Wakefulness-Promoting Agents: 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.Receptors, Adrenergic, alpha-2: A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.Receptors, Adrenergic, beta-2: 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.Receptors, Adrenergic: 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.Receptors, Adrenergic, alpha: 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.Receptors, Adrenergic, beta-1: 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.Receptors, Adrenergic, alpha-1: 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.Receptors, Adrenergic, beta: 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.Receptors, Adrenergic, beta-3: 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.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.Adrenergic beta-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.Adrenergic beta-2 Receptor Agonists: Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.Adrenergic alpha-Antagonists: 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.Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Adrenergic beta-Agonists: Drugs that selectively bind to and activate beta-adrenergic receptors.Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.Adrenergic Antagonists: Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.Isoproterenol: 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.Adrenergic Agonists: Drugs that bind to and activate adrenergic receptors.Propanolamines: AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.Adrenergic beta-3 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.Norepinephrine: 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.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Adrenergic beta-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC BETA-1 RECEPTORS.Adrenergic alpha-1 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.Iodocyanopindolol: A highly selective and specific beta antagonist that is used to characterize beta-adrenoceptors.Dihydroalprenolol: 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.Epinephrine: 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.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.Adrenergic beta-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-1 RECEPTORS.alpha 1-Antitrypsin: Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.Adrenergic beta-Antagonists: 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.Pindolol: 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)Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Dioxanes: 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)Arrestins: Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.GTP-Binding Proteins: 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.-.Cyclic AMP: 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.Molecular Sequence Data: 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.Signal Transduction: 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.Propranolol: 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.Cricetinae: 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: 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.Butoxamine: A beta-2 selective adrenergic antagonist. It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS.Adrenergic beta-3 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-3 RECEPTORS.beta-Adrenergic Receptor Kinases: G-protein-coupled receptor kinases that mediate agonist-dependent PHOSPHORYLATION and desensitization of BETA-ADRENERGIC RECEPTORS.GTP-Binding Protein alpha Subunits, Gs: A family of heterotrimeric GTP-binding protein alpha subunits that activate ADENYLYL CYCLASES.Clenbuterol: A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.Cyclic AMP-Dependent Protein Kinases: 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.Transfection: 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.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Kinetics: The rate dynamics in chemical or physical systems.Protein Binding: 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.Binding, Competitive: 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.QuinoxalinesBase Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.Adrenergic Agents: 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.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.Amino Acid Sequence: 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.Oxymetazoline: A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)Rats, Sprague-Dawley: 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.
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- ...
... 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. "Dopamine: Biological activity". IUPHAR/BPS guide to pharmacology. International Union of Basic ... Dopamine binds to alpha-1 and beta-1 adrenergic receptors. Mediated through myocardial beta-1 adrenergic receptors, dopamine ...
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 0-7817-7311-3. 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-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- ... 1169 (1): 209-213. doi:10.1111/j.1749-6632.2009.04864.x. Archived from the original (PDF) on 15 April 2012. Retrieved 11 ...
... all of which act as receptor antagonists of muscarinic acetylcholine receptors) are effective for treating asthma and COPD- ... Beta2-adrenergic agonists are recommended for bronchospasm. Short acting (SABA) Terbutaline Salbutamol Levosalbutamol Long ... Both of these medications activate alpha-1 adrenergic receptors that result in smooth muscle constriction. Non-selective beta ... Beta blockers bind into the β2 receptors and block the action of epinephrine and norepinephrine from binding to its receptors, ...
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 ... It exhibits agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with ...
... alpha 1b- and alpha 1d-adrenergic receptor mRNA in the rat brain and spinal cord". Journal of chemical neuroanatomy. 13 (2): ... and syncope are associated with the body's poor ability to control blood pressure without active alpha-adrenergic receptors. ... A larger controlled Phase II "Clinical Trial of the Adrenergic Alpha-1 Antagonist Prazosin for Alcohol Dependence" is currently ... These receptors are found on vascular smooth muscle, where they are responsible for the vasoconstrictive action of ...
See also receptor antagonist) α 2 {\displaystyle \alpha _{2}} receptors. Agonists of α 2 {\displaystyle \alpha _{2}} receptors ... The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert opposite physiologic ... alpha _{2}} receptors in the vascular smooth muscle cells). Usage of β 2 {\displaystyle \beta _{2}} receptor agonists as ... However, in clinical practice drugs applied intravenously that are agonists of α 2 {\displaystyle \alpha _{2}} receptors ( ...
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." J. Pharmacol. Exp. Ther. 224 559-566. T. Hibino, M. ... An adrenergic antagonist selective for α1 receptors. Reversal of reserpine-induced hypothermia by a drug is a classical test ...
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/ ...
... alpha}2-Adrenergic Receptor Subtypes Archived 2011-03-05 at the Wayback Machine. J. Pharmacol. Exp. Ther. 322: pp. 214-221 ( ... Ephedrine works by turning on the α and β adrenergic receptors. Ephedrine was first isolated in 1885. It is on the World Health ... 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 ...
... 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 ... "Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine ...
... 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, ... 1969 Mar;12(2):326-9. PMID 5791620 Morrow AL, Creese I. Characterization of alpha 1-adrenergic receptor subtypes in rat brain: ... Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety. Pharmaceutica Acta Helvetiae. 2000 Mar;74(2- ...
... increased alpha 2 adrenergic receptor density, and decreased alpha 1 receptor density. Furthermore, norepinephrine transporter ... Increased numbers of T-Cells presenting activation markers, levels of neopterin, IFN gamma, sTNFR, and IL-2 receptors have been ... 5-HT2A receptor binding appears to be unregulated in depressed patients. Studies on 5-HTT binding are variable but tend towards ... 5-HT1A receptor binding literature is inconsistent however it leans towards a general decrease in the mesiotemporal cortex. ...
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. ...
... alpha-2 adrenergic receptor - alpha-beta T-cell antigen receptor - alpha-fetoprotein - alpha-globulin - alpha-macroglobulin - ... T-cell antigen receptors - tachykinin - tachykinin receptor - talin protein - tandem repeat sequence - taste bud - TATA box - ... alpha adrenergic receptor - Alpha helix - alpha-1 adrenergic receptor - ... interferon receptor - interferon type I - interferon type II - interferon-alpha - interferon-beta - interleukin receptor - ...
... alpha-adrenergic, and histamine receptors to clinical potency". The American Journal of Psychiatry. 137 (12): 1518-22. PMID ... This is likely due to the fact that chlorpromazine antagonizes the D2 receptor which is one of the receptors dopamine, a ... Histamine receptors (H1 receptors, accounting for sedation, antiemetic effect, vertigo, and weight gain) α1- and α2-adrenergic ... Also associated with weight gain as a result of blockage of the adrenergic alpha 1 receptor) M1 and M2 muscarinic acetylcholine ...
... 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 sarcoplasma contain a host of receptors (prostacyclin, endothelin, serotonin, muscarinic receptors, ...
The second group contains the alpha (α) adrenoreceptors. There are only α1 and α2 receptors. Adrenergic receptors are located ... Alpha-2 Adrenergic Receptor Agonists: A Review of Current Clinical Applications, Giovannitti Jr, J. A., Thoms, S. M., & ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... The first group of receptors are the beta (β) adrenergic receptors. There are β1, β2, and β3 receptors. ...
... an adrenergic receptor associated with the sympathetic nervous system and pharmacotherapeutics Alpha 1-antitrypsin deficiency, ... proteins or receptors. ... Alpha 1 or Alpha-1 may refer to: Alpha-1 adrenergic receptor, ... The Adventure Begins Alpha 1 (Robert Silverberg anthology) is a science fiction anthology edited by Robert Silverberg first ... a protein in humans that is associated with fetal development Alpha-One, a spacecraft in Buzz Lightyear of Star Command: ...
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: 832-839. McKeage, Kate; Plosker, Greg L. (2002-03-01). "Alfuzosin". ... are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha- ... Alpha-Blockers)" (PDF). British Hypertension Society. "CV Pharmacology , Alpha-Adrenoceptor Antagonists (Alpha-Blockers)". ...
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 ...
Additionally, l-THP displays significant binding to 5-HT1A and alpha-2 adrenergic receptors. In the case of 5-HT1A receptors, l ... Along with dopamine receptors, l-THP has been reported to interact with a number of other receptor types, including alpha-1 ... alpha adrenergic and serotonin receptors. The Ki values for l-THP at D1 and D2 dopamine receptors are approximately 124 nM (D1 ... adrenergic receptors, at which it functions as an antagonist, and GABA-A receptors, through positive allosteric modulation. ...
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 ... also called alpha-adrenergic blocking agents) constitute a variety of drugs that block alpha-1-adrenergic receptors in arteries ...
... s (originally, "eugrégorique" or "eugregoric"),[1] also known as wakefulness-promoting agents and wakefulness-promoting drugs, are a class of drugs that promote wakefulness and alertness.[2][3] They are medically indicated for the treatment of certain sleep disorders including excessive daytime sleepiness (EDS) in narcolepsy or obstructive sleep apnea (OSA).[2][3] They generally have a very low addictive potential.[2][3] Eugeroics are also often prescribed off-label for the treatment of EDS in idiopathic hypersomnia,[4] a rare and often debilitating sleep disorder which currently has no official treatments approved by the Food and Drug Administration (FDA). Modafinil and armodafinil each act as a selective, weak, atypical dopamine reuptake inhibitor (DRI)[2][3] whereas adrafinil acts as a prodrug for modafinil. Other eugeroics include solriamfetol, which acts as a norepinephrine-dopamine reuptake inhibitor (NDRI), and pitolisant, which acts as a histamine 3 (H₃) receptor ...
A norepinephrine releasing agent (NRA), also known as an adrenergic releasing agent, is a catecholaminergic type of drug which induces the release of norepinephrine (noradrenaline) and epinephrine (adrenaline) from the pre-synaptic neuron into the synapse. This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine therefore an increase in adrenergic neurotransmission. A closely related type of drug is a norepinephrine reuptake inhibitor (NRI). Another class of drugs that stimulates adrenergic activity is the adrenergic receptor agonist class. NRAs are used for a variety of clinical indications including the following: For the treatment of attention deficit hyperactivity disorder (ADHD) - e.g., amphetamine, methamphetamine, pemoline As anorectics in the treatment of obesity - e.g., amphetamine, phentermine, benzphetamine, ...
3.0.CO;2-3. PMID 9359081. Hoehe MR, Berrettini WH, Schwinn DA, Hsieh WT (1993). "A two-allele PstI RFLP for the alpha-1C adrenergic receptor gene (ADRA1C)". Hum. Mol. Genet. 1 (5): 349. doi:10.1093/hmg/1.5.349-a. PMID 1363873. Schwinn DA, Lomasney JW, Lorenz W, et al. (1990). "Molecular cloning and expression of the cDNA for a novel alpha 1-adrenergic receptor subtype". J. Biol. Chem. 265 (14): 8183-9. PMID 1970822. Hirasawa A, Shibata K, Horie K, et al. (1995). "Cloning, functional expression and tissue distribution of human alpha 1c-adrenoceptor splice variants". FEBS Lett. 363 (3): 256-60. doi:10.1016/0014-5793(95)00330-C. PMID 7737411. Diehl NL, Shreeve SM (1995). "Identification of the alpha 1c-adrenoceptor in rabbit arteries and the human saphenous vein using the polymerase chain reaction". Eur. J. Pharmacol. 268 (3): 393-8. ...
... s are the primary receptors on which clonidine and other imidazolines act. There are three main classes of imidazoline receptor: I1 is involved in inhibition of the sympathetic nervous system to lower blood pressure, I2 has as yet uncertain functions but is implicated in several psychiatric conditions, and I3 regulates insulin secretion. As of 2017, there are three known subtypes of imidazoline receptors: I1, I2, and I3. The I1 receptor appears to be a G protein-coupled receptor that is localized on the plasma membrane. It may be coupled to PLA2 signalling and thus prostaglandin synthesis. In addition, activation inhibits the sodium-hydrogen antiporter and enzymes of catecholamine synthesis are induced, suggesting that the I1 receptor may belong to the neurocytokine receptor family, since its signaling pathways are similar to those of interleukins. It is found in the neurons of the ...
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. They activate mitogenic responses and regulate growth and proliferation of many cells. ...
Adverse drug reactions associated with the use of beta blockers include: nausea, diarrhea, bronchospasm, dyspnea, cold extremities, exacerbation of Raynaud's syndrome, bradycardia, hypotension, heart failure, heart block, fatigue, dizziness, alopecia (hair loss), abnormal vision, hallucinations, insomnia, nightmares, sexual dysfunction, erectile dysfunction and/or alteration of glucose and lipid metabolism. Mixed α1/β-antagonist therapy is also commonly associated with orthostatic hypotension. Carvedilol therapy is commonly associated with edema.[44] Due to the high penetration across the blood-brain barrier, lipophilic beta blockers, such as propranolol and metoprolol, are more likely than other less lipophilic beta blockers to cause sleep disturbances, such as insomnia, vivid dreams and nightmares.[45] Adverse effects associated with β2-adrenergic receptor antagonist activity (bronchospasm, peripheral vasoconstriction, alteration of glucose and lipid ...
The alpha-2B adrenergic receptor (α2B adrenoceptor), is a G-protein coupled receptor. It is a subtype of the adrenergic receptor family. The human gene encoding this receptor has the symbol ADRA2B. ADRA2B orthologs have been identified in several mammals. α2-adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. This gene encodes the α2B subtype, which was observed to associate with eIF-2B, a guanine nucleotide exchange protein that functions in regulation of translation. A polymorphic variant of the α2B subtype, which lacks 3 glutamic acids from a glutamic acid repeat element, ...
... (INN) is a drug which is used in scientific research. It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor.[1][2] Idazoxan has been under investigation as an antidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment in schizophrenia. Due to its alpha-2 receptor antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area thought to be involved in the pathogenesis of schizophrenia. ...
Millan MJ, Newman-Tancredi A, Rivet JM, Brocco M, Lacroix P, Audinot V, Cistarelli L, Gobert A (1997). "S 15535, a novel benzodioxopiperazine ligand of serotonin (5-HT)1A receptors: I. Interaction with cloned human (h)5-HT1A, dopamine hD2/hD3 and h alpha2A-adrenergic receptors in relation to modulation of cortical monoamine release and activity in models of potential antidepressant activity". J Pharmacol Exp Ther. 282 (1): 132-147. PMID 9223549 ...
Millan MJ, Newman-Tancredi A, Rivet JM, Brocco M, Lacroix P, Audinot V, Cistarelli L, Gobert A. (1997). "S 15535, a novel benzodioxopiperazine ligand of serotonin (5-HT)1A receptors: I. Interaction with cloned human (h)5-HT1A, dopamine hD2/hD3 and h alpha2A-adrenergic receptors in relation to modulation of cortical monoamine release and activity in models of potential antidepressant activity". J Pharmacol Exp Ther. 282 (1): 132-147. PMID 9223549. ...
Ruuskanen JO, Xhaard H, Marjamäki A, Salaneck E, Salminen T, Yan YL, Postlethwait JH, Johnson MS, Larhammar D, Scheinin M (January 2004). "Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in zebrafish". Molecular Biology and Evolution 21 (1): 14-28. PMID 12949138. doi:10.1093/molbev/msg224. Cite uses deprecated parameter ...
Ruuskanen JO, Xhaard H, Marjamäki A, Salaneck E, Salminen T, Yan YL, Postlethwait JH, Johnson MS, Larhammar D, Scheinin M (2004). „Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in zebrafish". Molecular Biology and Evolution. 21 (1): 14-28. PMID 12949138. doi:10.1093/molbev/msg224 ...
Hoyer, D.; Engel, G. (1983). „Binding of 125I-cyanopindolol to beta-1-adrenoceptors in a high and low affinity state". Journal of Receptor Research. 3 (1-2): 45-59 ...
alpha 2C Adrenergic Receptor兔多克隆抗体(ab123368)可与人样本反应并经WB实验严格验证。 ... Anti-alpha 2C Adrenergic Receptor抗体. 参阅全部 alpha 2C Adrenergic Receptor 一抗. ... Neuroscience Neurotransmission Receptors / Channels GPCR Adrenergic Receptors Anti-alpha 2C Adrenergic Receptor抗体(ab123368). ... The alpha 2C Adrenergic Receptor controls the release of neurotransmitter from
It contains beta receptors which h lends it an amazing property of increasing fat-free mass in human body. You must now that ... Hoshino D et al . Clenbuterol, a beta2-adrenergic agonist, reciprocally alters PGC-1 alpha and RIP140 and reduces fatty acid ... then it would have harmful effects on your health causing receptor over-saturation. ... It also possesses the ability to promote lipolysis via acting on ß3 receptors in the adipose tissue. For years, Clenbuterol has ...
Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ... 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 ...
... 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 ...
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 ...
... 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 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- ...
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 ...
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. ...
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 ...
... 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 ...
IP accumulation was decreased about 40-fold after receptor inactivation with 1 μM phenoxybenzamine. These results suggest that ... Minneman, K. P., Mumford, G. K., & Abel, P. W. (1988). High efficiency coupling of alpha-1 adrenergic receptors to inositol ... Minneman, K. P. ; Mumford, G. K. ; Abel, P. W. / High efficiency coupling of alpha-1 adrenergic receptors to inositol ... Minneman, KP, Mumford, GK & Abel, PW 1988, High efficiency coupling of alpha-1 adrenergic receptors to inositol phospholipid ...
... alpha-1b and alpha-1d adrenergic receptors and that differed in molecular size from the native sequences. Total RNA was ... In the present study, we quantified alpha-1a, alpha-1b and alpha-1d adrenergic receptor mRNA in 19 adult rat tissues through ... In the present study, we quantified alpha-1a, alpha-1b and alpha-1d adrenergic receptor mRNA in 19 adult rat tissues through ... In the present study, we quantified alpha-1a, alpha-1b and alpha-1d adrenergic receptor mRNA in 19 adult rat tissues through ...
1988) Alpha-2A and alpha-2B adrenergic receptor subtypes: Antagonist binding in tissues and cell lines containing only one ... 1995) Alpha-2 adrenergic receptors: Immunohistochemical localization and role in mediating inhibition of adrenergic RVLM ... 1994) Characterization of [3H]RX821002 binding to alpha-2 adrenergic receptor subtypes. J Pharmacol Exp Ther 268:1362-1367. ... 1994) Alpha2A-adrenergic receptors are present in lower brainstem catecholaminergic and serotonergic neurons innervating spinal ...
Interaction of Imidazoline Alpha-Adrenergic Receptor Antagonists with Histamine Receptors. Powell, James R.; Shamel, L. Blair ... Thyroxine and Propylthiouracil Effects on Alpha- and Beta-Adrenergic Receptor Number, ATPase Activities, and Sialic Acid ...
... but may have similar receptor occupancy to the more potent SGAs.(Seeman, 2002) It has alpha-adrenergic antagonism and ... It has less affinity for D2 receptors than risperidone and a greater affinity for 5HT2A and 5HT2C serotonin receptors. ... It is an antagonist at alpha-2-adrenergic autoreceptors thereby increasing norepinephrine and serotonin release, and it blocks ... Clonidine, initially developed as an antihypertensive, is an alpha-2-adrenergic autoreceptor agonist which serves to decrease ...
  • 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)
  • 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)
  • Shumay E, Gavi S, Wang HY and Malbon CC (2004) Trafficking of beta2adrenergic receptors: insulin and beta‐agonists regulate internalisation by distinct cytoskeletal pathways. (els.net)
  • 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)
  • 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)
  • Other effects on smooth muscle are contraction in: Ureter Uterus (when pregnant) Urethral sphincter Bronchioles (although minor to the relaxing effect of β2 receptor on bronchioles) Iris dilator muscle Seminal tract, resulting in ejaculation Activation of α1-adrenergic receptors produces anorexia and partially mediates the efficacy of appetite suppressants like phenylpropanolamine and amphetamine in the treatment of obesity. (wikipedia.org)
  • Activation of α 1 -adrenergic receptors produces anorexia and partially mediates the efficacy of appetite suppressants like phenylpropanolamine and amphetamine in the treatment of obesity . (gutenberg.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)
  • 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)
  • Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling (By similarity). (uniprot.org)
  • β2- Adrenergic Receptor-Mediated HIF-1α Upregulation Mediates Blood Brain Barrier Damage in Acute Cerebral Ischemia Disruption of the blood brain barrier (BBB) within the thrombolytic time window is an antecedent event to intracerebral hemorrhage in ischemic stroke. (tripdatabase.com)
  • This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. (genecards.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)
  • 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)
  • Saw palmetto extract (SPE), used widely for the treatment of benign prostatic hyperplasia (BPH) has been shown to bind alpha(1)-adrenergic, muscarinic and 1,4-dihydropyridine (1,4-DHP) calcium channel antagonist receptors. (nih.gov)
  • Observational Study in Patients Suffering From Benign Prostatic Hyperplasia Treated With Alpha - adrenergic Blockade Observational Study in Patients Suffering From Benign Prostatic Hyperplasia Treated With Alpha - adrenergic Blockade - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. (tripdatabase.com)
  • Blockade of the alpha 1 receptor decreases urethral resistance and may relieve the obstruction and BPH symptoms. (nih.gov)
  • 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)
  • 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)
  • Pre-diabetes augments neuropeptide Y1- and a1-receptor control of basal hindlimb vascular tone in young ZDF rats. (abcam.com)
  • 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)