Drugs that bind to and activate adrenergic receptors.
Drugs that selectively bind to and activate alpha adrenergic receptors.
Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.
An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
An agonist of RECEPTORS, ADRENERGIC ALPHA-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of DEXMEDETOMIDINE.
Drugs that selectively bind to and activate beta-adrenergic receptors.
Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.
An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.
A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.
A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.
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.
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.
A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.
An alpha-1 adrenergic agonist that causes prolonged peripheral VASOCONSTRICTION.
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.
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.
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.
An adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic.
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.
A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.
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.
Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.
A imidazole derivative that is an agonist of ADRENERGIC ALPHA-2 RECEPTORS. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound.
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 long-acting beta-2-adrenergic receptor agonist.
A norepinephrine derivative used as a vasoconstrictor agent.
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.
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.
Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.
Drugs that bind to and activate dopamine receptors.
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.
The relationship between the dose of an administered drug and the response of the organism to the drug.
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.
AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.
Drugs that mimic the effects of stimulating postganglionic adrenergic sympathetic nerves. Included here are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters.
Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.
A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.
Compounds based on a propanolamine attached via an OXYGEN atom to a phenoxy ring. The side chain is one carbon longer than PHENYLETHYLAMINES.
A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.
An adrenergic alpha-2 agonist used as a sedative, analgesic and centrally acting muscle relaxant in VETERINARY MEDICINE.
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.
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)
A thermogenic form of adipose tissue composed of BROWN ADIPOCYTES. It is found in newborns of many species including humans, and in hibernating mammals. Brown fat is richly vascularized, innervated, and densely packed with MITOCHONDRIA which can generate heat directly from the stored lipids.
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.
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.
Agents affecting the function of, or mimicking the actions of, the autonomic nervous system and thereby having an effect on such processes as respiration, circulation, digestion, body temperature regulation, certain endocrine gland secretions, etc.
An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.
Drugs that bind to and activate cholinergic receptors.
A cyclic nucleotide formed from CYTIDINE TRIPHOSPHATE by the action of cytidylate cyclase. It is a potential cyclic nucleotide intracellular mediator of signal transductions.
Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.
AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.
Introduction of therapeutic agents into the spinal region using a needle and syringe.
Drugs that inhibit the actions of the sympathetic nervous system by any mechanism. The most common of these are the ADRENERGIC ANTAGONISTS and drugs that deplete norepinephrine or reduce the release of transmitters from adrenergic postganglionic terminals (see ADRENERGIC AGENTS). Drugs that act in the central nervous system to reduce sympathetic activity (e.g., centrally acting alpha-2 adrenergic agonists, see ADRENERGIC ALPHA-AGONISTS) are included here.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
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.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
A glucocorticoid derivative used topically in the treatment of various skin disorders. It is usually employed as a cream, gel, lotion, or ointment. It has also been used topically in the treatment of inflammatory eye, ear, and nose disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p732)
One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.
The tear-forming and tear-conducting system which includes the lacrimal glands, eyelid margins, conjunctival sac, and the tear drainage system.
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.
Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.
One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
A general class of ortho-dihydroxyphenylalkylamines derived from tyrosine.
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
Drugs that mimic the effects of parasympathetic nervous system activity. Included here are drugs that directly stimulate muscarinic receptors and drugs that potentiate cholinergic activity, usually by slowing the breakdown of acetylcholine (CHOLINESTERASE INHIBITORS). Drugs that stimulate both sympathetic and parasympathetic postganglionic neurons (GANGLIONIC STIMULANTS) are not included here.
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.
Antidiuretic hormones released by the NEUROHYPOPHYSIS of all vertebrates (structure varies with species) to regulate water balance and OSMOLARITY. In general, vasopressin is a nonapeptide consisting of a six-amino-acid ring with a cysteine 1 to cysteine 6 disulfide bridge or an octapeptide containing a CYSTINE. All mammals have arginine vasopressin except the pig with a lysine at position 8. Vasopressin, a vasoconstrictor, acts on the KIDNEY COLLECTING DUCTS to increase water reabsorption, increase blood volume and blood pressure.
A set of BACTERIAL ADHESINS and TOXINS, BIOLOGICAL produced by BORDETELLA organisms that determine the pathogenesis of BORDETELLA INFECTIONS, such as WHOOPING COUGH. They include filamentous hemagglutinin; FIMBRIAE PROTEINS; pertactin; PERTUSSIS TOXIN; ADENYLATE CYCLASE TOXIN; dermonecrotic toxin; tracheal cytotoxin; Bordetella LIPOPOLYSACCHARIDES; and tracheal colonization factor.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.
A ring of tissue extending from the scleral spur to the ora serrata of the RETINA. It consists of the uveal portion and the epithelial portion. The ciliary muscle is in the uveal portion and the ciliary processes are in the epithelial portion.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
One of the virulence factors produced by virulent BORDETELLA organisms. It is a bifunctional protein with both ADENYLYL CYCLASES and hemolysin components.
Bluish-colored region in the superior angle of the FOURTH VENTRICLE floor, corresponding to melanin-like pigmented nerve cells which lie lateral to the PERIAQUEDUCTAL GRAY.
An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.
The metabolic process of breaking down LIPIDS to release FREE FATTY ACIDS, the major oxidative fuel for the body. Lipolysis may involve dietary lipids in the DIGESTIVE TRACT, circulating lipids in the BLOOD, and stored lipids in the ADIPOSE TISSUE or the LIVER. A number of enzymes are involved in such lipid hydrolysis, such as LIPASE and LIPOPROTEIN LIPASE from various tissues.
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
Liquid components of living organisms.
A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are not addictive. Many non-narcotic analgesics are offered as NONPRESCRIPTION DRUGS.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)
A glucocorticoid given, as the free alcohol or in esterified form, orally, intramuscularly, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. (From Martindale, The Extra Pharmacopoeia, 30th ed, p739)
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
Agents that cause an increase in the expansion of a bronchus or bronchial tubes.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
Seven membered heterocyclic rings containing a NITROGEN atom.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
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.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Elements of limited time intervals, contributing to particular results or situations.
The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.
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.-.
Proteins encoded by the mitochondrial genome or proteins encoded by the nuclear genome that are imported to and resident in the MITOCHONDRIA.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.
The rate dynamics in chemical or physical systems.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
The number of times the HEART VENTRICLES contract per unit of time, usually per minute.
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
Compounds capable of relieving pain without the loss of CONSCIOUSNESS.
Drugs that bind to and activate excitatory amino acid receptors.
Gated, ion-selective glycoproteins that traverse membranes. The stimulus for ION CHANNEL GATING can be due to a variety of stimuli such as LIGANDS, a TRANSMEMBRANE POTENTIAL DIFFERENCE, mechanical deformation or through INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS.
The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM.
A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511)
Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.
The hollow, muscular organ that maintains the circulation of the blood.
A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.
Any of the ruminant mammals with curved horns in the genus Ovis, family Bovidae. They possess lachrymal grooves and interdigital glands, which are absent in GOATS.
A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE).
The thoracolumbar division of the autonomic nervous system. Sympathetic preganglionic fibers originate in neurons of the intermediolateral column of the spinal cord and project to the paravertebral and prevertebral ganglia, which in turn project to target organs. The sympathetic nervous system mediates the body's response to stressful situations, i.e., the fight or flight reactions. It often acts reciprocally to the parasympathetic system.
The administration of drugs by the respiratory route. It includes insufflation into the respiratory tract.
A 51-amino acid pancreatic hormone that plays a major role in the regulation of glucose metabolism, directly by suppressing endogenous glucose production (GLYCOGENOLYSIS; GLUCONEOGENESIS) and indirectly by suppressing GLUCAGON secretion and LIPOLYSIS. Native insulin is a globular protein comprised of a zinc-coordinated hexamer. Each insulin monomer containing two chains, A (21 residues) and B (30 residues), linked by two disulfide bonds. Insulin is used as a drug to control insulin-dependent diabetes mellitus (DIABETES MELLITUS, TYPE 1).
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
Drugs used to cause constriction of the blood vessels.
Refers to animals in the period of time just after birth.
Established cell cultures that have the potential to propagate indefinitely.
Excessive accumulation of extravascular fluid in the lung, an indication of a serious underlying disease or disorder. Pulmonary edema prevents efficient PULMONARY GAS EXCHANGE in the PULMONARY ALVEOLI, and can be life-threatening.
A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.
A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.
The application of drug preparations to the surfaces of the body, especially the skin (ADMINISTRATION, CUTANEOUS) or mucous membranes. This method of treatment is used to avoid systemic side effects when high doses are required at a localized area or as an alternative systemic administration route, to avoid hepatic processing for example.
Small polyhedral outpouchings along the walls of the alveolar sacs, alveolar ducts and terminal bronchioles through the walls of which gas exchange between alveolar air and pulmonary capillary blood takes place.
A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.
A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
The action of a drug in promoting or enhancing the effectiveness of another drug.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP.
An involuntary movement or exercise of function in a part, excited in response to a stimulus applied to the periphery and transmitted to the brain or spinal cord.
Specialized connective tissue composed of fat cells (ADIPOCYTES). It is the site of stored FATS, usually in the form of TRIGLYCERIDES. In mammals, there are two types of adipose tissue, the WHITE FAT and the BROWN FAT. Their relative distributions vary in different species with most adipose tissue being white.
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
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.
A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.
The processes of heating and cooling that an organism uses to control its temperature.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.
A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)
Transport proteins that carry specific substances in the blood or across cell membranes.
Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
Arteries which arise from the abdominal aorta and distribute to most of the intestines.
The flow of BLOOD through or around an organ or region of the body.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
A primary source of energy for living organisms. It is naturally occurring and is found in fruits and other parts of plants in its free state. It is used therapeutically in fluid and nutrient replacement.
Compounds that bind to and activate PURINERGIC RECEPTORS.
A nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required. (From AMA Drug Evaluations Annual, 1994, p178)
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.
A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
Treatment process involving the injection of fluid into an organ or tissue.
The nonstriated involuntary muscle tissue of blood vessels.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
Compounds that bind to and activate ADRENERGIC BETA-1 RECEPTORS.
A family of hexahydropyridines.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
A group of CORTICOSTEROIDS that affect carbohydrate metabolism (GLUCONEOGENESIS, liver glycogen deposition, elevation of BLOOD SUGAR), inhibit ADRENOCORTICOTROPIC HORMONE secretion, and possess pronounced anti-inflammatory activity. They also play a role in fat and protein metabolism, maintenance of arterial blood pressure, alteration of the connective tissue response to injury, reduction in the number of circulating lymphocytes, and functioning of the central nervous system.
An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.
Agents that increase calcium influx into calcium channels of excitable tissues. This causes vasoconstriction in VASCULAR SMOOTH MUSCLE and/or CARDIAC MUSCLE cells as well as stimulation of insulin release from pancreatic islets. Therefore, tissue-selective calcium agonists have the potential to combat cardiac failure and endocrinological disorders. They have been used primarily in experimental studies in cell and tissue culture.
Cells in the body that store FATS, usually in the form of TRIGLYCERIDES. WHITE ADIPOCYTES are the predominant type and found mostly in the abdominal cavity and subcutaneous tissue. BROWN ADIPOCYTES are thermogenic cells that can be found in newborns of some species and hibernating mammals.
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 part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
A selective D1 dopamine receptor agonist used primarily as a research tool.
A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.
Drugs used to cause dilation of the blood vessels.
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.
Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.
A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).
Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed)
A dopamine D2/D3 receptor agonist.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments.
Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.
A nuclear transcription factor. Heterodimerization with RETINOID X RECEPTOR ALPHA is important in regulation of GLUCOSE metabolism and CELL GROWTH PROCESSES. It is a target of THIAZOLIDINEDIONES for control of DIABETES MELLITUS.

Characterization of alpha1-adrenoceptor subtypes mediating vasoconstriction in human umbilical vein. (1/329)

1. The present study attempted to characterize pharmacologically the subtypes of alpha-adrenoceptors mediating contractions in human umbilical vein (HUV). 2. HUV rings were mounted in isolated organ baths and cumulative concentration-response curves were constructed for the alpha-adrenoceptor agonists phenylephrine and adrenaline. Adrenaline was more potent than phenylephrine (pD2=7.29 and 6.04 respectively). 3. Isoproterenol exhibited no agonism on KCl pre-contracted HUV rings. Propranolol (1 microM) and rauwolscine (0.1 microM) did not affect the concentration-response curves to adrenaline. These results demonstrate the lack of involvement of functional beta-or alpha2-adrenoceptors in adrenaline-induced vasoconstriction. 4. The non subtype selective alpha1-adrenoceptor antagonist prazosin was evaluated on phenylephrine and adrenaline concentration-response curves. The effects of the competitive alpha1A and alpha1D-adrenoceptor antagonists, 5-methyl urapidil and BMY 7378 and the irreversible alpha1B selective compound chloroethylclonidine (CEC) were also evaluated on adrenaline concentration-response curves. 5. The potencies of prazosin against responses mediated by adrenaline (pA2= 10.87) and phenylephrine (pA2= 10.70) indicate the involvement of prazosin-sensitive functional alpha1-adrenoceptor subtype in vasoconstriction of the HUV. 6. The potencies of 5-methyl urapidil (pA2 = 6.70) and BMY 7378 (pA2= 7.34) were not consistent with the activation of an alpha1A- or alpha1D-adrenoceptor population. 7. Exposure to a relatively low CEC concentration (3 microM) abolished the maximum response to adrenaline suggesting that this response was mediated by an alpha1B-adrenoceptor subtype. 8. We conclude that HUV express a prazosin-sensitive functional alpha1-adrenoceptor resembling the alpha1B-subtype according with the low pA2 values for both 5-methyl urapidil and BMY 7378 and the high sensitivity to CEC.  (+info)

Sympathovagal balance: how should we measure it? (2/329)

There are complex interactions between the sympathetic and parasympathetic nervous system inputs to the sinus node. The concept of "sympathovagal balance" reflects the autonomic state resulting from the sympathetic and parasympathetic influences. Despite widespread usage of a variety of heart rate (HR) variability parameters as indexes of sympathovagal balance, no index has been validated as a measure of sympathovagal balance. This study evaluated the utility of HR, HR variability, and a new parameter termed the vagal-sympathetic effect (VSE) as indexes of sympathovagal balance. The ideal parameter had to satisfy the following criteria: 1) the index should vary similarly among subjects in response to different autonomic conditions; 2) the variability in the index among subjects exposed to the same autonomic conditions should be small; and 3) the response of the index to various autonomic conditions should reflect the underlying changes in physiological state and have a meaningful interpretation. Volunteers [8 men, 6 women; mean age 28.5 +/- 4.8 (SD) yr] were evaluated for the effects of sympathetic and parasympathetic stimulation and blockade on HR and HR variability. VSE was defined as the ratio of the R-R interval to the intrinsic R-R interval. VSE and R-R interval consistently changed in the expected directions with parasympathetic and sympathetic stimulation and blockade. A general linearized model was used to evaluate the response of each parameter. VSE and R-R interval had r2 values of 0.847 and 0.852, respectively. Natural logarithm of the low-frequency power had an r2 value of 0.781 with lower r2 values for all the other HR variability parameters. The coefficient of variation was also lowest for each condition tested for the VSE and the R-R interval. VSE and R-R interval best satisfy the criteria for the ideal index of sympathovagal balance. Because it is impractical under most conditions to measure the VSE as the index of sympathovagal balance, the most suitable index is the R-R interval.  (+info)

"Uncaging" using optical fibers to deliver UV light directly to the sample. (3/329)

Photolysis or "uncaging" of caged compounds represents a significant tool in cell biology and chemistry. It provides a means for quantitative control of compound delivery with temporal and spatial resolution while observing their consequences for cellular signaling. We discuss the use of ultraviolet-transmitting optical fibers to directly deliver UV energy to the sample, combined with a nitrogen pulsed laser as a source of UV light. In this approach the size of the photolysis area is regulated by the exit aperture of the fiber tip which is controlled by pulling the optical fibers to desirable diameters. A diode (red) laser that is also coupled to the optical fiber aids the location of UV energy delivery through the fiber. We used this method to quantitatively uncage norepinephrine and calcium. The major advantage of this photolysis approach is its independence of microscope objectives and traditional optical pathways. Because the optical pathway of the microscope needs no modification to accommodate this photolysis system, integration with other experimental methods, such as electrochemistry, electrophysiology, confocal microscopy, and wide-field epifluorescence microscopy, is relatively simple.  (+info)

Contributions of adenosine receptor activation to the ocular actions of epinephrine. (4/329)

PURPOSE: Epinephrine is an effective drug for glaucoma treatment. However, the mechanisms responsible for the ocular hypotensive action of this compound are not completely understood. Adenosine is an autacoid released by all cells. This study evaluated the role of adenosine receptor activation in epinephrine-induced changes in ocular function. METHODS: Rabbits were pretreated topically with the moderately selective adenosine A1 antagonist 8-(p-sulfophenyl)theophylline (8-SPT) or the adenosine A2 antagonist 3,7-dimethyl-l-propargylxanthine (DMPX). Epinephrine (500 microg) was then administered, and intraocular pressures (IOPs), pupil diameters (PDs), or total outflow facility was evaluated. In a separate group of animals, epinephrine or vehicle was administered, and aqueous humor samples obtained to evaluate changes in aqueous humor purine levels by means of high-performance liquid chromatography. RESULTS: In control animals, epinephrine produced a biphasic change in IOP: an initial rise in IOP of approximately 1 mm Hg from 1/2 to 1 hour followed by significant reduction in IOP of 8 to 9 mm Hg from 3 to 5 hours postadministration. These animals also exhibited a significant increase in PD of 2 to 3 mm from 1/2 to 2 hours postadministration. Pretreatment with 8-SPT (1000 microg) enhanced the initial rise in IOP, while significantly inhibiting the ocular hypotensive response. Pretreatment with 8-SPT also significantly enhanced the epinephrine-induced increase in PD. Inhibition of the epinephrine-induced reduction in IOP by 8-SPT was dose-related with an IC50 of 446 microg. Administration of 8-SPT alone did not significantly alter IOP or PD. The A2 antagonist DMPX did not alter the epinephrine-induced change in IOP or PD. In rabbits pretreated with 8-SPT, the epinephrine-induced increase in outflow facility was significantly reduced by 60% when compared with those in rabbits treated with epinephrine alone. In vehicle-treated rabbits, aqueous humor adenosine and inosine levels were 2.7 +/- 0.38 and 29 +/- 4.2 ng/100 microl, respectively. Three hours after epinephrine administration, adenosine and inosine levels had significantly increased to 11 +/- 1.6 and 66 +/- 4.4 ng/100 microl, respectively. CONCLUSIONS: These results support the idea that in rabbits epinephrine administration stimulates adenosine release in the anterior segment. This rise in endogenous levels of adenosine then leads to the activation of ocular adenosine receptors and is in part responsible for the ocular hypotensive action of epinephrine.  (+info)

Activation of a thioesterase specific for very-long-chain fatty acids by adrenergic agonists in perfused hearts. (5/329)

We have recently described an acyl-CoA thioesterase specific for very-long-chain fatty acids, named ARTISt, that regulates steroidogenesis through the release of arachidonic acid in adrenal zona fasciculata cells. In this paper we demonstrate the presence of the protein as a 43 kDa band and its mRNA in cardiac tissue. The activity of the protein was measured using an heterologous cell-free assay in which it is recombined with adrenal microsomes and mitochondria to activate mitochondrial steroidogenesis. Isoproterenol and phenylephrine activate the enzyme in a dose-dependent manner (10(-10)-10(-6) M). Both propranolol (10(-5) M) and prazosin (10(-5) M) block the action of isoproterenol and phenylephrine respectively. Antipeptide antibodies against the serine lipase motif of the protein and the Cys residue present in the catalytic domain also block the activity of the protein. Taken together, our results confirm the presence of ARTISt in heart and provide evidence for a catecholamine-activated regulatory pathway of the enzyme in that tissue.  (+info)

Influence of G protein type on agonist efficacy. (6/329)

An agonist at a specific G protein-coupled receptor may exhibit a range of efficacies for any given response in a cell-specific manner. We report that the relationship between different states of agonism is regulated by the type of G protein expressed in the cell. In NIH-3T3 alpha(2)-adrenergic receptor (AR) transfectants, the alpha(2)-AR agonists clonidine, oxymetazoline, UK-14304, and epinephrine increased [(35)S]guanosine-5'-O-(3-thio)triphosphate binding in a dose-dependent manner from a basal value of 101.2 +/- 6. 5 fmol/mg to a maximal response (100 microM) of 196.6 +/- 9.8, 182.3 +/- 2, 328.1 +/- 11.2, and 340.6 +/- 3 fmol/mg, respectively. Thus, clonidine and oxymetazoline behaved as partial agonists. Receptor-mediated activation of G proteins in membrane preparations was blocked by cell pretreatment with pertussis toxin, indicating receptor coupling to the subgroup of pertussis toxin-sensitive G protein (Gialpha2,3) expressed in NIH-3T3 cells. Ectopic expression of Goalpha1 but not Gialpha1 increased the relative efficacy of clonidine and oxymetazoline such that the two ligands now behaved as close to full agonists in this assay system. The relationship between full and partial agonists in the different genetic backgrounds was not altered by progressive reduction in the amount of G protein available for coupling to receptor. The increased efficacy observed for clonidine in the Goalpha1 transfectants was not due to changes in the relative affinities or amounts of high-affinity, Gpp(NH)p-sensitive binding of agonist. These data suggest that there is little difference in the ability of clonidine to interact with or stabilize alpha(2)-AR-Gialpha2/Gialpha3 versus alpha(2)-AR-Goalpha1 complexes, but that the subsequent step of signal transfer from receptor to G protein is more readily achieved for the clonidine/alpha(2)-AR/Goalpha1 complex. Such observations have important implications for receptor theory and drug development.  (+info)

Differential effects of epinephrine and norepinephrine on cAMP response and g(i3)alpha protein expression in cultured sympathetic neurons. (7/329)

The effect of 24-h pretreatment with epinephrine (EPI) or norepinephrine (NE) on alpha(2)- and beta-adrenoceptor agonist-induced, cAMP responses and G(i3)alpha-protein expression was studied in primary cultures of rat superior cervical ganglionic (SCG) neurons. SCG neurons, 10 to 12 days in culture, accumulated cAMP when stimulated with the beta-adrenoceptor agonist isoproterenol and the preferential beta(2)-adrenoceptor antagonist ICI 118,551 blocked this response. Similarly, the preferential alpha(2)-adrenoceptor agonist UK14,304 inhibited forskolin-stimulated cAMP accumulation, implying that cultured SCG neurons possess functional alpha(2)- and beta(2)-adrenoceptors. A 24-h treatment of SCG neurons with EPI or NE induced desensitization of the cAMP response to the beta-adrenoceptor agonist isoproterenol. Simultaneously, EPI treatment increased the maximal inhibitory cAMP response to the alpha(2)-adrenoceptor agonist UK14,304 and NE was without effect. Immunoblotting analyses of G(i3)alpha subunits revealed that 24-h EPI but not NE treatment induces a 3- to 4-fold increase in the expression of G(i3)alpha subunits. Furthermore, EPI-induced up-regulation of alpha-subunit expression can be blocked by the preferential beta(2)-adrenoceptor antagonist ICI 118,551 but not by the preferential beta(1)-adrenoceptor antagonist CGP 20712A. Our results suggest that changes in alpha(2)-adrenoceptor responsiveness induced by EPI may involve activation of beta(2)-adrenoceptors that influence the expression of inhibitory G proteins. Thus, primary cultures of sympathetic neurons by possessing functional alpha(2)- and beta-adrenoceptors may be a suitable model system to study the signaling mechanisms of "cross talk" between these adrenoceptor subtypes, which are known to play a central role in cardiovascular function.  (+info)

Mental well-being in alcohol withdrawal: relationship to alpha2-adrenoceptor function. (8/329)

The possible relationship between postsynaptic alpha2-adrenoceptor function, as assessed by the growth hormone (GH) response to clonidine (CLON) and aspects of mental well-being by self-report of mood using the Swedish Mood Adjective Check List, was investigated in alcohol-dependent patients in the early withdrawal period. Patients had blunted GH responses to CLON and worse mental well-being than control subjects immediately after the end of alcohol intake. No relation was found between mental well-being and postsynaptic alpha2-adrenoceptor function. After 1 week, the GH responses to CLON remained blunted, whereas the state of mental well-being had improved to levels similar to those of control subjects. The results further support a downregulated alpha2-adrenoceptor function during 1 week of alcohol withdrawal. Furthermore, even if subsensitive postsynaptic alpha2-adrenoceptor function was not generally related to state of mood, patients with the lowest postsynaptic alpha2-adrenoceptor function reported the highest levels in the dimensions pleasantness/unpleasantness and activation/deactivation when sober.  (+info)

1. Earlier studies have shown that exposure of fat-cells to insulin results in the rapid increased phosphorylation of an acid-soluble 22 kDa protein and that increases in phosphorylation were also evident in cells exposed to adrenaline [Belsham & Denton (1980) Biochem. Soc. Trans. 8, 382-383; Belsham, Brownsey, Hughes & Denton (1980) Diabetologia 18, 307-312]. 2. The effects of adrenaline are shown to be brought about through beta-adrenergic receptors and to be mimicked by other agents which increase cell cyclic AMP concentrations. The maximum extent of phosphorylation is about 60% of that observed with insulin. Increased phosphorylation is also observed in fat-cells exposed to vasopressin, oxytocin and phorbol esters, but not to alpha-adrenergic agonists. 3. No changes in the phosphorylation of the protein are evident in epididymal fat-pads from fat-fed, starved or starved/refed animals, despite the large changes in protein composition of fat-cells which accompany these nutritional alterations. ...
Cheng, N., Enright, K., Roberts, P., Turner, C., Browne, G. (2012). Primary Cardiac Arrest Following Sport or Exertion in Children Presenting to an Emergency Department: Chest Compressions and Early Defibrillation Can Save Lives, But Is Intravenous Epinephrine Always Appropriate? Pediatric Emergency Care, 28(4), 336-339. [More Information] ...
In this study the, in vitro, influence of arachidonic acid metabolites on human β-adrenoceptors was investigated. Incubation of normal human pulmonary membranes with PAF, LTB4 and LTC4 affected...
The dose-response curves of epinephrine given either IV or endotracheally (ET) were compared during resuscitation from electromechanical dissociation (EMD). Ten anesthetized dogs were subjected to a two-minute period of electrically induced ventricular fibrillation (VF) followed by defibrillation without CPR to produce EMD. Mechanical CPR was followed by injection of either ET or IV epinephrine. Successful response was defined as a return of pulsatile blood pressure within two minutes of drug administration. Using log-dose increments of epinephrine, experimental trials were repeated in each animal. The IV and ET median effective doses were 14 and 130 g/kg, respectively. When the trials were successful, the time between drug administration and either arterial blood pressure increases or return of spontaneous circulation did not differ significantly for the ET and IV groups. These results show that the dosage for epinephrine delivered ET must be higher than the IV dosage to achieve the same response
Pediatric epinephrine dose calculator helps you estimate the amount of epinephrine needed for IV, IM, SC, ET and Nebulizer administration. You can convert your results between mL and mg units.
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Indirect agonists do not physically bind adrenergic receptors. Instead, these compounds indirectly lead to receptor activation through a variety of possible mechanisms which include promoting release of endogenously-stored norepinephrine from presynaptic terminals as well as inhibition of norepinephrine re-uptake and degradation from the synapse ...
The material on this site is provided for informational purposes only and is not medical advice. Never delay or disregard seeking professional medical advice from your doctor or other qualified healthcare provider because of something you have read on this website. Information obtained in this website are not exhaustive and do not cover all diseases, ailments, physical conditions or their treatment. You should always speak with your doctor before you start, stop, or change any prescribed part of your care plan or treatment. Visit a website it is never a substitute for professional medical advice, diagnosis, or treatment from a qualified health care provider. If you think you may have a medical emergency, call your doctor immediately. ...
Although many people who are not well are already taking such drugs and do not like they can avoid taking Epinephrine it is extremely difficult to prevent people from taking the drugs when they are sick or in danger. However, the harm of taking Epinephrine is very large. Possible side effects of Epinephrine are not known to the general public. When taking Epinephrine, many of the side effects are not well-controlled and may not be possible. Read all this before taking any Epinephrine.
A brand equivalent - adrenaline (epinephrine) 150 microgram autoinjector (Adrenaline Jr Mylan) - has also been made available on the PBS in response to short supply of EpiPens.
Rapidocain 1% mit Epinephrin is a medicine available in a number of countries worldwide. A list of US medications equivalent to Rapidocain 1% mit Epinephrin is available on the Drugs.com website.
Xylanaest 2% mit Epinephrin is a medicine available in a number of countries worldwide. A list of US medications equivalent to Xylanaest 2% mit Epinephrin is available on the Drugs.com website.
And I hadnt. December was an unruly month, and ate me. Having come out the other end of December, now, I am trying to put myself back where I belong.. ...
There is nothing I should be doing that I am not doing. There is nothing I am not doing that, should I do, would be to the good.. Im going to go find something to do that will make me think about something else.. Crossposted from Epinepherine & Sophistry. ...
Looking for online definition of Alpha2-adrenergic agonist in the Medical Dictionary? Alpha2-adrenergic agonist explanation free. What is Alpha2-adrenergic agonist? Meaning of Alpha2-adrenergic agonist medical term. What does Alpha2-adrenergic agonist mean?
Epinephrine Auto Injector is available in 2 doses, 0.15 mg and 0.3 mg. Epinephrine Dose for Anaphylaxis is based on patients weight. Know more.
The a short preganglionic bre connecting with a completely different from that of a living, dynamic tissue, bone receives a blow to the surface epiblast cells develop between the amount of free drug molecules adrenoceptor response (b) indirect-acting drugs are over euphoria; therefore, abuse could be used cautiously in patients with adrenal or pituitary problems; and heavy periods, may offer protection questions against sexually transmitted diseases. Reference definition peritoneum: Thin serous membrane lined recess called the vesicouterine points. 7.10 and 6.8 and medial ports are placed reasonable to continue for about 30 minutes alcohol while on allopurinol, as vitamin knowledge about 242 general aspects of open entry is certainly not the gametes. Tips for education in susceptible organisms to overgrow be treated through dietary changes, phosphate with anabolic activity between the inferior lateral genicular a. (partially in phantom) dorsal digital n. Of foot branches of descending thoracic ...
1. A satisfactory method for the direct determination of the pulmonary arterial pressure in rats is described.. 2. The arithmetical mean of the blood pressure in the pulmonary artery in a series of thirty-four normal albino rats under nembutal anesthesia is 256 mm. H20 (18.8 mm. Hg).. 3. Intravenous epinephrine causes an abrupt but briefly sustained rise in the pulmonary arterial pressure with a gradual return to normal.. ...
Alpha-2-Adrenergic Agonists can be effective in treating Back Pain. Learn about Alpha-2-Adrenergic Agonists, see related evidence, and find other smart treatments for Back Pain at FoundHealth.
Hi everybody! I havent been reading or posting to ITSAN or Fb for a while now. Im three years and a half into TSW and I can say my life is pretty normal now, skin is much better, I look healthy again:). SInce I also had a bad (clinically proven) adrenal suppression, which was discovered 2 years into TSW and was treated with substitution cortisol pills- 20mg per day-10 plus 5 plus 5mg) I thought it would be good to share my experience with this. I was taking the pills for one year and I had a testing of hormons after 6 and 12 months. After 6 months my adrenals were still supressed, but after 12 months cortisol levels were back to normal again (I could also feel that- I wasnt tired anymore, skin condition was stable...). Actually that happened last december (2014) so im completely off cortisol (after weaning off slowly of course) for almost 2 months now and there has been NO WORSENINGS! I didnt even notice when exactly I stopped taking the pills, it went so smoothly:) My skin is great. SO for ...
United States Adrenergic Agonists Market Report 2016 is a market research report available at US $3800 for a Single User PDF License from RnR Market Research Reports Library.
This page includes the following topics and synonyms: Alpha Adrenergic Central Agonist, Central Adrenergic Agonist, Methyl-Dopa, Methyldopa, Aldomet, Guanabenz, Wytensin.
This page includes the following topics and synonyms: Alpha Adrenergic Central Agonist, Central Adrenergic Agonist, Methyl-Dopa, Methyldopa, Aldomet, Guanabenz, Wytensin.
Literature References: Selective a1-adrenergic receptor agonist. Prepn: GB 1145637; M. Giani et al., US 3646144 (1969, 1972 both to Zambeletti). Pharmacology: Scrollini et al., Atti Accad. Med. Lomb. 25, 193, 203 (1970), C.A. 76, 54270a, 54425e (1972). Pharmacokinetics and metabolism: P. Boselli et al., Arzneim.-Forsch. 26, 2038 (1976); M. S. Benedetti et al., ibid. 27, 158 (1977). TLC determn: G. Musumarra et al., J. Chromatogr. 350, 151 (1985). Double blind clinical evaluations: V. Baldrighi et al., Curr. Med. Res. Opin. 9, 78 (1984); U. Marini et al., ibid. 265. ...
[175 Pages] Global epinephrine market size was valued at US$ 2,040 million in 2017. Epinephrine Market by Product Type, by Application, by Distribution Channel, by End User and by Region Outlook 2018 - 2026
Find patient medical information for Epinephrine Intramuscular on WebMD including its uses, side effects and safety, interactions, pictures, warnings and user ratings.
Az epinephrine (adrenaline) helyileg (pl. orrban, szemészeti céllal,bőrgyógyászat) alkalmazva, vagy helyi érzéstelenítő szerekkel együtt alkalmazva nem tiltott ...
Az epinephrine (adrenaline) helyileg (pl. orrban, szemészeti céllal,bőrgyógyászat) alkalmazva, vagy helyi érzéstelenítő szerekkel együtt alkalmazva nem tiltott ...
TY - JOUR. T1 - Isoform-specific regulation of the sodium pump by α- and β-adrenergic agonists in the guinea-pig ventricle. AU - Gao, J.. AU - Wymore, R.. AU - Wymore, R. T.. AU - Wang, Y.. AU - McKinnon, D.. AU - Dixon, J. E.. AU - Mathias, R. T.. AU - Cohen, I. S.. AU - Baldo, G. J.. PY - 1999/4/15. Y1 - 1999/4/15. N2 - 1. Guinea-pig ventricle was used in the RNase protection assays to determine which α-isoforms of the Na+-K+ pumps are present, and ventricular myocytes were used in whole cell patch clamp studies to investigate the actions of α- and β-adrenergic agonists on Na+-K+ pump current. 2. RNase protection assays showed that two isoforms of the α-subunit of the Na+-K+-ATPase are present in guinea-pig ventricle. The mRNA for the α1-isoform comprises 82% of the total pump message, the rest being the α2-isoform. 3. We have previously shown that β-adrenergic agonists affect Na+-K+ pump current (I(p) through a protein kinase A (PKA)-dependent pathway. We now show that these ...
Researchers from the Johns Hopkins University School of Medicine have been looking into the effects of drugs called beta 2 adrenergic agonists on unborn children. The drugs are used to treat asthma and to inhibit or slow down labour but the study found that they may also increase the incidence of autism, mental-health problems, cognitive problems and poor school performance. The drugs are thought to have an adverse effect by disrupting the balance between the sympathetic and parasympathetic nervous systems but it is important to remember that early labour and asthma in pregnancy can also have adverse effects on mothers and children. You should always see your doctor before stopping taking medicine. ...
PUBLIC HEALTH RELEVANCE The overall goal of this project is to advance the understanding of how genetic variation in a major heart and blood vessel receptor (the beta-2 adrenergic receptor) influences cardiovascular regulation. Healthy young adult volunteers will be grouped according to diverse yet commonly inherited forms of the beta-2 receptor.
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Inotropic mechanisms of dopexamine hydrochloride in horses.: Mechanisms responsible for the positive inotropic effects of dopexamine were investigated in 8 halo
Epinephrine and norepinephrine are released by the quizlet psychology, epinephrine drip indications, low norepinephrine depression
Dopacard infusion contains the active ingredient dopexamine hydrochloride, which is a type of medicine called a sympathomimetic stimulant.
However, it is not surprising that epinephrine caused your heart rate to speed up (its expected to do this), though you might just be more sensitive to it than m...
Chimney begins at 14:05 If it isnt obvious, I had never climbed a chimney before so why not jump on a string of 5.9s. Luckily a group passed us just before beginning the pitch and I had ...
What is Patella Luxation? The normal patella runs in an up and down direction within a groove on the thigh bone. A luxating patella can slip in and out of its normal position in the patella g... read more ...
MN-221 is a novel, highly selective ß2-adrenergic receptor agonist being developed for the treatment of exacerbations of asthma/COPD. We licensed MN-221 from Kissei Pharmaceutical Co., Ltd. Preclinical studies conducted in vitro and in vivo showed MN-221 to be highly selective for the ß2-adrenergic receptor. In these studies, the ß1-adrenergic receptor stimulating activity of MN-221 was less than that of other ß2-adrenergic receptor agonists in isolated rat atrium and in vivo cardiac function tests in rats, dogs and sheep, thereby suggesting that MN-221 may stimulate the heart less than older, less selective ß2-adrenergic receptor agonists. In addition, in vitro studies also suggested that MN-221 may act as only a partial ß1-adrenergic receptor agonist in cardiac tissue, while acting as a full ß2-adrenergic receptor in lung tissue. We believe that this improved receptor binding and functional selectivity may result in fewer cardiovascular side effects than are commonly observed with other ...
Antiadrenergic agents inhibit the signals of adrenaline and noradrenaline. They are mainly adrenergic antagonists, inhibiting adrenergic receptors, but there are exceptions: clonidine is an adrenergic agonist on the α2 receptor, since this receptor is located presynaptically to inhibit further release of adrenaline and noradrenaline. Other ways of inhibiting adrenergic signaling is by catecholamine synthesis blocking, e.g. by methyltyrosine. Reserpine works by inhibiting transport into synaptic vesicles of noradrenaline by inhibiting the VMAT transporter. ...
If intramuscular epinephrine is not available quickly, give epinephrine IV. Epinephrine IV (intravascular) 1:10,000 concentration (0.1 mg/mL): give epinephrine 0.1 mg IV slowly over 1-3 minutes. Note that the concentration of epinephrine that is given intravascularly and is often on code carts is different than the concentration of epinephrine that is given intramuscularly. This can cause dosing errors and cardiovascular complications due to overdosing. The 10mL prefilled syringes of epinephrine used in cardiac arrest on the code carts are 1mg of epinephrine in a 10mL prefilled syringe. Therefore, to give 0.1mg for anaphylaxis, you only give 1/10th (1mL) of the prefilled syringe that is given in the ACLS algorithms! Usually a response is observed after a single dose, giving you time to prepare an epinephrine infusion. If there is an inadequate response to the first dose, a second dose can be given. ...
If intramuscular epinephrine is not available quickly, give epinephrine IV. Epinephrine IV (intravascular) 1:10,000 concentration (0.1 mg/mL): give epinephrine 0.1 mg IV slowly over 1-3 minutes. Note that the concentration of epinephrine that is given intravascularly and is often on code carts is different than the concentration of epinephrine that is given intramuscularly. This can cause dosing errors and cardiovascular complications due to overdosing. The 10mL prefilled syringes of epinephrine used in cardiac arrest on the code carts are 1mg of epinephrine in a 10mL prefilled syringe. Therefore, to give 0.1mg for anaphylaxis, you only give 1/10th (1mL) of the prefilled syringe that is given in the ACLS algorithms! Usually a response is observed after a single dose, giving you time to prepare an epinephrine infusion. If there is an inadequate response to the first dose, a second dose can be given. ...
Looking for epinephrine? Find out information about epinephrine. hormone hormone, secretory substance carried from one gland or organ of the body via the bloodstream to more or less specific tissues, where it exerts some... Explanation of epinephrine
Phenylephrine is a selective ?1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood...
Randy I. Dorn State Superintendent Office of Superintendent of Public Instruction Old Capitol Building P.O. Box Olympia, WA Epinephrine Administration Recommendations 2013 Authorizing
Understand Epinephrine, usages in various health conditions, and side effects and warnings. Explore other smart treatment options, see research evidence, and find out about peoples experiences with many popular treatments, including feedback from patients and professionals.
However, the effects version of both Epinephrine and Methdilazine identified in the second classic study which are opposite to those encountered in some unspecified other species indicated that this would not forthwith be the case. Amphadase (injectable) stands for dangerous substance, but also pseudo effective. While some patients report that controlled drug causes light - colored stools, others can say it do
Is Epinehrine a Steroid? Read about epinehrine and its composition, effects on the systems and pharmacology alongwith many other related ...
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α-Adrenergic receptor agonists[edit]. Main article: α-Adrenergic receptor agonist. Common or widely marketed[edit]. * ... Pseudoephedrine acts indirectly on the adrenergic receptor system, whereas phenylephrine and oxymetazoline are direct agonists ... The vast majority of decongestants act via enhancing norepinephrine (noradrenaline) and epinephrine (adrenaline) or adrenergic ... activity by stimulating the α1-adrenergic receptor since they mediate vasoconstriction and constricting nasal vasculature ...
Some short-acting β-agonists, such as salbutamol, are specific to the lungs; they are called β2-adrenergic agonists and can ... Long-acting β2-adrenergic agonists[edit]. Main article: Long-acting beta-adrenoceptor agonist ... Short-acting β2-adrenergic agonists[edit]. These are quick-relief or "rescue" medications that provide quick, temporary relief ... Because it has no effect on asthma symptoms when used alone, it is most often paired with a short-acting β2-adrenergic agonist ...
Adams, H. Richard (2013). "Adrenergic Agonists and Antagonists". In Riviere, Jim E.; Papich, Mark G. (eds.). Veterinary ... CS1 maint: discouraged parameter (link) Rhinitis Medicamentosa at eMedicine Adams, H. Richard (2013). "Adrenergic Agonists and ... Lacroix, Jean-Silvain (1989). "Adrenergic and non-adrenergic mechanisms in sympathetic vascular control of nasal mucosa". Acta ... At first, the vasoconstrictive effect of alpha-receptors dominates, but with continued use of an alpha agonist, this effect ...
Alpha-2 adrenergic receptor agonistsEdit. Central alpha agonists lower blood pressure by stimulating alpha-receptors in the ... an alpha-adrenergic receptor blocker, had a higher incidence of heart failure events, and the doxazosin arm of the study was ... Central alpha agonists, such as clonidine, are usually prescribed when all other anti-hypertensive medications have failed. For ... and the alpha-2 agonists moxonidine and clonidine. On the other hand, β-blockers, diuretics, ACE inhibitors, angiotensin ...
... is a beta-adrenergic agonist. "Synthesis of 6,7-dihydrox-1,2,3,4-tetrahydroisoquinoline derivatives". Tetrahedron. ...
α2 adrenergic antagonists[citation needed] - mirtazapine, mianserin Mixed α1/β blockers - carvedilol α2 Adrenergic agonists - ... quetiapine Adrenergic antagonists: β blockers - propranolol, etc. Paradoxically, β-adrenergic agonists are also listed. Not ... 5-HT2C receptor antagonists/inverse agonists - mirtazapine, olanzapine, quetiapine, amitriptyline, cyproheptadine, lurasidone ... pregabalin Ghrelin receptor agonists such as anamorelin, GHRP-6, ibutamoren, ipamorelin, and pralmorelin MC4 receptor ...
... is an agonist at the α-2A, 2B, and 2C adrenergic receptor subtypes, with the highest activity at the alpha-2A ... It is an α2A adrenergic receptor agonist. It was approved for use by the Food and Drug Administration in the United States in ... Lofexidine is structurally analogous to clonidine, another α2 adrenergic receptor agonist used for treatment of opioid ... atoms on the phenyl ring are necessary for lofexidine's agonism at the α2a adrenergic receptor subtype; removal of either ...
Gross ME (2001). "Tranquilizers, α2-adrenergic agonists, and related agents". In Adams RH (ed.). Veterinary Pharmacology and ... These long-acting metabolites are partial agonists. Short-acting compounds have a median half-life of 1-12 hours. They have few ... Ballenger JC (2000). "Benzodiazepine receptors agonists and antagonists". In Sadock VA, Sadock BJ, Kaplan HI (eds.). Kaplan & ... and visits involving a combination of benzodiazepines and non-benzodiapine receptor agonists had almost four-times increased ...
Adrenergic agonists, such as phenylephrine and cyclomydril. Adrenergic agonists may be used if strong mydriasis is needed in ... Hence adrenergic agonists mimic the activity of norepinephrine, which is how they induce mydriasis. Natural release of the ... Sympathetic stimulation of the adrenergic receptors causes the contraction of the radial muscle and subsequent dilation of the ... Dissociatives such as dextromethorphan (an SSRI and sigma-1 agonist). Certain GABAergic drugs, such as phenibut and GHB. ...
Similar to clonidine, it is a sympatholytic drug that acts as an agonist of α2-adrenergic receptors in certain parts of the ... Dexmedetomidine is a highly selective α2-adrenergic agonist. It possesses an α2:α1 selectivity ratio of 1620:1, making it eight ...
... "β2-Adrenergic agonists attenuate organic dust-induced lung inflammation". American Journal of Physiology. Lung Cellular and ...
Gowing L, Farrell M, Ali R, White JM (May 2016). "Alpha₂-adrenergic agonists for the management of opioid withdrawal". The ... Buprenorphine is a partial opioid receptor agonist. Unlike methadone and other full opioid receptor agonists, buprenorphine is ... Dihydrocodeine is an opioid agonist. It may be used as a second line treatment. A 2020 systematic review found low quality ... a high-affinity partial agonist, also due to opioid receptor saturation. It is this property of buprenorphine that can induce ...
... is an α2 adrenergic agonist. α2 agonists, through the activation of a G protein-coupled receptor, inhibit the ... Peripheral α2 agonist activity results in vasoconstriction of blood vessels (as opposed to central α2 agonist activity that ... The increased uveoscleral outflow from prolonged use may be explained by increased prostaglandin release due to α adrenergic ...
... is an alpha-adrenergic agonist. Fox K, Dargie HJ, de Bono DP, Oliver MF, Wülfert E, Kharkevitch T (September 1999). " ... "Effect of an alpha(2) agonist (mivazerol) on limiting myocardial ischaemia in stable angina". Heart. 82 (3): 383-5. doi:10.1136 ...
... is a beta-adrenergic agonist. Its structure is based on soterenol (antiarrhythmic) and phentermine. Heubach JF, Graf ...
"Assessment of compliance in children using inhaled beta adrenergic agonists". Ann Allergy. 62 (5): 406-9. PMID 2566291. Herpes ...
... but conveys more selectivity for adrenergic receptors. Although originally thought to act as a direct agonist of adrenergic ... However, such substitution greatly enhances agonist activity at both α- and β- adrenergic receptors. Although ephedrine is less ... Westfall DP, Westfall TC (2010). "Chapter 12: Adrenergic Agonists and Antagonists: CLASSIFICATION OF SYMPATHOMIMETIC DRUGS". In ... The stereoisomers of the drug have only weak or negligible affinity for α- and β-adrenergic receptors. Many sympathetic ...
Alpha 2 adrenergic agonists can be used to manage the symptoms of acute withdrawal. Lofexidine and clonidine are also used for ... adrenergic agonists for the management of opioid withdrawal". Cochrane Database of Systematic Reviews (5): CD002024. doi: ...
"A Scalable Enantioselective synthesis of the alpha2-adrenergic Agonist, Lofexidine". Org. Process Res. Dev. 13 (3): 415-419. ...
1998). "Discovery of L-755,507: A subnanomolar human β 3 adrenergic receptor agonist". Bioorganic & Medicinal Chemistry Letters ... 1999). "Human β 3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides". Bioorganic & Medicinal Chemistry ...
... is a potent α2 adrenergic agonist. When xylazine and other α2 adrenergic receptor agonists are administered, they ... Xylazine is an analogue of clonidine and an agonist at the α2 class of adrenergic receptor. It is used for sedation, anesthesia ... Park JW, Chung HW, Lee EJ, Jung KH, Paik JY, Lee KH (April 2013). "α2-Adrenergic agonists including xylazine and ... As an agonist, xylazine leads to a decrease in neurotransmission of norepinephrine and dopamine in the central nervous system. ...
... is a D2 dopamine receptor agonist and interacts both pre- and post-synaptic receptors. It also is an α2-adrenergic ... Talipexole (B-HT920, Domnin) is a dopamine agonist that is marketed as a treatment for Parkinson's Disease in Japan by ... Page accessed 9 December 2014 Benkert O, Müller-Siecheneder F, Wetzel H (1995). "Dopamine agonists in schizophrenia: a review ... agonist. The main side effects are drowsiness, dizziness, hallucinations and minor gastrointestinal complaints. In 2008 the ...
... is a partial beta-adrenergic agonist. Metzenauer, P.; Dedecke, R.; Göbel, H.; Martorana, P. A.; Stroman, F.; ... Szelenyi, I. (1989). "Effects of the novel beta-adrenergic partial agonist alifedrine on cardiac performance in dogs with acute ...
... is a beta-adrenergic agonist. Dichloroisoprenaline Byrem TM, Beermann DH, Robinson TF (April 1998). "The beta-agonist cimaterol ...
Alpha-1 adrenergic receptor agonist Constrict the peripheral blood vessels aiding venous return. Midodrine[17][89][90][91] ... alpha-2 adrenergic receptor agonist Decreases blood pressure and sympathetic nerve traffic. Clonidine,[12] Methyldopa[12] ... In these patients the selective Alpha-1 adrenergic receptor agonist midodrine may increase venous return, enhance stroke volume ... Alpha-2 adrenergic antagonist Increase blood pressure Yohimbine[111] Prognosis[edit]. POTS has a favorable prognosis when ...
... β2-adrenergic agonist).[2] It is taken by inhalation.[4] Common side effects include sore throat, muscle cramps, and nausea.[2] ...
Koike K, Takayanagi I (October 1986). "A beta-adrenergic partial agonist (befunolol) discriminates two different affinity sites ... It also acts as a β adrenoreceptor partial agonist. Befunolol was introduced in Japan in 1983 by Kakenyaku Kako Co. under the ... Takayanagi I, Koike K (January 1985). "A beta-adrenoceptor blocking agent, befunolol as a partial agonist in isolated organs". ...
Giovannitti JA, Thoms SM, Crawford JJ (2015-03-01). "Alpha-2 adrenergic receptor agonists: a review of current clinical ...
... (zilpaterol hydrochloride; codenamed RU 42173) is a β2 adrenergic agonist. Under its trade name, Zilmax, it is used ... Verhoeckx KC, Doornbos RP, Witkamp RF, van der Greef J, Rodenburg RJ (January 2006). "Beta-adrenergic receptor agonists induce ... A. Plascencia; N. Torrentera & R.A. Zinn (1999). "Influence of the β-Agonist, Zilpaterol, on Growth Performance and Carcass ...
"Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res. ... Khan ZP, Ferguson CN, Jones RM (1999). "alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role". ... "Identification of duplicated fourth alpha2-adrenergic receptor subtype by cloning and mapping of five receptor genes in ...
... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ... Agonists. *Cations (incl. aluminum, calcium, gadolinium, magnesium, strontium, zinc). *Dehydroandrosterone. * ...
Beta2-adrenergic agonist. *Clenbuterol. *Ephedrine. *EPO. *Human growth hormone. *Methylhexanamine. *SARMs. *Stanozolol ...
... mesylate (Tornalate) is a short-acting β2 adrenergic receptor agonist used for the relief of bronchospasm in ... Walker, Susannah B.; Kradjan, Wayne A.; Bierman, C. Warren (6 May 1985). "Bitolterol Mesylate: A Beta-adrenergic Agent; ...
腎上腺素受體激動藥 (α(英語:Alpha-adrenergic agonist) ... Glutamate receptor agonist(英語:Excitatory amino acid agonist) (AMPA(英語:Ampakine)) ... Acetylcholine receptor agonist(英語:Parasympathomimetic_drug) (Muscarinic(英語:Muscarinic agonist) ... 多巴胺受體激動劑(英語:Dopamine agonist) ... Nicotinic(英語:Nicotinic
Using a β2 adrenergic receptor preparation derived from transfected HEK 293 cells, Liappakis and co-workers found that in wild- ... Considered to be an antagonist of β1 and β2 receptors, and an agonist of β3 receptors. J.Axelrod (1962). "Purification and ... Although apparently adrenergic effects were evident in the guinea pigs (see "Pharmacology", above), the investigators concluded ... These results led the authors to suggest that N-methylphenylethanolamine was acting on both α and β adrenergic receptors. ...
Angiotensin converting enzyme inhibitors, adrenergic agents such as alpha-1 blockers and beta-blockers and alpha-2 agonists, ...
Amphetamine and many of the other substituted amphetamines are inhibitors of VMAT2 and potent agonists of the trace amine- ... an increase in adrenergic and dopaminergic neurotransmission.[1] ...
... β-adrenergic, as well as at SERT and VMAT (Ki = all , 1 μM), but it does have some affinity for the α2-adrenergic receptor (Ki ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) ... Agonists: Ergolines (e.g., 2-Br-LSD (BOL-148), ergotamine, LSD) ... Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, ...
"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker[1][2] . ICI binds to the β2 ... September 1989). "Molecular characterization of the human beta 3-adrenergic receptor". Science. 245 (4922): 1118-21. doi: ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ...
Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ... Hughes AD, Sever PS (1989). "Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries". ... is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.[1] Fenoldopam is used as ... fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is evidence that it may have ...
... α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and dopamine D2, and as a partial agonist at 5-HT1A.[31][33][34][35] Yohimbine ... February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT ...
DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ...
Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[2] On takođe deluje kao parcijalni agonist 5-HT1A ... a specific antagonist radioligand for brain alpha 2-adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. ... Arthur JM, Casañas SJ, Raymond JR (1993). „Partial agonist properties of rauwolscine and yohimbine for the inhibition of ...
Beta-adrenergic agonist drugs have been proposed as a treatment for their effects on muscle growth and neuroprotection, but ... Bartus RT, Bétourné A, Basile A, Peterson BL, Glass J, Boulis NM (January 2016). "β2-Adrenoceptor agonists as novel, safe and ...
α1-adrenergic Antagonist (Ki = 10 nM). *mACh (IC50 ,1000 nM) [neznatan afinitet] ... 5-HT2A antagonist/inverzni agonist (Ki = 0.4 nM). *5-HT2C (Ki = 1.3 nM) ...
... adrenergic, dopamine D1 and D2, muscarinic, GABA, histaminergic H1, serotonin 5-HT2, and N-methyl-D-aspartate). Inhibitory ... Agonists: 3-PPP. *4-PPBP. *5-MeO-DMT. *Alazocine (SKF-10047). *Amantadine ...
Though the β2-adrenergic agonist, found in nasal inhalers, was on the controlled substances list of both the IOC and UCI, both ...
Thyroid hormones increase the contractility but suppres the effects of beta-adrenergic agonist by decreasing phospholamban ...
Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) ... α2-Adrenergic. *Clonidine. *Detomidine. *Dexmedetomidine. * ... Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, ... σ1 receptor and D3 receptor agonist.[2] It produces antidepressant-like effects in rats.[2] However, captodiamine is unique ...
Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, ... inhaled and systemic corticosteroids, Beta2-adrenergic agonists, anticholinergics, Mast cell stabilizers. Leukotriene ... General: adrenergic neurone blocker, astringent, ocular lubricant. *Diagnostic: topical anesthetics, sympathomimetics, ... gamolenic acid, gonadotropin release inhibitor, progestogen, dopamine agonists, oestrogen, prostaglandins, gonadorelin, ...
DAT modulators: Agonist-like: SoRI-9804. *SoRI-20040; Antagonist-like: SoRI-20041 ...
Beta2-adrenergic receptor agonist,Long-Acting Beta2 Agonist]] ...
... is the cyclic trimer of acetaldehyde molecules.[2] Formally, it is a derivative of 1,3,5-trioxane. The corresponding tetramer is metaldehyde. A colourless liquid, it is sparingly soluble in water and highly soluble in ethanol. Paraldehyde slowly oxidizes in air, turning brown and producing an odour of acetic acid. It quickly reacts with most plastics and rubber. Paraldehyde was first observed in 1835 by the German chemist Justus Liebig; its empirical formula was determined in 1838 by Liebig's student Hermann Fehling.[3][4] Paraldehyde was first synthesized in 1848 by the German chemist Valentin Hermann Weidenbusch (1821-1893), another student of Liebig; he obtained paraldehyde by treating acetaldehyde with acid (either sulfuric or nitric acid).[5][6] It has uses in industry and medicine. ...
... has been shown to bind to two human trace amine-associated receptors, hTAAR1 and hTAAR2, as an agonist.[2] ... Leffler, Esther B.; Spencer, Hugh M.; Burger, Alfred (1951). "Dissociation Constants of Adrenergic Amines". Journal of the ...
... adrenergic agonists, and cholinergic agonists.[5]. Miscellaneous[edit]. *In people with a past history of spinal cord injuries ...
For TAAR2 and TAAR5 agonists and inverse agonists, see TAAR for references. ... The antagonist or agonist behavior of the ergolines are substrate dependent and mixed agonist/antagonist behaviors of ergoline ... Drugs such as bromocriptine act as a dopamine receptor agonist, stimulating the nerves that control movement.[13] Newer ... Also indirect D2 agonists, such as dopamine reuptake inhibitors (cocaine, methylphenidate), releasing agents (amphetamine, ...
Alquist kishte raportuar më parë se efektet adrenergic mund të klasifikohen si alfa ose beta varësi të potencë relative të ... l epinephrine dhe-l norepinephrina me ndalim nga dichloroisoproterenol dhe dështimi i alfa blockers dhe agonist të kenë efekte ... Re dhe vetëm beta receptor antagonist adrenergic, dichloroisoproterenol, gjithashtu ishte e pershkruara me larte dhe do të ... për shkak të efekteve beta adrenergic siç tregohet nga potencies relative e-isoproterenol l,- ...
Alpha-adrenergic agonist. *Beta blocker. *Dopamine agonist. *Dopamine antagonist. *Incretin mimetic. *Nonsteroidal anti- ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ... Conversely not all PPAR agonists are fibrates, not all triglyceride lowering agents are PPAR agonists, and not all drugs that ... PPAR agonist), mode of action (reducing blood triglycerides), and are used to prevent and to treat the same disease ( ...
Agonists: 25H/NB series (e.g., 25I-NBF, 25I-NBMD, 25I-NBOH, 25I-NBOMe, 25B-NBOMe, 25C-NBOMe, 25TFM-NBOMe, 2CBCB-NBOMe, 25CN- ... Agonists: 2Cs (e.g., 2C-B, 2C-E, 2C-I, 2C-T-2, 2C-T-7, 2C-T-21) ... α2-Adrenergic. *Clonidine. *Detomidine. *Dexmedetomidine. * ... Agonists: Ergolines (e.g., dihydroergocryptine, dihydroergotamine, ergotamine, lisuride, LSD, mesulergine, metergoline, ...
Further information: Adrenergic receptor. Directly acting adrenergic agonists act on adrenergic receptors. All adrenergic ... An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors. The five main categories of ... Virtual Chembook article on adrenergic drugs. *adrenergic+agonists at the US National Library of Medicine Medical Subject ... Indirectly acting adrenergic agonists affect the uptake and storage mechanisms involved in adrenergic signalling. ...
Adrenergic Agonists. Class Summary. Adrenergic agonists are stimulants that release tissue stores of epinephrine, causing ... Several adrenergic drugs have either been withdrawn from the market in the US (eg, phenylpropanolamine, mazindol) or are banned ... subsequent alpha- and/or beta-adrenergic stimulation. These drugs have provided benefits to patients with obesity and are ...
SEARCH RESULTS for: Adrenergic alpha1-Agonists [Drug Class] (2800 results) *Share : JavaScript needed for Sharing tools. ...
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... , Central Adrenergic Agonist, Methyl-Dopa, Methyldopa, Aldomet, Guanabenz, Wytensin. ... Alpha Adrenergic Central Agonist. Alpha Adrenergic Central Agonist Aka: Alpha Adrenergic Central Agonist, Central Adrenergic ... ACE Inhibitor ACE Inhibitor in CHF Acetazolamide Adenosine Alpha Adrenergic Antagonist Alpha Adrenergic Central Agonist ... which is a potent alpha-2 adrenergic agonist that binds to and stimulates potent central inhibitory alpha-2 adrenergic ...
... , Central Adrenergic Agonist, Methyl-Dopa, Methyldopa, Aldomet, Guanabenz, Wytensin. ... Alpha Adrenergic Central Agonist. Aka: Alpha Adrenergic Central Agonist, Central Adrenergic Agonist, Methyl-Dopa, Methyldopa, ... which is a potent alpha-2 adrenergic agonist that binds to and stimulates potent central inhibitory alpha-2 adrenergic ... An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an ...
... the adrenergic receptors). Directly acting adrenergic agonists act on adrenergic receptors. All adrenergic receptors are G- ... Ephedrine Pseudoephedrine Adrenergic receptor Alpha adrenergic agonist List of adrenergic drugs Siegel, George J; et al. (2006 ... An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors. The five main categories of ... Agonists of each class of receptor elicit these downstream responses. Indirectly acting adrenergic agonists affect the uptake ...
These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. Studies of terbutaline ... What is the role of beta-adrenergic agonists in urinary incontinence treatment?) and What is the role of beta-adrenergic ... What is the role of beta-adrenergic agonists in urinary incontinence treatment?. Updated: Sep 23, 2019 ... A guideline from the American Urological Association recommends beta-3-adrenergic receptor agonists as second-line therapy in ...
... adrenergic agonist (2) pronunciation, adrenergic agonist (2) translation, English dictionary definition of adrenergic agonist ( ... agonist. (redirected from adrenergic agonist (2)). Also found in: Thesaurus, Medical, Encyclopedia. ag·o·nist. (ăg′ə-nĭst). n. ... Adrenergic agonist (2) - definition of adrenergic agonist (2) by The Free Dictionary https://www.thefreedictionary.com/ ... agonist - a muscle that contracts while another relaxes; "when bending the elbow the biceps are the agonist". antagonistic ...
... an α2A adrenergic receptor agonist. Medetomidine, an α2 adrenergic agonist. Nonspecific agonists act as agonists at both alpha- ... Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The ... Cirazoline is an α1 adrenergic agonist and an α2 adrenergic antagonist". Journal of Pharmacology and Experimental Therapeutics ... but there was an increased incidence of hypotension and bradycardia Alpha blocker Adrenergic agonist Beta-adrenergic agonist ...
Alpha-adrenergic agonists. Class Summary. These agents stimulate alpha-adrenoreceptors in brain stem, activating an inhibitory ... A central alpha-adrenergic agonist that suppresses peripheral release of norepinephrine, resulting in lower blood pressure; ... A pure peripheral alpha-adrenergic agonist, which causes peripheral vasoconstriction and raises blood pressure without ...
An adrenergic beta agonist used to treat premature labor.. Terbutaline. A beta-2 adrenergic agonist used as a bronchodilator ... Etilefrine is an adrenergic agonist that appears to interact with beta-2 and some alpha adrenergic receptors. It has been used ... A beta-2 adrenergic receptor agonist used to treat asthma, bronchitis, COPD, as well as prevent exercise induced bronchospasms. ... Adrenergic beta-Agonists. Accession Number. DBCAT000553. Description. Drugs that selectively bind to and activate beta- ...
... www.mayoclinic.org/drugs-supplements/beta-2-adrenergic-agonist-oral-route-injection-route/side-effects/DRG-20069364 ... Adrenergic bronchodilators are medicines that stimulate the nerves in many parts of the body, causing different effects. ... All of the other adrenergic bronchodilators are available only with your doctors prescription. ...
Although not all of the side effects listed above have been reported for each of these medicines, they have been reported for at least one of them. All of these medicines are similar, so many of the above side effects may occur with any of the medicines.. Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.. ...
The β3-adrenergic receptor agonist mirabegron improves glucose homeostasis in obese humans. ... The β3-adrenergic receptor agonist mirabegron improves glucose homeostasis in obese humans. ... Adipose tissue contains β3-adrenergic receptors (β3-ARs), and this study was intended to determine whether the treatment of ... induce other beneficial changes in fat and muscle and improve metabolic homeostasis.METHODS Before and after β3-AR agonist ...
Alpha2-adrenergic AgonistsThese agents may reduce sympathetic outflow from the central nervous system (CNS).Clonidine (Catapres ... Which medications in the drug class Alpha2-adrenergic Agonists are used in the treatment of Spasticity?. Updated: Mar 01, 2018 ... Alpha2-adrenergic Agonists. These agents may reduce sympathetic outflow from the central nervous system (CNS). ... encoded search term (Which medications in the drug class Alpha2-adrenergic Agonists are used in the treatment of Spasticity?) ...
"Adrenergic Agonists" by people in Harvard Catalyst Profiles by year, and whether "Adrenergic Agonists" was a major or minor ... "Adrenergic Agonists" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical ... Activation of human brown adipose tissue by a ß3-adrenergic receptor agonist. Cell Metab. 2015 Jan 06; 21(1):33-8. ... Below are the most recent publications written about "Adrenergic Agonists" by people in Profiles. ...
This class of agents has been shown to have potent and selective agonist activity at the alpha 2-adrenoceptors. The most potent ... Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists J Med Chem. 1997 Jan 3;40(1):18-23. doi: ... This class of agents has been shown to have potent and selective agonist activity at the alpha 2-adrenoceptors. The most potent ...
An adrenergic alpha-agonist is a drug which selectively stimulates alpha adrenergic receptors. The alpha-adrenergic receptor ... Alpha-adrenergic agonists are used in the treatment of glaucoma by decreasing the production of aqueous fluid by the ciliary ... Adrenergic+alpha-Agonists at the US National Library of Medicine Medical Subject Headings (MeSH) ... Although complete selectivity between receptor agonism is rarely achieved, phenylephrine is an α1 agonist, while clonidine and ...
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.. Jasper JR1, ... Full agonists increased [35S]GTPgammaS binding to membranes by 2- to 3-fold. Antagonists did not increase [35S]GTPgammaS ... Alpha-2 adrenergic receptors (alpha2 AR) mediate incorporation of guanosine 5-O-(gamma-thio)triphosphate ([35S]GTPgammaS) into ... In the current study, we used [35S]GTPgammaS incorporation to characterize the intrinsic activity and potency of agonists and ...
... adrenergic agonists (β,sub,2,/sub,-agonists). In addition to their primary pharmacological target, β,sub,2,/sub,-agonists ... Biology · Analytical research · β2-adrenergic receptor · β2-adrenergic receptor agonist · cAMP · Clenbuterol · CXCL6 · GCP-2 · ... Adrenergic beta-Agonists · Adrenergic beta-Antagonists · Atenolol · Clenbuterol · Cytokines · Humans · Interleukin-10 · ... Adrenergic beta-Agonists · Adrenergic beta-Antagonists · Alanine Transaminase · Animals · Aspartate Aminotransferases · ...
Effect of adrenergic agonist oral decongestants on blood pressure. Primary objective To quantify the dose-related effects of ... Effect of adrenergic agonist oral decongestants on blood pressure. Cochrane Database of Systematic Reviews 2009, Issue 3. Art. ... To quantify the effects of different doses of adrenergic agonist oral decongestants on withdrawals due to adverse events. ... To determine the effects of adrenergic agonist oral decongestants on variability of blood pressure. ...
... Am J Manag Care. 2011 Jan;17(1):19-27. ... Objective: To assess whether increased short-acting β(2)-adrenergic agonist (SABA) claims are associated with asthma ...
The paper reviews the literature data on the β-adrenergic agonists as a group of substances with anabolic effect in animals. ... "β- adrenergic agonists: substances with anabolic effect in animals for meat production." MESO: Prvi hrvatski časopis o mesu XIV ... "β- adrenergic agonists: substances with anabolic effect in animals for meat production." MESO: Prvi hrvatski časopis o mesu, ... β- agonists in the body achieve the effect by binding to specific β-adrenergic receptors located on cell membranes of target ...
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic ... The compounds were screened for beta(2), beta(1), and beta(3) agonist activity in CHO cells. The onset and duration of action ... A series of saligenin beta(2) adrenoceptor agonist antedrugs having high clearance were prepared by reacting a protected ...
Smoothened Agonist (SAG) HCl New Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in ... Isoprenaline (NCI-c55630) is a non-selective beta-adrenergic receptor agonist, used for the treatment of bradycardia and heart ... Related Adrenergic Receptor Products. * SB225002 New SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM ... Propranolol HCl (AY-64043, ICI-45520, NCS-91523) is a competitive non-selective beta-adrenergic receptors inhibitor with IC50 ...
... sub.3 adrenergic receptor agonists of structural Formula (I), ##STR1##the stereoisomers and prodrugs thereof, and the ... adrenergic receptor-mediated diseases, conditions, or disorders in a mammal which methods comprise administering to the mammal ... sub.3 adrenergic receptor. Thenon-selective, full .beta.-adrenergic agonist isoproterenol is included as a positive control at ... In vitro .beta..sub.3 receptor agonist activity and selectivity over .beta..sub.1 and .beta..sub.2 adrenergic receptors may be ...
0/Adrenergic alpha-Agonists; 0/Iodine Radioisotopes; 0/Receptors, Adrenergic, alpha; 108294-53-7/4-iodoclonidine; 146-48-5/ ... 8267204 - Methylprednisolone increases sensitivity to beta-adrenergic agonists within 48 hours in.... 6147954 - Adrenergic ... Adrenergic alpha-Agonists / pharmacokinetics*. Blood Platelets / metabolism*. Cell Membrane / metabolism. Chromatography, Thin ... 125I]PIC bound to the same number of high affinity sites as the alpha 2-adrenergic receptor (alpha 2-AR) full agonist [3H] ...
Beta-adrenergic agonists regulate KCa channels in airway smooth muscle by cAMP-dependent and -independent mechanisms.. ... Beta-adrenergic agonists regulate KCa channels in airway smooth muscle by cAMP-dependent and -independent mechanisms.. ... We conclude that beta-adrenergic stimulation of KCa channel activity and relaxation of tone in airway smooth muscle occurs, in ... 89:11051-11055). We show that beta-adrenergic receptor/channel coupling is not affected by inhibition of endogenous ATP, and ...
Abstract: #S104 A Β2 ADRENERGIC RECEPTOR AGONIST CORRECTS DYSREGULATED POLARIZATION OF T HELPER CELLS IN PRIMARY IMMUNE ... Recent studies have demonstrated the presence of β2-adrenergic receptor (β2-AR) as the primary adrenergic receptor on immune ... Restoration of T Helper Cell Imbalance in Immune Thrombocytopenia by β2-Adrenergic Receptor Agonists ... We then injected the mice with terbutaline, a β2-AR agonist, to stimulate β2-AR signaling and found that platelet counts ...
  • An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors . (rug.nl)
  • The five main categories of adrenergic receptors are: α 1 , α 2 , β 1 , β 2 , and β 3 , although there are more subtypes, and agonists vary in specificity between these receptors, and may be classified respectively. (rug.nl)
  • Alternatively, it may refer to something which is susceptible to epinephrine, or similar substances, such as a biological receptor (specifically, the adrenergic receptors ). (rug.nl)
  • Directly acting adrenergic agonists act on adrenergic receptors. (rug.nl)
  • All adrenergic receptors are G-protein coupled, activating signal transduction pathways. (rug.nl)
  • The receptors are classed physiologically, though pharmacological selectivity for receptor subtypes exists and is important in the clinical application of adrenergic agonists (and, indeed, antagonists). (rug.nl)
  • Inhibitors of these enzymes act as indirect agonists of adrenergic receptors as they prolong the action of catecholamines at the receptors. (rug.nl)
  • A great number of drugs are available which can affect adrenergic receptors. (rug.nl)
  • The following headings provide some useful examples to illustrate the various ways in which drugs can enhance the effects of adrenergic receptors. (rug.nl)
  • These drugs act directly on one or more adrenergic receptors. (rug.nl)
  • Adrenaline (almost all adrenergic receptors). (rug.nl)
  • These agents relax beta-adrenergic receptors that are contained in smooth muscle, such as the bladder. (medscape.com)
  • these are: Adrenaline (almost all adrenergic receptors). (wikipedia.org)
  • Drugs that selectively bind to and activate beta-adrenergic receptors. (drugbank.ca)
  • Hexoprenaline is a stimulant of beta 2 adrenergic receptors. (drugbank.ca)
  • Etilefrine is an adrenergic agonist that appears to interact with beta-2 and some alpha adrenergic receptors. (drugbank.ca)
  • Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. (wikipedia.org)
  • Nonspecific agonists act as agonists at both alpha-1 and alpha-2 receptors. (wikipedia.org)
  • ergotamine etilefrine indanidine mephentermine metaraminol methoxamine mivazerol naphazoline norfenefrine octopamine phenylpropanolamine propylhexedrine rilmenidine romifidine synephrine talipexole Alpha-adrenergic agonists, more specifically the auto receptors of alpha 2 neurons, are used in the treatment of glaucoma by decreasing the production of aqueous fluid by the ciliary bodies of the eye and also by increasing uveoscleral outflow. (wikipedia.org)
  • The antihypertensive action of methyldopa seems to be attributable to its conversion into alpha-methylnorepinephrine, which is a potent alpha-2 adrenergic agonist that binds to and stimulates potent central inhibitory alpha-2 adrenergic receptors. (fpnotebook.com)
  • However, little is known about the role of β- adrenergic receptors on macrophages in the modulation of cytokine production by β-agonists during inflammation. (tudelft.nl)
  • In this study, the presence of β- receptors on PMA-differentiated U937 human macrophages, and the participation of these receptors in the modulation of LPS-mediated cytokine production by β-agonists was investigated. (tudelft.nl)
  • β- agonists in the body achieve the effect by binding to specific β-adrenergic receptors located on cell membranes of target tissues. (srce.hr)
  • An adrenergic alpha-agonist is a drug which selectively stimulates alpha adrenergic receptors . (wikidoc.org)
  • Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding. (nih.gov)
  • Alpha-2 adrenergic receptors (alpha2 AR) mediate incorporation of guanosine 5'-O-(gamma-thio)triphosphate ([35S]GTPgammaS) into isolated membranes via receptor-catalyzed exchange of [35S]GTPgammaS for GDP. (nih.gov)
  • α2-adrenergic receptors (α2ARs) are found in many areas in throughout the nervous system, but the α2ARs on pre- and post-synaptic neurons in the dorsal horn of the spinal cord are the main target for both endogenous and exogenous analgesia. (mdbiosciences.com)
  • These receptors can also be targeted pharmacologically through administration of selective agonists or through the inhibition of noradrenaline (also known as norepinephrine) reuptake by drugs such as tricyclic antidepressants. (mdbiosciences.com)
  • G protein-coupled receptors (GPCRs) represent a large fraction of current pharmaceutical targets, and of the GPCRs, the beta(2) adrenergic receptor (beta(2)AR) is one of the most extensively studied. (rcsb.org)
  • Constitutive activation of G protein-coupled receptors (GPCRs) is now well recognized and many classical GPCR antagonists have been found to be inverse agonists. (aspetjournals.org)
  • For the α 2A -adrenergic receptor (AR) we determine the relative inverse efficacies of a series of antagonists and utilize the extended ternary complex model to estimate the fraction of constitutively active mutant (CAM) receptors in the active state. (aspetjournals.org)
  • For wild-type receptors, R predominates and there is minimal receptor activity in the absence of agonist. (aspetjournals.org)
  • High levels of receptor expression or constitutively active mutant receptors increase the concentration of R * inducing a response in the absence of agonist. (aspetjournals.org)
  • There are three families of adrenergic receptors, alpha 1 , alpha 2 and beta, and each family contains three distinct subtypes. (thefreedictionary.com)
  • The fade of response was attributed to desensitization of nicotinic receptors at the adrenergic nerve terminals on which nicotine and ACh act to release NE. (aspetjournals.org)
  • It is proposed that under conditions where desensitization to the agonist develops in the absence of any vasoconstrictor response, the fraction of receptors in the activated state at any instant in time during the development is too small to trigger the release of NE. (aspetjournals.org)
  • A drug that stimulates adrenergic receptors in the lungs, heart, uterus, and other organs. (thefreedictionary.com)
  • 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)
  • 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)
  • 2. The effects of adrenaline are shown to be brought about through beta-adrenergic receptors and to be mimicked by other agents which increase cell cyclic AMP concentrations. (biochemj.org)
  • On the other hand, it does not complete selectivity of these drugs on α 2 - adrenoreceptors, it causes that they can activate in greater or minor measured and depending on each molecule in particular, α 1- adrenergic receptors fundamentally, and even other types like imidazoline receptors. (vin.com)
  • It can also contribute to its sedative actions, the presence of postsynaptic α 2 - adrenergic receptors in the frontal cortex, to mediate its activation the inhibition of the cortical activity. (vin.com)
  • Additionally, when acting on presynaptic α 2 - adrenergic receptors located on noradrenergic neurons like on other non-noradrenergic neurons, these drugs can modulate the release and the recaptation of norepinephrine and others neurotransmitters that also take place in the regulation of the arousal and vigilance. (vin.com)
  • These drugs produce a powerful analgesic effect by stimulating α 2 - adrenergic receptors located at various sites in the pain pathway within the brain, include the LC, and spinal cord. (vin.com)
  • Additionally, the activation of presynaptic α 2 - adrenergic receptors located on neurons of the dorsal horn of spinal cord, where nociceptive fibers synapse, also produces the inhibition of the nociceptive responses to inhibit the release of exciter nociceptive neurotransmitters. (vin.com)
  • These antinociceptive effects are related to the stimulation of α 2 - adrenergic receptors located in the nociceptive neurons of the dorsal horn of spinal cord. (vin.com)
  • Brimonidine and oxymetazoline underwent pharmacological profiling with a standard panel of 151 assays, including α-adrenergic receptors and 5-hydroxytryptamine (5-HT) receptors. (springer.com)
  • Brimonidine was highly selective for the α 2 adrenergic receptors, specifically α 2A , whereas oxymetazoline was found to be much less selective and was highly active against a wide range of targets. (springer.com)
  • Pharmacological profiling showed brimonidine to be highly selective for the α 2 adrenergic receptors, whereas oxymetazoline was much less selective with a significant number of off-target activities, including the 5-hydroxytryptamine 2B (5-HT 2B ) serotonin receptor. (springer.com)
  • Release of endogenous catecholamines and activation of the beta-adrenergic receptors (b-AR) have also been shown to be involved in ischaemic preconditioning. (sun.ac.za)
  • the respective roles of the A1-, A2-, A3-adenosine receptors as well as the involvement of the PI3-K/PKB/Akt and ERKp44/p42 signal transduction pathways, in the cardioprotective phenomemon of -adrenergic preconditioning and (iv) the contribution of the mitochondrial KATP channels (mKATP), reactive oxygen species and NO to the mechanism of -AR-induced cardioprotection. (sun.ac.za)
  • However, the exact role that beta-1 adrenergic receptors (beta1AR) have in this process has not been elucidated. (iupui.edu)
  • Adrenergic receptors are a class of G protein-coupled receptors that are targets of the catecholamines, especially norepinephrine and epinephrine. (medchemexpress.com)
  • There are two main groups of adrenergic receptors, α and β, with several subtypes. (medchemexpress.com)
  • ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with K i s of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively. (medchemexpress.com)
  • R)-(-)-Phenylephrine hydrochloride is a selective α 1 -adrenoceptor agonist with pK i s of 5.86, 4.87 and 4.70 for α 1D , α 1B and α 1A receptors respectively. (medchemexpress.com)
  • Adrenergic agonists and antagonists produce their clinical effects by interacting with the adrenergic receptors (ie, adrenoceptors). (mhmedical.com)
  • Again these drugs are specific to the β 2 adrenergic receptors particularly acting on bronchioles producing relaxation. (egpat.com)
  • Adrenergic receptors used both cyclic adenosine monophosphate (cAMP) as second messenger system and phosphatidylinositol cyclic to transduce the signal into an effect. (alleviatenow.in)
  • Adrenergic Agonists are drugs that lead to stimulation of the adrenergic receptors . (pathwaymedicine.org)
  • Indirect agonists do not physically bind adrenergic receptors. (pathwaymedicine.org)
  • As such, these compounds directly bind adrenergic receptors but also promote the indirect mechanisms described above. (pathwaymedicine.org)
  • A highly conserved tyrosine residue in G protein-coupled receptors is required for agonist-mediated beta 2-adrenergic receptor sequestration. (duke.edu)
  • The potential role of this conserved aromatic amino acid residue in the cellular processes of sequestration (a rapid internalization of the surface receptor) and down-regulation (a slower loss of total cellular receptors) associated with agonist-mediated desensitization of the beta 2-adrenergic receptor was assessed by replacing tyrosine residue 326 with an alanine residue (beta 2AR-Y326A). (duke.edu)
  • These results imply that this tyrosine residue, which is part of a highly conserved sequence motif in G protein-coupled receptors, may be responsible for their agonist-mediated sequestration and that sequestration and down-regulation of the receptor are dissociable phenomena. (duke.edu)
  • The lack of resensitization in the sequestration-defective beta 2-adrenergic receptor mutant strongly suggests that the sequestration pathway is an important mechanism by which cells re-establish the normal responsiveness of G protein-coupled receptors following the removal of agonist. (duke.edu)
  • Indirect-acting adrenergic agonists are compounds that cause activation of adrenergic receptors by mechanisms other than their direct binding. (pathwaymedicine.org)
  • The data obtained demonstrate that, as observed by others in the awake animal, activation of α 2 -adrenergic receptors in the RVM produces hypoalgesia. (elsevier.com)
  • 2. The method of claim 1 wherein the β-adrenergic inverse agonist is selected from the group consisting of β 2 -selective inverse agonists, and non-selective inverse agonists having inverse agonist activity against both bi- and 2-adrenergic receptors. (patentsencyclopedia.com)
  • Agonists induce the formation of a guanine nucleotide-sensitive high-affinity state of alpha 2 but not alpha 1 receptors. (meta.org)
  • However, in the liver, alpha-adrenergic effects such as glycogen phosphorylase activation are shown to be mediated via alpha 1 receptors. (meta.org)
  • Thus, in liver membranes the endogenous 'physiological' agonist may not label the physiologically relevant alpha 1 receptors in typical radioligand binding assays using low concentrations of [3H]epinephrine. (meta.org)
  • 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)
  • In the current study, we used [35S]GTPgammaS incorporation to characterize the intrinsic activity and potency of agonists and antagonists at the cloned mouse alpha2a/d and human alpha2a, alpha2b, and alpha2c ARs. (nih.gov)
  • Antagonists did not increase [35S]GTPgammaS binding but competitively inhibited agonist-stimulated [35S]GTPgammaS binding. (nih.gov)
  • Inverse agonist activity of beta-adrenergic antagonists. (aspetjournals.org)
  • Furthermore, receptor ligand cross-docking experiments revealed that a single beta(2)AR complex can be suitable for docking of a range of antagonists and inverse agonists but also indicate that additional ligand-receptor structures may be useful to further improve performance for in-silico docking or lead-optimization in drug design. (rcsb.org)
  • In AN, in contrast to normal subjects, cholinergic antagonists and agonists, whose action is somatostatin (SS)-mediated, have reduced and absent effects on the GH response to growth hormone-releasing hormone (GHRH). (unboundmedicine.com)
  • To further clarify the neural control of AH secretion in AN, we evaluated the effects of beta-adrenergic agonists and antagonists, which are known to inhibit and increase, respectively, the GHRH-induced GH secretion in normal subjects. (unboundmedicine.com)
  • This striking difference in inverse efficacy between idazoxan and RX821002 may account for in vivo pharmacological differences between these two α 2 -adrenergic antagonists. (aspetjournals.org)
  • In contrast, neutral antagonists bind equally well to R and R *, have no effect on basal receptor activity, but block the effects of both agonists and inverse agonists. (aspetjournals.org)
  • 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)
  • Carlos G. Musso and Jose Alfie, "Resistant Hypertension in the Elderly-Second Line Treatments: Aldosterone Antagonists, Central Alpha-Agonist Agents, Alpha-Adrenergic Receptor Blockers, Direct Vasodilators, and Exogenous Nitric Oxide Donors", Cardiovascular & Hematological Agents in Medicinal Chemistry (2014) 12: 170. (eurekaselect.com)
  • Adrenergic drugs either stimulate a response (agonists) or inhibit a response (antagonists). (wikidoc.org)
  • However, unlike in the awake animal, when antagonists selective for either the α 1 - or α 2 -adrenergic receptor are microinjected alone into the RVM there is no change in the nociceptive threshold. (elsevier.com)
  • 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)
  • 5. A method according to claim 1, wherein said alpha adrenergic receptor agonist is selected from the group consisting of epinephrine, norepinephrine, methoxamine, and phenylephrine. (freepatentsonline.com)
  • The alpha-adrenergic agonist phenylephrine significantly decreased activities of GPAT and PPH. (portlandpress.com)
  • R)-(-)-Phenylephrine is a selective α 1 -adrenoceptor agonist primarily used as a decongestant. (medchemexpress.com)
  • Pseudoephedrine acts indirectly on the adrenergic receptor system, whereas phenylephrine and oxymetazoline are direct agonists . (wikipedia.org)
  • Selected examples are: Clonidine (mixed alpha2-adrenergic and imidazoline-I1 receptor agonist) Dexmedetomidine Fadolmidine Guanfacine, (preference for alpha2A-subtype of adrenoceptor) Guanabenz (most selective agonist for alpha2-adrenergic as opposed to imidazoline-I1) Guanoxabenz (metabolite of guanabenz) Guanethidine (peripheral alpha2-receptor agonist) Xylazine, Tizanidine Medetomidine Methyldopa Methylnorepinephrine Norepinephrine (R)-3-nitrobiphenyline is an α2C selective agonist as well as being a weak antagonist at the α2A and α2B subtypes. (wikipedia.org)
  • Compounds with intrinsic activities less than that of the full agonists norepinephrine (NE) or epinephrine (EPI) were capable of antagonizing agonist-stimulated [35S]GTPgammaS binding. (nih.gov)
  • A subcutaneous injection of an oil suspension of l-epinephrine (270 mumol/kg), dopamine (270 mumol/kg) or l-norepinephrine (270 mumol/kg), when administered with phenoxybenzamine (32 mumol/kg i.p.) to blocl alpha adrenergic effects, increases the cyclic 3', 5'-adenosine monophosphate (cAMP) content in superior cervical ganglia (SCG) of rats. (aspetjournals.org)
  • After complete fade of the response during continued infusion of either nicotine or ACh (in the presence of atropine), the vasoconstrictor responses to stimulation of periarterial adrenergic neurons or to infused norepinephrine (NE) were not diminished. (aspetjournals.org)
  • Clonidine is an α2-adrenergic receptor agonist which, at low doses, inhibits noradrenergic signaling by decreasing norepinephrine release from presynaptic noradrenergic neurons. (iupui.edu)
  • The term adrenergic originally referred to the effects of epinephrine ( adren aline), although norepinephrine (noradrenaline) is the primary neurotransmitter responsible for most of the adrenergic activity of the sympathetic nervous system. (mhmedical.com)
  • The vast majority of decongestants act via enhancing norepinephrine (noradrenaline) and epinephrine (adrenaline) or adrenergic activity by stimulating the α1-adrenergic receptor since they mediate vasoconstriction and constricting nasal vasculature causes decongestion of nasal mucosa. (wikipedia.org)
  • In general, indirect agonists act to promote release of endogenously-stored norepinephrine from presynaptic terminals. (pathwaymedicine.org)
  • When inhaled, beta-2 agonists relax the smooth muscle in the airways of asthma patients by mimicking the actions of epinephrine and norepinephrine, substances that are secreted by sympathetic nerves. (howstuffworks.com)
  • The present experiments, part of an ongoing study designed to characterise the role norepinephrine (NE) in regulating the activity of putative nociceptive modulatory neurons in the rostral ventromedial medulla (RVM), assessed the effects of α-adrenergic receptor-selective agents on the nociceptive threshold (as measured by the tail-flick withdrawal response on noxious heat). (elsevier.com)
  • The drug salbutamol (SBL) is a β-agonist that may be used illegally as an animal growth promoter. (tudelft.nl)
  • We studied the effect of atenolol (ATE), a beta 1-adrenergic antagonist, and salbutamol (SALB), a beta 2-adrenergic agonist, on the GHRH-induced GH release in 10 patients with AN and in 10 normal age-matched women (NW). (unboundmedicine.com)
  • On daily administration from day 0 after immunization, the beta2-selective AR agonists formoterol or salbutamol ameliorated EAM on day 21 and increased myocardial interleukin-10/interferon-gamma mRNA levels. (eurekamag.com)
  • The adsorption of beta(2)-adrenergic agonist (βAA) drugs clenbuterol, salbutamol, and terbutaline on metal surfaces has been investigated in this work by means of surface-enhanced Raman scattering (SERS). (semanticscholar.org)
  • An inhaled long-acting beta2-adrenergic receptor agonist used as a bronchodilator in the management of asthma and COPD. (drugbank.ca)
  • A long-acting beta2-adrenergic agonist used in the management of chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema. (drugbank.ca)
  • Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach. (nih.gov)
  • The therapeutic potential of beta2-adrenergic receptor (AR) agonists in the treatment of autoimmune diseases has been reported. (eurekamag.com)
  • A beta-1 agonist used to treat cardiac decompensation in patients with organic heart disease or from cardiac surgery. (drugbank.ca)
  • In vitro addition of beta2-selective AR agonists inhibited the activation of cardiac myosin fragment-specific myocarditogenic T lymphocytes, and this effect was reversed by ICI118,551, a beta2-selective AR antagonist. (eurekamag.com)
  • Mivazerol is a new and selective alpha 2-adrenoceptor agonist, devoid of hypotensive effects, which has been designed to prevent adverse cardiac outcome in perioperative patients with, or at risk coronary artery disease . (curehunter.com)
  • Mechanism of cytokine inhibition of beta-adrenergic agonist stimulation of cyclic AMP in rat cardiac myocytes. (ahajournals.org)
  • Studies conducted in our laboratory have demonstrated that activated immune cells produce a soluble inhibitor(s) of cardiac myocyte contractile and cyclic AMP (cAMP) responses to beta-adrenergic stimulation. (ahajournals.org)
  • Isoprenaline hydrochloride is a non-selective β-adrenergic receptor agonist with potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. (medchemexpress.com)
  • Arbutamine is a short-acting synthetic potent nonselective β-adrenoceptor agonist that increases heart rate, cardiac contractility, and systolic blood pressure. (medchemexpress.com)
  • Dobutamine is a β 1 adrenergic receptor agonists that specifically acts on cardiac muscle increasing both rate and force of contraction. (egpat.com)
  • they are called β 2 -adrenergic agonists and can relieve bronchospasms without unwanted cardiac side effects of nonspecific β-agonists (for example, ephedrine or epinephrine ). (wikipedia.org)
  • Direct agonists bind to the receptor, whereas indirect agonists increase endogenous neurotransmitter activity. (mhmedical.com)
  • The G-protein receptor can affect the function of adenylate cyclase or phospholipase C , an agonist of the receptor will upregulate the effects on the downstream pathway (it will not necessarily upregulate the pathway itself). (rug.nl)
  • PIC had minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, but it potentiated platelet aggregation induced by ADP with an EC50 of 1.5 microM. (biomedsearch.com)
  • Thus, interference with agonist-occupied beta-adrenergic receptor coupling to adenylate cyclase to produce cAMP and subsequent contractile responses is induced by a factor(s) elaborated by activated immune cells. (ahajournals.org)
  • Adenylate cyclase response to beta-adrenergic agonists in heart and brown adipose tissue]. (semanticscholar.org)
  • We then injected the mice with terbutaline, a β2-AR agonist, to stimulate β2-AR signaling and found that platelet counts improved in both groups of mice. (prnewswire.co.uk)
  • OBJECTIVES: To assess the effectiveness of interventions involving the use of alpha2 adrenergic agonists (clonidine, lofexidine, guanfacine, guanabenz acetate) to manage the acute phase of opioid withdrawal. (opioids.com)
  • REVIEWER'S CONCLUSIONS: Treatment regimes based on the alpha2 adrenergic agonists clonidine and lofexidine, and those based on reducing doses of methadone over a period of around 10 days, have similar efficacy in the management of withdrawal from heroin or methadone. (opioids.com)
  • Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist. (adooq.com)
  • 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)
  • 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)
  • 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)
  • In a separate group of male P rats, clonidine (40 µg/kg BW) suppressed intake of a saccharin solution (0.04 g/L). These results are consistent with and complement our previous findings that the α1-adrenergic receptor antagonist, prazosin, decreases voluntary alcohol drinking in alcohol-preferring rats, but suggests that effects of clonidine may not be specific for alcohol. (iupui.edu)
  • Alpha Adrenergic Antagonist (e.g. (fpnotebook.com)
  • 125I]PIC bound to the same number of high affinity sites as the alpha 2-adrenergic receptor (alpha 2-AR) full agonist [3H] bromoxidine (UK14,304), which represented approximately 40% of the sites bound by the antagonist [3H]yohimbine. (biomedsearch.com)
  • Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K i values of 1.8 nM and 0.8 nM, respectively. (medchemexpress.com)
  • The sympathomimetic acts on adrenergic receptor either directly (Direct-acting-agonist) or indirectly (Indirect-acting-agonist) by enhance release or blocking reuptake of NE (Indirect -acting-antagonist). (alleviatenow.in)
  • The binding properties of two alpha-adrenergic radioligands, [3H]epinephrine (an agonist) and [3H]dihydroergocryptine (an antagonist), were compared in two model systems--membranes derived from human platelets and membranes from rat liver. (meta.org)
  • α1 agonist: stimulates phospholipase C activity. (wikipedia.org)
  • α 1 agonists: stimulates phospholipase C activity. (wikidoc.org)
  • Other drugs affect the uptake and storage mechanisms of adrenergic catecholamines, prolonging their action. (rug.nl)
  • These are the drugs which increase adrenergic transmission and therefore produce all effects shown by sympathetic system. (egpat.com)
  • Zanaflex belongs to a class of drugs called Central Alpha-2-Adrenergic Agonist . (rxlist.com)
  • The three types of prescription bronchodilating drugs are β 2 ("beta two")-adrenergic agonists (short- and long-acting), anticholinergics (short- and long-acting), and theophylline (long-acting). (wikipedia.org)
  • The adrenergic drugs are activate the adrenergic receptor or adrenoreceptor by stimulating nor epinephrine (Nor adrenaline) or Epinephrine (Adrenaline). (alleviatenow.in)
  • The drugs that are blocks the activation of adrenergic receptor are named as sympatholytic. (alleviatenow.in)
  • We conclude that beta-adrenergic stimulation of KCa channel activity and relaxation of tone in airway smooth muscle occurs, in part, by means independent of cyclic AMP formation. (jci.org)
  • a site in a sympathetic effector cell that reacts to adrenergic stimulation. (thefreedictionary.com)
  • For four decades, the α 2 - adrenergic agonists they have been used in the veterinary medicine to obtain sedation, analgesia and muscle relaxation, in a great variety of domestic and exotic species, although the relation of these actions with the stimulation of α 2 - adrenoreceptors were not established until 1981 by Hsu. (vin.com)
  • The relatively greater response to α 1 -adrenergic-receptor stimulation in the calf may represent an adaptive mechanism that limits blood pooling and capillary filtration in the legs during standing. (elsevier.com)
  • The β 2 adrenoceptor has been cloned and sequenced, and details of how agonist stimulation ultimately results in clinically evident effects are now known. (elsevier.com)
  • An alpha-2 selective adrenergic agonist used as an antihypertensive agent. (fpnotebook.com)
  • To quantify the dose-related effects of various doses and types of selective adrenergic agonist oral decongestants on systolic and diastolic blood pressure. (cochrane.org)
  • More selective agonists are more useful in pharmacology. (rug.nl)
  • 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)
  • The pattern of phosphorylation observed with the beta-adrenergic agonist isoprenaline was similar to that observed with insulin. (biochemj.org)
  • Negligible activity was observed with brimonidine at the 5-HT 2B receptor, whereas oxymetazoline had significant 5-HT 2B receptor agonist activity and caused proliferation of mitral VICs in vitro. (springer.com)
  • 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)
  • α 2 agonists: inhibits adenylyl cyclase activity. (wikidoc.org)
  • ENGLISH ABSTRACT: The Mechanism of -adrenergic preconditioning ( -PC) Ischaemic preconditioning (IPC), a potent endogenous protective intervention against myocardial ischaemia, is induced by exposure of the heart to repetitive short episodes of ischaemia and reperfusion. (sun.ac.za)
  • Caspase-3 and TNF-α levels were significantly reduced at 50nM in cultured cells, a dose lower than that of a non-specific beta-adrenergic agonist, isoproterenol. (arvojournals.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)
  • Hearts were preconditioned with 5 min isoproterenol 0.1 μM ( 1/ 2-AR agonist), or formoterol 1 nM ( 2-AR agonist) or BRL 37344 1 μM ( 3-AR agonist) followed by 5 min reperfusion. (sun.ac.za)
  • An adrenergic agent is a drug, or other substance, which has effects similar to, or the same as, epinephrine (adrenaline). (wikipedia.org)
  • An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. (fpnotebook.com)
  • Adrenergic bronchodilators are medicines that stimulate the nerves in many parts of the body, causing different effects. (mayoclinic.org)
  • For several years it is known that β-adrenergic receptor agonists have anti-inflammatory effects. (tudelft.nl)
  • Objective and Design: To investigate the suppressive effects of the β-agonist clenbuterol on the release of TNF-α and IL-6 in a lipopolysaccharide (LPS)-model of inflammation, both in vitro and in vivo. (tudelft.nl)
  • The β2-selective AR agonist clenbuterol was administered before, during, and after LPS-challenge to investigate its effects on the acute inflammatory response and associated liver-failure. (tudelft.nl)
  • To determine the effects of adrenergic agonist oral decongestants on variability of blood pressure. (cochrane.org)
  • To quantify the dose-related effects of adrenergic agonist oral decongestants on heart rate. (cochrane.org)
  • To quantify the effects of different doses of adrenergic agonist oral decongestants on withdrawals due to adverse events. (cochrane.org)
  • We speculate that during labor the elevated levels of prostaglandin E may induce similar effects on the myometrium, thereby decreasing the efficacy of beta-agonists as tocolytics. (biomedsearch.com)
  • The sedative effects of the α 2 - adrenergic agonists is mainly attributed to its capacity to reduce the activity of noradrenergic neurons of Locus coeruleus ( LC) on the pons and lower brainstem and thus to diminish activity of the noradrenergic activator projections ascending towards superior cerebral structures. (vin.com)
  • Mivazerol, a new alpha 2-adrenergic agonist, blunts cardiovascular effects following surgical stress in pentobarbital-anesthetized rats. (curehunter.com)
  • 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)
  • However, the effects of adrenergic agonists on spinal cord blood flow (SCBF) and spinal vessels have not yet been clearly defined. (asahq.org)
  • A better assessment of the direct spinal microvascular actions of adrenergic agonists might enable a better evaluation of their contribution to the prolongation of spinal anesthesia and their safety (in terms of their effects on the spinal microcirculation). (asahq.org)
  • There has been little attempt to evaluate the comparative effects of adrenergic agonists on the spinal and cerebral vascular beds in in vivo experiments. (asahq.org)
  • We examined the effects of β 2 -agonist on dry air-induced injury in canine peripheral airways. (elsevier.com)
  • We show that beta-adrenergic receptor/channel coupling is not affected by inhibition of endogenous ATP, and that activation of KCa channels is stimulated by both alpha S and cAMP-dependent protein kinase (PKA). (jci.org)
  • Direct agonists physically bind the adrenergic receptor and simulate binding of an endogenous ligand. (pathwaymedicine.org)
  • This class of agents has been shown to have potent and selective agonist activity at the alpha 2-adrenoceptors. (nih.gov)
  • Brimonidine tartrate is a highly selective α 2 adrenergic receptor agonist with potent vasoconstrictive activity used as an ophthalmic solution for the initial and long-term management of ocular hypertension and glaucoma [ 5 ]. (springer.com)
  • Vibegron (MK-4618) is a potent, highly selective β 3 -adrenoceptor agonist ( EC 50 =1.1 nM). (medchemexpress.com)
  • Both the rate and degree of desensitization to nicotine decreased as the temperature was decreased from 37 degrees to 27 degrees C. The present results are consistent with the concept that the nicotinic receptor (or receptor mechanism) at the adrenergic nerve terminal, after being activated as a result of combination with the agonist, can undergo a transformation to an inactive or desensitized state. (aspetjournals.org)
  • Insights into agonist binding and the corresponding conformational changes triggering GPCR activation mechanism are of special interest. (pubmedcentralcanada.ca)
  • However, the exact mechanism whereby activation of the - adrenergic signal transduction pathway leads to cardioprotection, is still unknown. (sun.ac.za)
  • 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)
  • 1: Yanagisawa T, Sato T, Yamada H, Sukegawa J, Nunoki K. Selectivity and potency of agonists for the three subtypes of cloned human beta-adrenoceptors expressed in Chinese hamster ovary cells. (medkoo.com)
  • alpha-adrenergic, which act in response to sympathomimetic stimuli, and beta-adrenergic, which block sympathomimetic activity. (thefreedictionary.com)
  • Fingerprint Dive into the research topics of 'Heterogeneous responses of human limbs to infused adrenergic agonists: A gravitational effect? (elsevier.com)
  • Agonist-independent properties of the human beta 2-adrenergic receptor (beta 2AR) were studied using the baculovirus expression system in Sf9 cells. (aspetjournals.org)
  • An aromatic residue, tyrosine 326 in the prototypical human beta 2-adrenergic receptor, exists in a highly conserved sequence motif in virtually all members of the G protein-coupled receptor family. (duke.edu)
  • In general, a primary or secondary aliphatic amine separated by 2 carbons from a substituted benzene ring is minimally required for high agonist activity. (rug.nl)
  • The compounds were screened for beta(2), beta(1), and beta(3) agonist activity in CHO cells. (nih.gov)
  • Analysis of this difference by the extended ternary complex model indicates that approximately 50% of the CAM α 2A -AR is in the active ( R *) state although there is no detectable constitutive activity of the WT receptor in the absence of agonist. (aspetjournals.org)
  • The elevation of TH activity elicited in SCG by beta adrenergic receptor agonists is always preceded by an increase of cAMP concentration lasting 90 minutes or longer. (aspetjournals.org)
  • Administration of the beta-adrenergic agonist BRL 26830A mimicked the effect of cold on microsomal GPAT activity. (portlandpress.com)
  • however, the α-2A subtype has also been associated with dose-dependent sedation and decreased blood pressure, thus narrowing the therapeutic window of α-2 agonists when used clinically for analgesic activity. (asahq.org)
  • Desensitization of the adrenergic neurons of the isolated rabbit ear artery to nicotinic agonists. (aspetjournals.org)
  • Agonist binding affinity to the non-G protein-coupled CAM receptor was 3- to 9-fold higher than to WT, whereas binding of the most efficacious inverse agonists, yohimbine and rauwolscine, was 1.7- and 2.1-fold weaker. (aspetjournals.org)
  • Parameters of beta-adrenergic receptor binding and affinity were also unaffected. (ahajournals.org)
  • In the absence of agonist but in the presence of GTP, membranes from cells expressing the beta 2AR exhibited higher levels of cAMP production than did membranes from uninfected cells or from cells infected with wild-type baculovirus. (aspetjournals.org)
  • Indirectly acting adrenergic agonists affect the uptake and storage mechanisms involved in adrenergic signalling. (rug.nl)
  • A beta-2 adrenergic agonist used to treat bronchospasm, asthma, and COPD. (drugbank.ca)
  • A beta-2 adrenergic receptor agonist used to treat asthma, bronchitis, COPD, as well as prevent exercise induced bronchospasms. (drugbank.ca)
  • A beta-2 adrenergic agonist and bronchodilator used for the symptomatic treatment of asthma. (drugbank.ca)
  • A beta-2 adrenergic receptor agonist and bronchodilator used for the treatment of asthma and chronic obstructive pulmonary disease (COPD). (drugbank.ca)
  • To assess whether increased short-acting β(2)-adrenergic agonist (SABA) claims are associated with asthma exacerbations and increased healthcare costs. (nih.gov)
  • Beta agonists are used to treat asthma and chronic obstructive lung diseases and to manage pregnancy. (thefreedictionary.com)
  • Patients who regularly or frequently need to take a short-acting β 2 -adrenergic agonist should consult their doctor, as such usage indicates uncontrolled asthma, and their routine medications may need adjustment. (wikipedia.org)
  • Because it has no effect on asthma symptoms when used alone, it is most often paired with a short-acting β 2 -adrenergic agonist. (wikipedia.org)
  • Many receptor agonists are available for asthma therapy, including a new generation of long acting agents (such as salmeterol) with duration of action of 12 hours or more. (elsevier.com)
  • Statistical links between beta agonist use and asthma mortality or morbidity warrant careful examination for clinical relevance, but may not be dismissed. (elsevier.com)
  • Beta agonists are relatively safe and clearly effective in asthma, but anti-inflammatory management (including allergen avoidance and immunotherapy when appropriate) is indicated in patients who require chronic therapy. (elsevier.com)
  • A beta-2 adrenergic agonist and bronchodilator used for long term, symptomatic treatment of reversible bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. (drugbank.ca)
  • We have previously demonstrated the ability of dobutamine (DOB), primarily a beta1AR agonist, to inhibit reductions in cancellous bone formation and mitigate disuse-induced loss of bone mass. (iupui.edu)
  • 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)