof and mixtures thereof. (freepatentsonline.com)
  • 4. The implant of claim 1, wherein the alpha-2 adrenergic receptor agonist is brimonidine tartrate. (freepatentsonline.com)
  • 5. The implant of claim 1, wherein the alpha-2 adrenergic receptor agonist is dispersed within the biodegradable polymer. (freepatentsonline.com)
  • 7. The implant of claim 1, wherein the polymer releases drug at a rate effective to sustain release of an amount of the alpha-2 adrenergic receptor agonist from the implant for more than one month from the time the implant is placed in the vitreous of the eye. (freepatentsonline.com)
  • 8. The implant of claim 1, wherein the polymer releases drug at a rate effective to sustain release of an amount of the alpha-2 adrenergic receptor agonist from the implant for more than forty days from the time the implant is placed in the vitreous of the eye. (freepatentsonline.com)
  • In virgin rats, the PKC activator phorbol 12,13-dibutyrate (PDBu, 10 − 6 M) and the α-adrenergic agonist phenylephrine (Phe, 10 − 5 M) caused significant increases in active stress and PKC activity that were inhibited by the PKC inhibitors staurosporine and calphostin C. Western blot analysis in aortic strips of virgin rats showed significant amount of the α-PKC isoform. (physiology.org)
  • The alpha 1- agonist phenylephrine (PE) (10-100 microM) evoked complex [Ca2+]i signals (22 of 26 slices, 90 of 90 cells in responding slices) composed of both a prolonged component (5.1 +/- 1.8 min), synchronized in neighboring cells, and multiple, mainly asynchronous [Ca2+]i spikes (25.0 +/- 11.6 sec). (jneurosci.org)
  • The alpha 2-agonist clonidine (10- 100 microM) did not increase [Ca2+]i (n = 4 slices). (jneurosci.org)
  • The metabotropic agonist t-ACPD (30 or 50 microM) did not increase astrocytic [Ca2+]i in hippocampal slices (0 of 5), while kainate (200 microM or 1 mM) induced brief (1-2 min) [Ca2+]i increases only rarely (2 of 8 applications in 6 slices). (jneurosci.org)
  • At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. (wikipedia.org)
  • However, the alpha receptor mediating renal arteriolar vasoconstriction appeared to be of the alpha-1 subtype as there was a close correlation between the in vitro results and the binding data determined with [3H]prazosin (r = 0.93). (aspetjournals.org)
  • Expression of alpha 1 adrenergic receptor subtype mRNAs in the rat cardiovascular system with aging. (harvard.edu)
  • Subtype alpha-1 adrenergic receptors consist of Alpha-1A adrenergic receptor , Alpha-1B adrenergic receptor and Alpha-1D adrenergic receptor . (bio-rad.com)
  • We have used the subtype-selective radioligands [3H]prazosin (an alpha 1-adrenergic antagonist) and [3H]yohimbine (an alpha 2-adrenergic antagonist) to examine alpha-adrenergic receptors in rat renal cortical membranes. (aspetjournals.org)
  • To examine the PLC subtype mediating the alpha(1)-adrenergic receptor response, PLC-beta(1) and PLC-beta(3) were overexpressed in NCM using adenoviral infection (Ad-PLC-beta(1) NCM and Ad-PLC-beta(3) NCM, respectively) and PLC responses assessed from [(3)H]inositol phosphate (InsP) generation in the presence of 10 mm LiCl. (garvan.org.au)
  • It is a subtype of the adrenergic receptor family. (wikipedia.org)
  • Northern blot analysis of various rat tissues also shows the distribution expected of the alpha 1A receptor subtype with abundant expression in vas deferens followed by hippocampus, cerebral cortex, aorta, brainstem, heart and spleen. (nih.gov)
  • The second alpha 1-adrenergic receptor cloned represents the rat homolog of the hamster alpha 1B subtype. (nih.gov)
  • Alpha-1 adrenergic antagonists increased the probability of calculus expulsion by 27% (NNT=4). (scielo.br)
  • Hoffman BB (2001) Catecholamines, sympathetic drugs, and adrenergic receptor antagonists. (els.net)
  • This structure, followed by other co-crystals of β 2 AR ( Hanson and others 2008b ) and β 1 AR ( Warne and others 2008 ) with the antagonists (-)-timolol (PDB code 3D4S) and (-)-cyanopindolol (PDB code 2VT4) respectively, represents a leap forward in the understanding of the inactive state of adrenergic GPCRs. (pubmedcentralcanada.ca)
  • Alpha antagonists are used to treat what? (studystack.com)
  • non-selective adrenergic antagonists are used to treat what? (studystack.com)
  • 3H]Dihydroergocryptine, a nonselective alpha adrenergic antagonist, the alpha-1 selective antagonist, [3H]prazosin and the alpha-2 selective antagonist, [3H]yohimbine, were used to study binding sites in rat renal membranes. (aspetjournals.org)
  • In addition, in both the functional and [3H]prazosin binding studies, unlabeled prazosin ws 5 to 40-fold more potent than the nonselective antagonist, phentolamine, and 400- to 1500-fold more potent than the alpha-2 antagonist, yohimbine. (aspetjournals.org)
  • The effects of phenoxybenzamine on alpha 1- and alpha 2-adrenergic receptor binding sites were examined directly using radioligand binding assays of the antagonist drugs [125I]BE 2254 and [3H]rauwolscine, respectively, in homogenates of rat cerebral cortex. (meta.org)
  • This review analyzed the outcome of alpha adrenergic antagonist in children with ureteral calculi. (scielo.br)
  • Studies on RX 781094: a selective, potent and specific antagonist of alpha 2-adrenoceptors. (semanticscholar.org)
  • RAPAFLO (TM) is an effective, uniquely selective alpha-1 adrenergic receptor antagonist. (bio-medicine.org)
  • Binding of the selective alpha 1-adrenergic antagonist [3H]prazosin and the alpha 2-adrenergic antagonist [3H]rauwolscine was used for receptor studies in tissues of prehypertensive (24-day-old) and hypertensive (60-day-old) rats. (ahajournals.org)
  • Compared with their age-matched normotensive controls, MHS rats showed 1) a lower affinity for the antagonist (p less than 0.05) in the prehypertensive period, 2) absence of the normal age-related increase in receptor density, and 3) a lower density of [3H]rauwolscine binding sites (p less than 0.001) in the hypertensive period. (ahajournals.org)
  • PE responses were completely blocked by the alpha 1-antagonist prazosin (200 nM, n = 4 slices), but not by the alpha 2- antagonist yohimbine (n = 3 slices). (jneurosci.org)
  • RESULTS: Mononuclear leukocytes from women in active labor exhibited a significant attenuation of beta-adrenergic receptor function as a result of reduced adenylyl cyclase activity. (biomedsearch.com)
  • This effect could be induced in mononuclear leukocytes from nonlaboring women by preincubation with prostaglandin E but not oxytocin or prostaglandin F. CONCLUSIONS: Prostaglandin E induces heterologous desensitization of the beta-adrenergic receptor system in mononuclear leukocytes, comparable to that seen during labor. (biomedsearch.com)
  • Beta-adrenergic receptor interactions. (biomedsearch.com)
  • alpha-adrenergic, which act in response to sympathomimetic stimuli, and beta-adrenergic, which block sympathomimetic activity. (thefreedictionary.com)
  • 1996) The beta‐adrenergic receptor is a substrate for the insulin receptor tyrosine kinase. (els.net)
  • 1987) Ligand binding to the beta‐adrenergic receptor involves its rhodopsin‐like core. (els.net)
  • alpha- and beta-adrenergic pathways differentially regulate cell type-specific apoptosis in rat cardiac myocytes. (semanticscholar.org)
  • However, it is unknown if alpha- and beta-adrenergic pathways coordinately or differentially regulate apoptosis and if this apoptotic pathway uses common or cell type-specific apoptotic signals. (semanticscholar.org)
  • Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. (uniprot.org)
  • Analysis of the ligand binding properties of RA42 expressed in COS-7 cells with a variety of adrenergic ligands demonstrates a unique alpha 1-adrenergic receptor pharmacology. (nih.gov)
  • Journal of Pharmacology and Experimental Therapeutics , 244 (1), 226-230. (elsevier.com)
  • Minneman, KP, Mumford, GK & Abel, PW 1988, ' High efficiency coupling of alpha-1 adrenergic receptors to inositol phospholipid metabolism revealed by denervation of rat vas deferens ', Journal of Pharmacology and Experimental Therapeutics , vol. 244, no. 1, pp. 226-230. (elsevier.com)
  • We investigated the α-adrenergic pharmacology of analgesia using models of tactile hypersensitivity induced with chemical stimuli that sensitize pain pathways at spinal or peripheral sites. (asahq.org)
  • In smooth muscle cells of blood vessels the principal effect of activation of these receptors is vasoconstriction. (wikipedia.org)
  • In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more resistant to inhibition, and attenuation of α1-adrenergic-receptor-mediated vasoconstriction only occurs during heavy exercise. (wikipedia.org)
  • Resting muscle will not have its α1-adrenergic receptors blocked, and hence the overall effect will be α1-adrenergic-mediated vasoconstriction. (wikipedia.org)
  • To establish a correlation between binding and a biological function, the ability of alpha adrenergic agents to stimulate or inhibit vasoconstriction was quantified in vitro using an isolated perfused kidney preparation. (aspetjournals.org)
  • Despite the preponderance of alpha-2 receptors, the alpha receptor mediating renal vasoconstriction appears to be of the alpha-1 type. (aspetjournals.org)
  • Alpha receptor effects Vasoconstriction, reduced GI tract motility. (thefreedictionary.com)
  • Which adrenergic receptor is responsible for vasoconstriction of the arterioles in the skin and viscera, and intestinal relaxation? (studystack.com)
  • Autonomic Receptor-mediated Regulation of Production and Release of Nitric Oxide in Normal and Malignant Human Urothelial Cells. (abcam.com)
  • Differential regulation of alpha 1- and alpha 2-adrenergic receptors by guanyl nucleotides and Na. (aspetjournals.org)
  • Operating via heterotrimeric G proteins, adrenergic receptors constitute one of the most intensely studied classes of membrane proteins, whose expression and function are subject to regulation at many different levels, including transcriptional, posttranscriptional and posttranslational. (els.net)
  • Kohout TA and Lefkowitz RJ (2003) Regulation of G protein‐coupled receptor kinases and arrestins during receptor desensitization. (els.net)
  • Krupnick JG and Benovic JL (1998) The role of receptor kinases and receptors in G‐protein‐coupled receptor regulation. (els.net)
  • Shenoy SK, McDonal PH, Kohout TA and Lefkowitz RJ (2001) Regulation of receptor fate by ubiquitination of activated beta2‐adrenergic receptor and beta‐arrestin. (els.net)
  • Inhibitory presynaptic receptor regulation in ANS and ENS. (studystack.com)
  • DDT1 MF-2 cells, which are derived from hamster vas deferens smooth muscle, contain alpha 1-adrenergic receptors (54,800 +/- 2700 sites per cell) that are coupled to stimulation of inositol phospholipid metabolism. (duke.edu)
  • PLC-delta(1) overexpression selectively reduced NE-induced [(3)H]InsP responses, without affecting the ATP stimulation. (garvan.org.au)
  • alpha(1)-Adrenergic receptor activation caused phosphorylation of PLC-beta(1) but not PLC-beta(3), whereas stimulation by ATP induced phosphorylation of PLC-beta(3) but not PLC-beta(1. (garvan.org.au)
  • These data indicate (i) that the regions of the alpha 1AR that determine coupling to phosphatidylinositol metabolism are similar to those previously shown to be involved in coupling of beta 2AR to adenylate cyclase stimulation and (ii) that point mutations of a G-protein-coupled receptor can cause remarkable increases in sensitivity of biological response. (duke.edu)
  • Receptor activation leads to stimulation of PLC. (duke.edu)
  • a site in a sympathetic effector cell that reacts to adrenergic stimulation. (thefreedictionary.com)
  • In general, stimulation of alpha receptors is excitatory of the function of the host organ or tissue, and stimulation of the beta receptors is inhibitory. (thefreedictionary.com)
  • Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (nih.gov)
  • These results support a primary role of NE release and alpha 1-adrenoceptor stimulation in neuron-astrocyte communication in the mature CNS. (jneurosci.org)
  • Auf www.antikoerper-online.de finden Sie aktuell 44 Adrenoceptor alpha 1A (ADRA1A) ELISA Kits von 10 unterschiedlichen Herstellern. (antikoerper-online.de)
  • Chez www.anticorps-enligne.fr sont 7 Adrenoceptor alpha 1A (ADRA1A) Protéines de 4 de différents fournisseurs disponibles. (anticorps-enligne.fr)
  • The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. (wikipedia.org)
  • ADRA2B (Adrenoceptor Alpha 2B) is a Protein Coding gene. (genecards.org)
  • α1-receptors primarily mediate smooth muscle contraction, but have important functions elsewhere as well. (wikipedia.org)
  • During exercise, α1-adrenergic receptors in active muscles are attenuated in an exercise intensity-dependent manner, allowing the β2-adrenergic receptors which mediate vasodilation to dominate. (wikipedia.org)
  • alpha(1)-adrenergic receptors mediate LH-releasing hormone secretion through phospholipases C and A(2) in immortalized hypothalamic neurons. (duke.edu)
  • Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. (drugbank.ca)
  • GO annotations related to this gene include G-protein coupled receptor activity and alpha2-adrenergic receptor activity . (genecards.org)
  • Although binding of epinephrine to both alpha 1- and alpha 2-receptors could be modulated by guanyl nucleotides, we were unable to detect inhibition by epinephrine of basal or hormone-stimulated adenylate cyclase activity. (aspetjournals.org)
  • Beta receptors are divided into beta1, beta2, beta3, which are linked to Gs, and adenylate cyclase, increasing cAMP, which in turn drives cAMP-dependent protein kinase that mediates intracellular events. (thefreedictionary.com)
  • this effect was more Na+-selective at alpha 2- than at alpha 1-receptors. (aspetjournals.org)
  • The reduced NE response was associated with a selective loss of PLC-beta(1) expression in Ad-PLC-delta(1) NCM. (garvan.org.au)
  • RAPAFLO (TM) is a new, uniquely selective alpha blocker for the treatment of the signs and symptoms of BPH, launched earlier this month by Watson Pharmaceuticals, a leader in generic and specialty branded pharmaceuticals. (bio-medicine.org)
  • Selective modification of renal alpha 2-adrenergic receptors in Milan hypertensive rat strain. (ahajournals.org)
  • Trazodone hydrochloride is a selective serotonin reuptake inhibitor indicated for the treatment of major depressive disorder (MDD) ( 1 ). (nih.gov)
  • Phorbol esters promote alpha 1-adrenergic receptor phosphorylation and receptor uncoupling from inositol phospholipid metabolism. (duke.edu)
  • The effect of phorbol esters on norepinephrine-stimulated inositol phospholipid turnover and alpha 1-receptor phosphorylation showed the same rapid time course with a t1/2 less than 2 min. (duke.edu)
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs share many similarities in receptor phosphorylation, use of accessory proteins and sequestration of the receptors. (els.net)
  • Here, we report the effects of constitutive activation of α 1 -adrenergic signaling on connexin phosphorylation and cardiac conduction. (ahajournals.org)
  • H-Ras then activates v-raf-1 murine leukemia viral oncogene homolog 1 ( c-Raf-1 ) / Mitogen-activated protein kinase kinases 1 and 2 ( MEK1(MAP2K1) and MEK2(MAP2K2) )/ Mitogen activated protein kinase 1 ( ERK2(MAPK1) ) [ 1 ], [ 10 ]. (bio-rad.com)
  • The role of adrenergic activation on murine luteal cell viability and progesterone production. (semanticscholar.org)
  • It inhibits postsynaptic alpha-adrenergic receptors, resulting in vasodilation of veins and arterioles and a decrease in total peripheral resistance and blood pressure. (medscape.com)
  • Which adrenergic receptor causes vasodilation of skeletal muscle and liver, intestinal relaxation, bronchodilation, and increased metabolic rate? (studystack.com)
  • Xylometazoline is a direct acting sympathomimetic drug, which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. (hmdb.ca)
  • To avoid confusion, naming was continued with the letter D. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α1-adrenergic receptor in the central and peripheral nervous systems. (wikipedia.org)
  • The neurotransmitter norepinephrine has higher affinity for the α1 receptor than does the hormone epinephrine/adrenaline. (wikipedia.org)
  • In particular, norepinephrine decreases glutamatergic excitatory postsynaptic potentials by the activation of α1-adrenergic receptors. (wikipedia.org)
  • Norepinephrine also stimulates serotonin release by binding α1-adrenergic receptors located on serotonergic neurons in the raphe. (wikipedia.org)
  • The functional status of these alpha-1 adrenergic receptors was also assessed by measuring the norepinephrine-induced accumulation of inositol phosphates in myometrial tissue. (aspetjournals.org)
  • However, norepinephrine-induced increases in inositol 1,4,5-triphosphate were only observed in the outer layer. (aspetjournals.org)
  • At higher doses, olanzapine increased the concentrations of the norepinephrine metabolite, MHPG-SO4, probably by blocking alpha 1-adrenergic receptors. (nih.gov)
  • Activation of phospholipase C (PLC) in neonatal rat cardiomyocytes (NCM) generates primarily inositol 1,4,5-trisphosphate (Ins(1,4,5)P(3)) in response to rises in intracellular Ca(2+), or inositol 1,4-bisphosphate (Ins(1,4)P(2)) in response to norepinephrine (NE) (Matkovich, S. J. and Woodcock, E. A. (2000) J. Biol. (garvan.org.au)
  • Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α 1 -adrenergic receptor in the central and peripheral nervous systems . (gutenberg.org)
  • In denervated tissues, the potency of norepinephrine in stimulating [ 3 H]IP accumulation was decreased about 40-fold after receptor inactivation with 1 μM phenoxybenzamine. (elsevier.com)
  • These results suggest that there is a substantial alpha-1 adrenergic receptor reserve for stimulating [ 3 H]IP accumulation in rat vas deferens which is normally obscured by rapid inactivation of norepinephrine. (elsevier.com)
  • This receptor binds epinephrine and norepinephrine with approximately equal affinity. (uniprot.org)
  • With the immortalized hypothalamic LHRH neurons, we have found that alpha(1)-adrenergic agents directly stimulate the secretion of LHRH in a dose-dependent manner. (duke.edu)
  • PLC beta 1 and PLC beta 3 are expressed in GT1 neurons, and these PLCs are probably responsible for the release of diacylglycerol and IP as well as the increase in intracellular calcium. (duke.edu)
  • These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. (wikipedia.org)
  • This protein is a member of a subfamily of G protein-coupled receptors that regulate neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. (genecards.org)
  • We have now cloned two alpha 1-adrenergic receptors from a rat cerebral cortex cDNA library, using the hamster alpha 1B-adrenergic receptor as a probe. (nih.gov)
  • Expression of mRNA for this receptor is strongly detected in liver followed by heart, cerebral cortex, brain stem, kidney, lung, and spleen. (nih.gov)
  • In the cerebral cortex, no between-strain differences in alpha 1-adrenergic and alpha 2-adrenergic receptor density and affinity were observed in prehypertensive and hypertensive periods. (ahajournals.org)
  • The myocardium contains adrenergic receptors (ARs) of two main classes, β and α1. (pubmedcentralcanada.ca)
  • 15,16 Increased α 1 -adrenergic signaling in the myocardium of heart failure patients might contribute to defective cardiac conduction and to arrhythmias. (ahajournals.org)
  • The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein. (wikipedia.org)
  • α1-Adrenergic receptors are members of the G protein-coupled receptor superfamily. (wikipedia.org)
  • Marchese A, Chen C, Kim YM and Benovic JL (2003) The ins and outs of G‐protein‐coupled receptor trafficking. (els.net)
  • Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. (duke.edu)
  • A mutation of rs2322333, located in the intronic and 3' UTR (zeige UTS2R ELISA Kits ) part of the gene ADRA1A in chromosome 8, has a probability of being deleterious the abolition of ELAV-like protein 1 (ELAVL1 (zeige ELAVL1 ELISA Kits )) binding site rs2695260. (antikoerper-online.de)
  • The human gene encoding this receptor has the symbol ADRA2B. (wikipedia.org)
  • The alpha-1D adrenergic receptor (α 1D adrenoreceptor), also known as ADRA1D , is an alpha-1 adrenergic receptor , and also denotes the human gene encoding it. (wikipedia.org)
  • This gene encodes alpha-1D-adrenergic receptor. (wikipedia.org)
  • Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a single intron that interrupts the coding region. (wikipedia.org)
  • α 1 -Adrenergic signaling targets the transcription factor RTEF-1 (transcription enhancer factor-1-related factor) to upregulate gene expression in cultured cardiac myocytes. (ahajournals.org)
  • 17,18 To better understand how RTEF-1 regulates cardiac gene expression and affects cardiac function in vivo, we made transgenic mice that overexpress RTEF-1 in the heart. (ahajournals.org)
  • Expression of alpha-1 adrenergic receptor mRNA has been detected in several tissues, but previous studies with Northern blot analysis or RNase protection assays have provided only semiquantitative information. (elsevier.com)
  • In the present study, we quantified alpha-1a, alpha-1b and alpha-1d adrenergic receptor mRNA in 19 adult rat tissues through the use of reverse transcription (RT) and a competitive polymerase chain reaction (PCR). (elsevier.com)
  • Competitive RT-PCR is an accurate and sensitive method for the measurement of alpha-1 adrenergic receptor mRNA in small tissue samples. (elsevier.com)
  • The deduced amino acid sequence of clone RA42 encodes a protein of 560 amino acids whose putative topology is similar to that of the family of G-protein-coupled receptors. (nih.gov)
  • Internalized arrestin-receptor complexes traffic to intracellular endosomes, where they remain uncoupled from G-proteins. (uniprot.org)
  • Beta-arrestins function as multivalent adapter proteins that can switch the GPCR from a G-protein signaling mode that transmits short-lived signals from the plasma membrane via small molecule second messengers and ion channels to a beta-arrestin signaling mode that transmits a distinct set of signals that are initiated as the receptor internalizes and transits the intracellular compartment. (uniprot.org)
  • alpha 1-mediated [Ca2+]i transients were observed after removal of extracellular [Ca2+]o (n = 8 of 9 slices), indicating PE-induced Ca2+ release from intracellular stores. (jneurosci.org)
  • In addition to this newly issued patent Synaptic has 16 applications pending on its alpha adrenergic receptor and benign prostatic hyperplasia technology. (thefreedictionary.com)
  • The alpha adrenergic receptor system, which responds to the neurotransmitter adrenaline, is an important signaling mechanism in the body and is believed to be involved in such diverse therapeutic indications as cardiovascular disease, benign prostatic hyperplasia (BPH), pain and glaucoma. (thefreedictionary.com)
  • While detailed knowledge of ligand-receptor interactions would be instrumental in design of new and improved clinical candidates, the insight into spatial structure of GPCR has been limited to ab initio models ( Goddard and Abrol 2007 ) or models based on rhodopsin crystal structure ( Palczewski and others 2000 ). (pubmedcentralcanada.ca)
  • We have studied the effect of long-term (72 hour) intravenous infusions of methyldopa to awake restrained spontaneously hypertensive rats and normotensive Wistar-Kyoto control animals to look for differences in hypotensive effect, differences in concentrations of natural and alpha-methylated catecholamines, and differences in alpha 1 and alpha 2-adrenergic receptor populations. (ahajournals.org)
  • 1) Alpha receptors, which evoke an excitatory response of smooth muscle cells to catecholamines. (thefreedictionary.com)
  • 2) Beta receptors, which dampen the response to catecholamines. (thefreedictionary.com)
  • In patients with heart failure, chronically elevated catecholamines upset the balance between β- and α 1 -adrenergic receptors. (ahajournals.org)
  • Phenoxybenzamine is a nonselective alpha-adrenergic receptor blocker that antagonizes both alpha-1 and alpha-2 receptors. (medscape.com)
  • The advantage of prazosin over nonselective alpha-adrenergic blockers includes a lower incidence of adverse effects. (medscape.com)
  • However, literature about the use of alpha-1 adrenergic blockers in pediatric population with distal ureterolithiasis is still scarce. (scielo.br)
  • This review has the objective to evaluate the use of alpha-1 adrenergic blockers as medical expulsive treatment in children with distal ureterolithiasis. (scielo.br)
  • In the adult patient, there are various conservative treatments to treat calculi smaller than 12mm, such as the use of calcium blockers, non-steroidal anti-inflammatory agents, or alpha-1 adrenergic blockers, which is the better approach ( 9 ). (scielo.br)
  • The agents used include alpha-adrenergic blockers, 5-alpha-reductase inhibitors, phosphodiesterase-5 enzyme inhibitors, and various combinations. (medscape.com)
  • What is the suffix for alpha blockers? (studystack.com)
  • α1-AR gain-of-function in cardiac transgenic models generally supports the KO results, although phenotypes vary greatly with receptor level, promoter, and absence or presence of an activating mutation. (pubmedcentralcanada.ca)
  • Dr. Simpson is highly respected in the field of molecular cardiology and internationally-recognized for his contributions to our understanding of cardiac hypertrophy and alpha-1-adrenergic receptor (AR) biology. (grantome.com)
  • Collectively these Aims will establish a broader understanding of human cardiac alpha-1-AR biology and the mechanisms of HF. (grantome.com)
  • Cardiac alpha1-adrenergic receptors: novel aspects of expression, signaling mechanisms, physiologic function, and clinical importance. (semanticscholar.org)
  • In animal models of heart failure, cardiac α 1 -adrenergic signaling is constitutively activated. (ahajournals.org)
  • Methods and Results- Transgenic mice were generated with cardiac-specific overexpression of the transcription factor RTEF-1 (transcription enhancer factor-1-related factor), which mediates α 1 -adrenergic signaling in cardiac myocytes. (ahajournals.org)
  • Intercellular dye transfer between RTEF-1 transgenic cardiac myocytes confirmed impaired conduction at the cellular level. (ahajournals.org)
  • Confocal microscopy revealed increased levels of dephosphorylated connexin43 at the cardiac gap junctions in RTEF-1 mice, suggesting that defective conduction is a result of impaired gap-junction conductance rather than assembly. (ahajournals.org)
  • 1 Connexin40, 43, and 45 encode the cardiac gap-junction proteins. (ahajournals.org)
  • The ability of the atypical antipsychotic drug candidate olanzapine to antagonize dopamine, serotonin, alpha-adrenergic and muscarinic receptors in vivo was assessed by various neurochemical measurements in rat brain. (nih.gov)
  • The findings provide evidence that olanzapine antagonized dopamine, serotonin, alpha-adrenergic and muscarinic receptors in vivo, consistent with its high affinity for these receptor sites in vitro. (nih.gov)
  • Antibodies directed predominantly against the alpha(1)-adrenergig receptor were detected in patients suffering from widespread diseases such as hypertension and type 2 diabetes. (mdc-berlin.de)
  • We postulate that antibodies to the alpha(1)-adrenergig receptor are relevant pathomolecules in diseases of the central nervous system associated with vascular impairments. (mdc-berlin.de)
  • METHODOLOGY/PRINCIPAL FINDINGS: Using a rat model we studied the long-term action of antibodies against the alpha(1)-adrenergig receptor either induced by immunization with a receptor peptide or applied by intravenous injection. (mdc-berlin.de)
  • CONCLUSION/SIGNIFICANCE: We present evidence that antibodies to the α(1)-adrenergig receptor cause cerebrovascular impairments in the rat. (mdc-berlin.de)
  • 81 Adrenergic, alpha-1B-, Receptor (ADRA1B) Antibodies from 13 manufacturers are available on www.antibodies-online.com. (antibodies-online.com)
  • Treatment with phenoxybenzamine caused an irreversible, dose-dependent decrease in the density of both alpha 1- and alpha 2-adrenergic receptors. (meta.org)
  • Phenoxybenzamine was approximately 250-fold more potent at decreasing alpha 1-adrenergic receptor density than it was at decreasing alpha 2-adrenergic receptor density. (meta.org)
  • Moreover, the order of potencies of a variety of adrenergic agents, determined by competitive inhibition studies, suggested that the binding of each radioligand was to sites with alpha adrenergic specificity. (aspetjournals.org)
  • Blood vessels with α1-adrenergic receptors are present in the skin, the sphincters of gastrointestinal system, kidney (renal artery) and brain. (wikipedia.org)
  • Renal alpha-1 and alpha-2 adrenergic receptors: biochemical and pharmacological correlations. (aspetjournals.org)
  • These studies suggest that rat renal plasma membranes contain binding sites with both alpha-1 and alpha-2 adrenergic receptor specificity, in a ratio of approximately 1:3. (aspetjournals.org)
  • Cerebral and renal alpha-adrenergic receptors play an important role in the control of blood pressure. (ahajournals.org)
  • We studied alpha-adrenergic receptors in the cerebral and renal cortex of Milan hypertensive strain (MHS) and normotensive strain (MNS) rats, a genetic model of spontaneous hypertension linked to a kidney abnormality. (ahajournals.org)
  • In the renal cortex, the differences between MHS and MNS rats concerned alpha 2-adrenergic receptors only. (ahajournals.org)
  • Tao J, Wang HY and Malbon CC (2003) Protein kinase A regulates AKAP250 (gravin) scaffold binding to the beta2‐adrenergic receptor. (els.net)
  • Adrenergic alpha2 receptors (alpha2-adrenoceptors) are members of the adrenergic receptor group of G-protein-coupled receptors that also includes alpha1A, alpha1B, alpha1D, beta1, beta2 and beta3. (genecards.org)
  • Inactivation of dopamine D1 and D2 receptors by EEDQ was antagonized by olanzapine. (nih.gov)
  • G-proteins also activate Phospholipase C beta 1 ( PLC-beta1 ) [ 6 ]. (bio-rad.com)
  • Regions of the hamster alpha 1-adrenergic receptor (alpha 1 AR) that are important in GTP-binding protein (G protein)-mediated activation of phospholipase C were determined by studying the biological functions of mutant receptors constructed by recombinant DNA techniques. (duke.edu)
  • Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, including cardiovascular and pulmonary functions. (els.net)
  • Adrenergic responses were mediated by alpha 1- receptors localized to astrocytes because PE and NE increased [Ca2+]i of acutely isolated hippocampal astrocytes. (jneurosci.org)
  • The primary structure though most closely resembles that of an alpha 1-adrenergic receptor, having approximately 73% amino acid identity in the putative transmembrane domains with the previously isolated hamster alpha 1B receptor. (nih.gov)
  • Class A receptors, like ADRB2, OPRM1, ENDRA, D1AR and ADRA1B dissociate from beta-arrestin at or near the plasma membrane and undergo rapid recycling. (uniprot.org)
  • Receptor resensitization then requires that receptor-bound arrestin is removed so that the receptor can be dephosphorylated and returned to the plasma membrane. (uniprot.org)
  • [1] The neurotransmitter noradrenaline has higher affinity for the α1 receptor than does adrenaline (which is a hormone). (gutenberg.org)
  • The effect of surgical denervation on alpha-1 adrenergic receptor-stimulated inositol phosphate (IP) formation was examined in rat vas deferens. (elsevier.com)
  • Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. (meta.org)
  • Discover the latest research on adrenergic receptor trafficking here. (meta.org)
  • In ELISA experiment, the ELISA microwell plate was first coated with anti-FLAG M2 antibody, which recognizes the FLAG-tagged alpha(1A)-AR, then the cell lysis, anti-HA rabbit polyclonal antibody and HRP conjugated anti- rabbit antibody were added in turn. (bvsalud.org)
  • In co-immunoprecipitation experiments, HEK293 cells expressing alpha(1A)-AR or/and segment of BMP-1 were lysed and incubated with anti-FLAG M2 antibody, then the immunoprecipitation pellet was immunoblotted with either the HRP conjugated anti-FLAG antibody or the anti-HA antibody, which recognizes the HA-tagged segment of BMP-1. (bvsalud.org)
  • alpha1A -adrenergic receptors are stably expressed and stimulate cell migration and TGF-beta1 (zeige TGFB1 ELISA Kits ), IGF-1 (zeige IGF1 ELISA Kits ), hyaluronan and PIP (zeige PIP ELISA Kits ) production in human skin fibroblasts. (antikoerper-online.de)
  • The focus of work in this laboratory is on the elucidation of the molecular properties and regulatory mechanisms controlling the function of G protein-coupled receptors. (duke.edu)
  • Molecular cloning and expression of the cDNA for the alpha 1A-adrenergic receptor. (nih.gov)
  • Pharmacological and molecular cloning studies have demonstrated heterogeneity of alpha 1-adrenergic receptors. (nih.gov)
  • This procedure used internal cRNA standards as competitive templates that contained sequences complementary to the primers for alpha-1a, alpha-1b and alpha-1d adrenergic receptors and that differed in molecular size from the native sequences. (elsevier.com)
  • 1989) Molecular characterization of the human beta 3‐adrenergic receptor. (els.net)
  • Pre-diabetes augments neuropeptide Y1- and a1-receptor control of basal hindlimb vascular tone in young ZDF rats. (abcam.com)
  • Changes in brain alpha-adrenergic receptors after alpha-methyldopa administration to spontaneously hypertensive rats. (ahajournals.org)
  • alpha 1-Adrenergic receptor binding (prazosin) was increased, again more in hypertensive than in normotensive rats. (ahajournals.org)
  • The density of these receptors increased similarly with age in MHS and MNS rats. (ahajournals.org)
  • In addition, the lack of any guanylylimidodiphosphate effect on the l-epinephrine competition curve observed in MHS rats suggests the uncoupling of these receptors from the guanosine 5'-triphosphate binding protein. (ahajournals.org)
  • This is supported by reports that the expression and specific actions of NO synthase are elevated during late gestation in rats ( 1 , 5 ) and that the plasma level, metabolic production, and urinary excretion of cGMP, a second messenger of NO and a cellular mediator of vascular smooth muscle relaxation, are increased during pregnancy ( 4 ). (physiology.org)
  • Counterregulation by growth factor receptor tyrosine kinases and homologous desensitization by GRKs both stimulate the sequestration of β2‐AR. (els.net)
  • As assessed by NaDodSO4/polyacrylamide gel electrophoresis, the Mr 80,000 alpha 1-receptor ligand-binding subunit is a phosphopeptide containing 1.2 mol of phosphate per mol of alpha 1 receptor. (duke.edu)
  • In spite of significant sequence differences between human alpha-1ARs and their other species counterparts, previously established ligand selectivity remains fairly comparable. (duke.edu)
  • Ligand binding and RNA studies demonstrate that the GT1 cells contain both alpha(1A)- and alpha(1B)-ARs. (duke.edu)
  • Involved in the degradation of cAMP by recruiting cAMP phosphodiesterases to ligand-activated receptors. (uniprot.org)
  • These results demonstrate a critical role for the alpha(1B (zeige CACNA1B Proteine ))AR in baroreceptor-mediated adrenergic signaling at the vascular neuroeffector junction. (antikoerper-online.de)
  • Conclusion- Constitutive activation of α 1 -adrenergic signaling through the RTEF-1 transcription factor results in chronic elevation of PP1β expression and connexin dephosphorylation. (ahajournals.org)
  • Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling (By similarity). (uniprot.org)
  • protein kinase C modulates alpha1B-adrenergic receptor transfer to late endosomes and that Rab9 regulates this process and participates in G protein -mediated signaling turn-off. (antikoerper-online.de)