One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.
Compounds possessing both a hydroxyl (-OH) and an amino group (-NH2).
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.
Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.
A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
A beta-1 adrenergic antagonist that has been used in the emergency treatment of CARDIAC ARRYTHMIAS.
A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.
A vasodilator with general properties similar to NITROGLYCERIN but with a more prolonged duration of action. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1025)
Cell-surface proteins that bind epinephrine and/or norepinephrine with high affinity and trigger intracellular changes. The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. Adrenergic receptors may also be classified according to the subtypes of G-proteins with which they bind; this scheme does not respect the alpha-beta distinction.
One of 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.
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-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.
Drugs that selectively bind to and activate beta-adrenergic receptors.
AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.
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.
A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.
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 short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236)
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
An order of the class Amphibia, which includes several families of frogs and toads. They are characterized by well developed hind limbs adapted for jumping, fused head and trunk and webbed toes. The term "toad" is ambiguous and is properly applied only to the family Bufonidae.
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.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
Physiological processes and properties of the RESPIRATORY SYSTEM as a whole or of any of its parts.
Process of administering an anesthetic through injection directly into the bloodstream.
A general class of ortho-dihydroxyphenylalkylamines derived from tyrosine.
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.
The former British crown colony located off the southeast coast of China, comprised of Hong Kong Island, Kowloon Peninsula, and New Territories. The three sites were ceded to the British by the Chinese respectively in 1841, 1860, and 1898. Hong Kong reverted to China in July 1997. The name represents the Cantonese pronunciation of the Chinese xianggang, fragrant port, from xiang, perfume and gang, port or harbor, with reference to its currents sweetened by fresh water from a river west of it.
Services providing pharmaceutic and therapeutic drug information and consultation.
Prudent standard preventive measures to be taken by professional and other health personnel in contact with persons afflicted with a communicable disease, to avoid contracting the disease by contagion or infection. Precautions are especially applicable in the diagnosis and care of AIDS patients.
A country spanning from central Asia to the Pacific Ocean.
Modified cardiac muscle fibers composing the terminal portion of the heart conduction system.
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
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)
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.
An impulse-conducting system composed of modified cardiac muscle, having the power of spontaneous rhythmicity and conduction more highly developed than the rest of the heart.
The period of time following the triggering of an ACTION POTENTIAL when the CELL MEMBRANE has changed to an unexcitable state and is gradually restored to the resting (excitable) state. During the absolute refractory period no other stimulus can trigger a response. This is followed by the relative refractory period during which the cell gradually becomes more excitable and the stronger impulse that is required to illicit a response gradually lessens to that required during the resting state.
The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
Precordial pain at rest, which may precede a MYOCARDIAL INFARCTION.
A clinical syndrome characterized by the development of CHEST PAIN at rest with concomitant transient ST segment elevation in the ELECTROCARDIOGRAM, but with preserved exercise capacity.
Persistent and reproducible chest discomfort usually precipitated by a physical exertion that dissipates upon cessation of such an activity. The symptoms are manifestations of MYOCARDIAL ISCHEMIA.
The volume of water filtered out of plasma through glomerular capillary walls into Bowman's capsules per unit of time. It is considered to be equivalent to INULIN clearance.
The amount of PLASMA that perfuses the KIDNEYS per unit time, approximately 10% greater than effective renal plasma flow (RENAL PLASMA FLOW, EFFECTIVE). It should be differentiated from the RENAL BLOOD FLOW; (RBF), which refers to the total volume of BLOOD flowing through the renal vasculature, while the renal plasma flow refers to the rate of plasma flow (RPF).
The amount of PLASMA flowing to the parts of the KIDNEY that function in the production of urine. It is the amount of plasma perfusing the KIDNEY TUBULES per unit time, generally measured by P-AMINOHIPPURATE clearance. It should be differentiated from RENAL PLASMA FLOW which is approximately 10% greater than the effective renal plasma flow.
The circulation of the BLOOD through the vessels of the KIDNEY.
Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.
A statistical means of summarizing information from a series of measurements on one individual. It is frequently used in clinical pharmacology where the AUC from serum levels can be interpreted as the total uptake of whatever has been administered. As a plot of the concentration of a drug against time, after a single dose of medicine, producing a standard shape curve, it is a means of comparing the bioavailability of the same drug made by different companies. (From Winslade, Dictionary of Clinical Research, 1992)
The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity.
The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action.
The giving of drugs, chemicals, or other substances by mouth.
Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site.
The long-term (minutes to hours) administration of a fluid into the vein through venipuncture, either by letting the fluid flow by gravity or by pumping it.

Identification of cardiac beta-adrenergic receptors by (minus) [3H]alprenolol binding. (1/127)

(Minus) [3-H] alprenolol, a potent beta-adrenergic antagonist, was used to identify binding sites in a fraction of canine cyocardium. Beta adrenergic agonists and antagonists compete for these binding sites in a manner which directly parallels their known affinity for the cardiac beta-adrenergic receptor. Thus, binding was highly stereo-specific, with the (minus) isomers of beta-adrenergic agonists or antagonists being at least two orders of magnitude more potent than were the (plus) isomers in competing for these sites. The order of potency for inhibition of binding by beta-adrenergic agonists was (minus) isoproterenol greater than (minus) epinephrine greater than (minus) norepinephrine. The dissociation constant (KD) of (minus) alprenolol for the beta-adrenergic receptors was 7-11 nM as determined independently by direct binding studies or by inhibition of isoproterenol-stimulated adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1]. The beta-adrenergic antagonist (minus) propranolol also had high affinity for the binding sites (KD equals 12 nM). The physiologically inactive catechol-containing compounds pyrocatechol and (plus or minus) dihydroxymandelic acid, as well as the metabolite (plus or minus) normetanephrine, and the alpha-adrenergic antagonist phentolamine did not compete for the binding sites at a concentration of 160 muM. Binding was rapid (t1/2 less than 30 sec) and was rapidly reversible (t1/2 less than 15 sec). The binding sites were saturable and bound 0.35 pmol of (minus) [3-H] alprenolol per mg of membrane protein. These characteristics suggest that these binding sites represent the cardiac beta-adrenergic receptors.  (+info)

Catecholamine-induced subsensitivity of adenylate cyclase associated with loss of beta-adrenergic receptor binding sites. (2/127)

Injection of frogs with beta-adrenergic catecholamines for 1-24 hr produces marked subsensitivity of the erythrocyte membrane adenylate cyclase [ATP pyrophosphate-lyase (cyclizing); EC 4.6.1.1.] to in vitro stimulation by isoproterenol. The subsensitization is specific for catecholamine stimulation, since basal and fluoride-stimulated enzyme activity are unaffected. Maximum isoproterenol-stimulated adenylate cyclase activity declines by 75% in the isoproterenol-treated animals (P less than 0.001). The concentration of isoproterenol causing one-half maximal activation of adenylate cyclase, however, is unaltered. (-)[3H]Alprenolol, a potent competitive beta-adrenergic antagonist, was used to study directly the beta-adrenergic receptor binding sites in the erythrocyte membranes from control and subsensitized animals. A highly significant (P less than 0.005) 60% fall in the number of the beta-adrenergic receptor binding sites ("specific"(-)[3H]alprenolol binding sites) in the treated animals was found. The binding affinity of the sites was not markedly altered. These data suggest that beta-adrenergic catecholamines are able to regulate catecholamine sensitivity of tissues in vivo, by regulating the properties of the beta-adrenergic receptor binding sites.  (+info)

Rapid changes in rat pineal beta-adrenergic receptor: alterations in l-(3H)alprenolol binding and adenylate cyclase. (3/127)

The properties of the beta-adrenergic receptor which regulates adenylate cyclase [ATP pyrophosphate-lyase (cyclizing)8 EC 4.6.1.1] in the pineal gland are similar to the properties of the sites which specifically bind l-[3H]alprenolol, a potent beta-adrenergic antagonist. Stimulation of the beta-adrenergic receptor results in a 30-fold increase in the activity of N-acetyltransferase (= arylamine acetyltransferase; acetyl CoA:arylamine N-acetyltransferase, EC 2.3.1.5), an enzyme involved in the synthesis of thepineal hormone melatonin. In the normal diurnal light-dark cycle there is greater physiological stimulation of the beta-adrenergic receptor in the pineal during the night than during the day. Pineals from rats kept in constant light for 24 hr possess more hormone-sensitive adenylate cyclase and specifically bind more l-[3H]alprenolol than do pineals from rats kept in the dark overnight. When rats, exposed to light for 24 hr, are treated with the beat-adrenergic agonist isoproterenol, there is a rapid loss of both hormone-sensitive adenylate cyclase activity and specific l-[3H]alprenolol binding sites. There is no change in the affinity of adenylate cyclase for isoproterenol or for its substrate, ATP. Similarly, although there are fewer binding sites, there is no change in the affinity of the remaining sites for either agonist or antagonist. Inhibition of protein synthesis with cycloheximide does not affect the loss of either adenylate cyclase activity or specific binding sites. The data suggest that stimulation of the beta-adrenergic receptor causes a rapid decrease in the number of available receptors and in hormone-sensitive adenylate cyclase activity; conversely, lack of stimulation causes an increase in these parameters. It is suggested that these changes contribute to the phenomena of super- and subsensitivity in the pineal gland by regulating the capacity of the pineal to synthesize cyclic AMP in response to beta-adrenergic stimulation.  (+info)

Involvement of beta1- and beta2- but not beta3-adrenoceptor activation in adrenergic PYY secretion from the isolated colon. (4/127)

The secretion of PYY by endocrine L cells of the terminal gut is under the control of nutrients, the autonomic nervous system and hormones. Catecholamines, and the non-specific beta-adrenergic agonist isoproterenol induce PYY secretion from rat isolated colon or ileum. Because beta3-adrenergic receptors now appear to mediate many of the effects of catecholamines in the gastrointestinal tract, we investigated the involvement of beta1-, beta2-, and beta3-adrenoceptor stimulation in PYY secretion from the isolated, vascularly perfused rat colon. Infusion of 10(-6) M isoproterenol induced a transient increase in PYY secretion (from 36+/-4 to 87+/-20 fmol/2 min; n=7, P<0.05), that was abolished by a previous infusion of the beta1- and beta2-adrenergic blocker (and partial beta3-agonist) alprenolol (10(-6) M). The beta1-adrenergic agonist dobutamine and the beta-2 agonist terbutaline also (both at 10(-5) M) significantly stimulated PYY secretion, from 29+/-1 to 79+/-12 fmol/2 min and from 19+/-1 to 73+/-13 fmol/2 min respectively (n=7, P<0.05). Neither of the beta3-adrenergic agonists tested (BRL 37 344 (10(-5), 10(-6) M) and SR 58 611A (10(-6) M)) significantly stimulated PYY secretion, thus confirming the exclusive involvement of beta1- and beta2-receptors in beta-adrenergic agonist induced hormone secretion.  (+info)

Pharmacological analysis of dopamine action on the isolated dog atrium. (5/127)

The isolated right atrium of the dog was perfused with arterial blood introduced from a carotid artery of a support dog. The selective injection of dopamine, tyramine and norepinephrine into the cannulated sinus node artery induced dose-relatedly positive chronotropic and inotropic effects. However, for an equal increase in sinus rate, dopamine caused less increase in tension development than norepinephrine. Tyramine caused least increase in contractility. Effects induced by dopamine were not blocked by treatment with tetrodotoxin which blocked those induced by nicotine. Desmethylimipramine treatment significantly suppressed dopamine-induced effects and completely blocked tyramine-induced ones but rather enhanced norepinephrine-induced ones. Alprenolol inhibited effects of dopamine, tyramine and norepinephrine. From these results, it is concluded that positive chronotropic and inotropic effects of dopamine are partly due to tyramine-like effect which causes the release of norepinephrine from sympathetic storage sites.  (+info)

Maltodextrin-based proniosomes. (6/127)

Niosomes are nonionic surfactant vesicles that have potential applications in the delivery of hydrophobic or amphiphilic drugs. Our lab developed proniosomes, a dry formulation using a sorbitol carrier coated with nonionic surfactant, which can be used to produce niosomes within minutes by the addition of hot water followed by agitation. The sorbitol carrier in the original proniosomes was soluble in the solvent used to deposit surfactant, so preparation was tedious and the dissolved sorbitol interfered with the encapsulation of one model drug. A novel method is reported here for rapid preparation of proniosomes with a wide range of surfactant loading. A slurry method has been developed to produce proniosomes using maltodextrin as the carrier. The time required to produce proniosomes by this simple method is independent of the ratio of surfactant solution to carrier material and appears to be scalable. The flexibility of the proniosome preparation method would allow for the optimization of drug encapsulation in the final formulation based on the type and amount of maltodextrin. This formulation of proniosomes is a practical and simple method of producing niosomes at the point of use for drug delivery.  (+info)

Effect of chronic beta-adrenergic receptor blockade in congestive cardiomyopathy. (7/127)

Adrenergic beta-blocking agents were given to 7 patients with advanced congestive cardiomyopathy who had tachycardia at rest (98 plus or minus 13 beats/min). The patients were on beta-adrenergic receptor blockade for 2 to 12 months (average 5-4 months). One patient was given alprenolol 50 mg twice daily and the other patients were given practolol 50 to 400 mg twice daily. Virus infection had occurred in 6 of the patients before the onset of symptoms of cardiac disease. All patients were in a steady state or were progressively deteriorating at the start of beta-adrenergic receptor blockade. Conventional treatment with digitalis and diuretics was unaltered or reduced during treatment with beta-blocking agents. An improvement was seen in their clinical condition shortly after administration of the drugs. Continued treatment resulted in an increase in physical working capacity and a reduction of heart size. Noninvasive investigations including phonocardiogram, carotid pulse curve, apex cardiogram, and echocardiogram showed improved ventricular function in all cases. The present study indicates that adrenergic beta-blocking agents can improve heart function in at lease some patients with congestive cardiomyopathy. Furthermore, it is suggested that increased catecholamine activity may be an important factor for the development of this disease, as has been shown in animal experiments.  (+info)

Identification of beta-adrenergic receptors in human lymphocytes by (-) (3H) alprenolol binding. (8/127)

Human lymphocytes are known to posessess a catecholamine-responsive adenylate cyclase which has typical beta-adrenergic specificity. To identify directly and to quantitate these beta-adenergic receptors in human lymphocytes, (-) [3H] alprenolol, a potent beta-adrenergic antagonist, was used to label binding sites in homogenates of human mononuclear leukocytes. Binding of (-) [3H] alprenolol to these sites demonstrated the kinetics, affinity, and stereospecificity expected of binding to adenylate cyclase-coupled beta-adrenergic receptors. Binding was rapid (t1/2 less than 30 s) and rapidly reversible (t1/2 less than 3 min) at 37 degrees C. Binding was a saturable process with 75 +/- 12 fmol (-) [3H] alprenolol bound/mg protein (mean +/- SEM) at saturation, corresponding to about 2,000 sites/cell. Half-maximal saturation occurred at 10 nM (-) [3H] alprenolol, which provides an estimate of the dissociation constant of (-) [3H] alprenolol for the beta-adrenergic receptor. The beta-adrenergic antagonist, (-) propranolol, potently competed for the binding sites, causing half-maximal inhibition of binding at 9 nM. beta-Adrenergic agonists also competed for the binding sites. The order of potency was (-) isoproterenol greater than (-) epinephrine greater than (-)-norepinephrine which agreed with the order of potency of these agents in stimulating leukocyte adenylate cyclase. Dissociation constants computed from binding experiments were virtually identical to those obtained from adenylate cyclase activation studies. Marked stereospecificity was observed for both binding and activation of adenylate cyclase. (-)Stereoisomers of beta-adrenergic agonists and antagonists were 9- to 300-fold more potent than their corresponding (+) stereoisomers. Structurally related compounds devoid of beta-adrenergic activity such as dopamine, dihydroxymandelic acid, normetanephrine, pyrocatechol, and phentolamine did not effectively compete for the binding sites. (-) [3H] alprenolol binding to human mononuclear leukocyte preparations was almost entirely accounted for by binding to small lymphocytes, the predominant cell type in the preparations. No binding was detectable to human erythrocytes. These results demonstrate the feasibility of using direct binding methods to study beta-adrenergic receptors in a human tissue. They also provide an experimental approach to the study of states of altered sensitivity to catecholamines at the receptor level in man.  (+info)

TY - JOUR. T1 - Electrophysiological effects of alprenolol on depressed canine myocardium. AU - Guse, Paul A.. AU - Gaide, Marion S.. AU - Myerburg, Robert J.. AU - Epstein, Kristina. AU - Gelband, Henry. AU - Bassett, Arthur L.. PY - 1980/11. Y1 - 1980/11. N2 - The electrophysiological effects of the β-adrenergic antagonist, alprenolol, were compared in normal and depressed canine myocardium. Both (+) and (±)-alprenolol (5 x 10 -6 and 10 -5 mol.litre -1) decreased action potential amplitude and V̇max in Purkinje fibres superfused with Tyrodes solution in tissue bath. These concentrations shortened action potential duration and effective refractory period of Purkinje fibres but prolonged those of ventricular muscle. Alprenolol more markedly decreased V(max) and sometimes prevented action potential propagation in Purkinje fibres overlying infarcted regions. Similar depressant actions were noted in Purkinje fibres depolarised by exposure to 9 mmol.litre -1 K +. Depolarised and diseased ...
Alprenolol: Search drug information, interaction, images & medical diagnosis. The most comprehensive database of medicines available in China, Hong Kong, T...
hypothetical protein, 5-ht7, 5Ht7, 5-HT-7, 5-HT7 receptor, 5-HT receptor 7a, 5-HT-X, 5-hydroxytryptamine 7 receptor, 5-hydroxytryptamine7 receptor, 5-hydroxytryptamine (serotonin) receptor 7, 5-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled), 5-hydroxytryptamine (serotonin) receptor 7, adenylate cyclase-coupled, Anapl_03536, AS27_02610, AS28_04456, CB1_000689030, D623_10028851, GPRFO, H920_08680, high affinity serotonin receptor (5HT7), I79_004939, M91_18026, M959_09888, MDA_GLEAN10014860, N300_07498, N301_10640, N302_13493, N305_11464, N306_13870, N307_06146, N308_09036, N330_05281, N331_09625, N334_00682, PAL_GLEAN10018375, serotonin 5-hydroxytryptamine 7-a receptor, serotonin receptor 7, Y1Q_023580, Y956_01514, htr7 ...
Seven healthy volunteers showing a fourteenfold range in steady-state plasma concentrations on oral alprenolol (200 mg b.i.d.) were investigated by administration of 5 mg of the drug intravenously and then 50, 100, 150, and 200 mg as single oral doses. The rank order for individual steady-state plasma concentrations was the same as that for the relative bioavailability of the 200 mg dose. The area under the plasma concentration-time curve showed a nonlinear increase with the dose. As the relative availability was a good predictor of steady state while clearance after intravenous administration was not, it was concluded that differences in first-pass elimination markedly contribute to the interindividual variability in steady state plasma concentrations. After pentobarbital treatment, the area under the plasma concentration curve of the 200 mg dose was decreased to 32% and 59% of the pretreatment values in two subjects, but there was no change in the plasma half-life of alprenolol. This indicates
HEK293T-HuHTR7-FLAG cell line is a hypotriploid human cell line, which has been transfected with a human 5-hydroxytryptamine (serotonin) receptor 7, adenylate cyclase-coupled (HTR7) tagged in the N-terminus with FLAG to allow stably express of the human HTR7 tagged in the N-terminus with FLAG. It is an example of a cell line transfected using our proprietary CBTGS gene screening and amplification system.
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β2-Adrenergic receptors (β2AR) play important regulatory roles in a variety of cells and organ systems and are important therapeutic targets in the treatment of airway and cardiovascular disease. Prolonged use of β-agonists results in tolerance secondary to receptor down-regulation resulting in reduced therapeutic efficiency. The purpose of this work is to evaluate the signaling capabilities of the β2AR expressed by a recombinant adeno-associated viral (AAV) vector that also included an enhanced green fluorescent protein (EGFP) gene (AAV-β2AR/EGFP). By epifluorescence microscopy, ~40% of infected HEK 293 cells demonstrated EGFP expression. β2AR density measured with [3H]dihydroalprenolol ([3H]DHA) increased either 13- or 77-fold in infected cells compared to mock infected controls depending on the culture conditions used. The [3H]DHA binding was to a single receptor population with a dissociation constant of 0.42 nM, as would be expected for wild-type β2AR. Agonist competition assays with [3H]DHA
Antianginal drugs, including nitrates, beta-blockers, and calcium channel blockers, are used in the treatment of angina pectoris. Here is the latest research on their use and their mechanism of action. ...
Keywords: Sorbitol Based Proniosomes PermeabilityOral Cephlosporin. Introduction . absorbing the liquid with the tip of a piece of filter paper and sample was International Journal of Research in Pharmaceutical…25 Jun 2017 Publish your
We previously reported that Asn312 of the beta 2-adrenergic receptor and Asn385 in the homologous position in the 5-hydroxytryptamine1A receptor are important for binding to a class of beta-adrenergic receptor antagonists including propranolol and alprenolol. We proposed that the asparagine may be forming a hydrogen bond with the phenoxy oxygen common to these ligands. To further test this hypothesis we made alanine, threonine, phenylalanine, and glutamine substitutions at position 312 in the beta 2-adrenergic receptor. We observed that substitution with amino acids that permit formation of hydrogen bonds (threonine and glutamine) supported binding to aryloxyalkylamines, whereas substitution with amino acids that cannot form hydrogen bonds (alanine and phenylalanine) did not permit binding to these compounds. We were surprised to find that two of these substitutions led to an increase in affinity for alpha-adrenergic ligands. Substitution with glutamine and threonine at position 312 led to a ...
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0214]2-adrenergic receptor numbers were measured in asthmatic mice as follows. Asthmatic mice (ovalbumin-challenged) were treated as follows: Ctrl, no drug treatment with methacholine challenge; salbutamol, a short-acting β2 agonist; carvedilol, a β1, β2 non-selective inverse agonist with α1-adrenergic antagonist activity; nadolol, a highly specific, hydrophilic β1, β2 non-selective inverse agonist; and alprenolol, a β-adrenergic antagonist. Drug treatments were either a single treatment 15 minutes prior to methacholine challenge or ongoing for 28 days (salbutamol was delivered continuously via a subcutaneous osmotic minipump and alprenolol, carvedilol, and nadolol were in animal chow). Mice were sacrificed and lung membranes were isolated as follows. Frozen lung tissue was homogenized in an ice-cold buffer containing 0.32 M sucrose and 25 mM Tris (pH 7.4) using a polytron (Pro 200, Pro Scientific, Inc.). The homogenate was centrifuged at 1000×g for 10 min at 4° C. The resulting ...
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Sobolev A., Rosenkranz A., Kazarov A. A study of mechanisms of post-irradiation changes in adenylate-cyclase activity // International journal of radiation biology and related studies in physics, chemistry, and medicine. - 1983. - Vol. 44, no. 1. - P. 31-39. Hormone-stimulated adenylate-cyclase activity (via beta-adrenergic receptors) is reduced after in vitro irradiation of plasma membranes of frog erythrocytes, at a dose (650 Gy) which does not change the number of beta-adrenergic receptors but causes an oxidative degradation of membrane lipids. Peroxidation of membrane lipids without irradiation also results in a lesser stimulation of adenylate cyclase by the beta-agonist. A possible mechanism of change in adenylate-cyclase functioning is discussed. [ DOI ...
To more fully characterize the alterations in myocardial adrenergic and cholinergic receptors induced by the diabetic state, we investigated the binding characteristics of (-) [3H] dihydroalprenolol to beta adrenergic receptors (bAR), [3H] prazosin to alpha adrenergic receptors (aAR), and [3H] quinuclidinyl-benzilate to muscarinic cholinergic receptors (MCR) in myocardial membranes derived from rats 8 wk after treatment with streptozotocin. We also studied an equal number of animals from three control groups: free-eating nondi-abetics, pair-weighted nondiabetics, and streptozoto-cin-treated animals treated daily with insulin.. Diabetic hearts demonstrated 27% fewer bAR (P , 0.01) and 31% fewer aAR (P , 0.01) than free-eating controls, without changes in MCR, and without changes in antagonist affinity, agonist affinity, or agonist slope factor (pseudo-Hill coefficient) for any class of receptors. Food restriction had no effect on receptor characteristics, and treatment of diabetic rats with ...
Treatment of rats with chemical carcinogens, including 2-acetylaminofluorene (2-AAF), leads to a strong increase in the hepatic catecholamine-sensitive adenylate cyclase activity. The present study was undertaken to investigate the mechanism for the development of this increase. We report that hepatocytes isolated from rats which had been fed 2-AAF (0.025% w/w) for 8-12 weeks had an increased number of β-adrenoceptors, as determined by [3H]dihydroalprenolol binding to whole cells and [125I]iodocyanopindolol binding to washed particles. For both ligands the number of binding sites was about 4-fold higher in hepatocytes from 2-AAF-treated rats than in those from controls. The adenylate cyclase activity of the carcinogen-fed animals showed both a general increase manifested in the basal level (2-fold) and in the activities obtained by stimulation with guanine nucleotides (2-3-fold), cholera toxin (1.5-fold), and glucagon (1.3-fold) and a selective, larger increase in the β-adrenoceptor-linked ...
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. To examine the mechanism of this effect, metabolic assays were conducted on cultured rat cardiac myocytes incubated in the presence and absence of supernatants harvested from rat activated splenocyte cultures. Intracellular cAMP accumulation in response to isoproterenol was inhibited by up to 74% in a dose-dependent fashion by conditioned media containing soluble cytokines from activated immune cells. By use of myocyte cultures in which contaminating nonmyocyte proliferation was inhibited by nonlethal irradiation, this phenomenon was shown to be independent of mitogenic effects. Isobutylmethylxanthine, a phosphodiesterase inhibitor, did not ablate cytokine-induced inhibition of cAMP accumulation. Parameters of beta-adrenergic receptor binding and affinity were also unaffected. cAMP ...
Long-term administration of imipramine caused a decrease in serotonin2 receptor binding in rat brain cerebral cortex, an effect that was abolished by ovariectomy. In contrast, ovariectomy had no effect on imipramine-induced decreases in hippocampal serotonin or in cerebral cortical and hippocampal beta-adrenergic receptor binding. Administration of estradiol or progesterone separately or in combination reestablished the effect of imipramine treatment on cortical serotonin2 receptors. These results suggest that ovarian steroids may play an important, but subtle, role in the neurochemical and perhaps clinical response to this drug. ...
The effects of various adrenergic beta receptor agonists and antagonists on lipolysis (measured as glycerol release) in human adipose tissue in vitro were studied. Of the agonists investigated, the potency rank order was isoproteronol greater than norepinephrine greater than salbutamol. Adrenergic beta receptor blocking drugs inhibited catecholamineinduced lipolysis competitively. Propranolol was the overall most effective compound, followed by metoprolol, alprenolol and practolol, whereas butoxamine and H35/25 were weak inhibitors. The results indicate that the adrenergic reciptor mediating lipolysis in human adipose tissue is of type beta-1. Basal and theophylline-induced lipolysis was reduced when higher concentrations of these drug were used. ...
The structure-activity relationships were determined for adrenergic compounds which either activated or blocked the activation of a partially purified adenyl cyclase isolated from frog erythrocytes. The results suggested that the presence of a β-hydroxyl group was essential for activity and that the potency of agonists as well as antagonists increased with the size of the substituent group of the amino nitrogen. In addition to the requirements for receptor affinity, compounds with intrinsic activity (agonists) had to have either OH or CH2OH substituents in both the m- and p-positions of the benzene ring. Since these structural requirements agreed well with those reported for intact tissue preparations, utilization of this relatively simple, cell-free preparation of adenyl cyclase may be a useful method for studying compounds with beta-adrenengic activity and for further defining the chemical nature of a beta-adrenergic receptor.. ...
The effects of dietary fats consisting of different fatty acids on lipolytic activity and body fat accumulation were studied in rats. Sprague-Dawley male rats were meal-fed an isoenergetic diet based on either beef tallow or safflower oil for 8 weeks. Lipolytic activities in epididymal and subcutaneous adipose tissues were lower in the beef tallow diet group than in the safflower oil diet group. Body fat accumulation was greater in rats fed the beef tallow diet versus the safflower oil diet. Norepinephrine (NE) turnover rates used as an index of sympathetic activities in adipose tissues were lower in the beef tallow diet group. beta-Adrenergic receptor binding was determined with [3H]dihydroalprenolol. Binding affinities of beta-receptors in adipose tissues were significantly lower in the beef tallow diet group. Membrane fluidities of adipose tissues were also lower in the beef tallow diet group. Membrane fluidities were correlated with the affinities of the beta-receptor. We believe from these ...
The effects of dietary fats consisting of different fatty acids on lipolytic activity and body fat accumulation were studied in rats. Sprague-Dawley male rats were meal-fed an isoenergetic diet based on either beef tallow or safflower oil for 8 weeks. Lipolytic activities in epididymal and subcutaneous adipose tissues were lower in the beef tallow diet group than in the safflower oil diet group. Body fat accumulation was greater in rats fed the beef tallow diet versus the safflower oil diet. Norepinephrine (NE) turnover rates used as an index of sympathetic activities in adipose tissues were lower in the beef tallow diet group. beta-Adrenergic receptor binding was determined with [3H]dihydroalprenolol. Binding affinities of beta-receptors in adipose tissues were significantly lower in the beef tallow diet group. Membrane fluidities of adipose tissues were also lower in the beef tallow diet group. Membrane fluidities were correlated with the affinities of the beta-receptor. We believe from these ...
Glomerular filtration rate and renal plasma flow in patients with essential hypertension before and after tratment with alprenolol. ...
Chlordimeform (N(4-chloro-o-tolyl)-N, N-dimethylformamidine; CDM) is a formamidine insecticide/acaricide whose major active metabolite is its N-monomethyl analog, desmethylchlordimeform, (DCDM). While their pesticidal action in invertebrates appears to be related to activation of octopamine receptors, their mechanism of action in mammals has not been established. Because of similarities between octopamine and adrenergic receptors and suggestions of CDM and DCDM action on adrenoceptors, the in vitro interactions of CDM and DCDM with adrenoceptors were studied. In mouse brain membrane preparations CDM inhibited the binding of [3H]-clonidine to alpha2- adrenoceptors and of [3H]-WB4101 to alpha1-adrenoceptors with IC50 values of 18.2 and 87 μM, respectively. DCDM was a much more potent inhibitor, with IC50 values toward alpha2−, and alpha1-adrenoceptors of 44 nM and 1 μM, respectively. Both compounds were only weak inhibitors of the binding of [3H]-dihydroalprenolol to beta-adrenoceptors and of [3H]
Synonyms for beta-adrenergic blocking agent in Free Thesaurus. Antonyms for beta-adrenergic blocking agent. 3 synonyms for beta-adrenergic blocking agent: beta blocker, beta-adrenergic blocker, beta-blocking agent. What are synonyms for beta-adrenergic blocking agent?
Combining with epinephrine or norepinephrine to initiate a change in cell activity via activation of a G protein, with pharmacological characteristics of beta-adrenergic receptors; the activity involves transmitting the signal to the Gs alpha subunit of a…
We have recently described the affinity chromatography purification of the turkey erythrocyte beta-adrenergic receptor. The minute amounts obtained initially precluded extensive biochemical characterization. To improve the yield of the receptor, the erythrocyte membranes have been prepared by a new method. This procedure resulted in a 10-fold higher receptor density in comparison with the membrane preparation used previously. The new membranes also contained a catecholamine-sensitive guanine triphosphatase and an adenylate cyclase sensitive to Gpp(NH)p and l-epinephrine. Solubilization by a double digitonin extraction resulted in a preparation containing 4-6 pmoles of 3H-dihydroalprenolol binding sites per mg of membrane protein. A single step of affinity chromatography on alprenolol-sepharose of the soluble digitonin extract resulted in an additional 1,000-fold purification of the receptor. The overall purification factor was 20,000 relative to the binding activity of the crude membrane ...
TY - JOUR. T1 - Skin fibroblast beta-adrenergic receptor function in manie-depressive illness. AU - Berrettini, Wade H.. AU - Bardakjian, Josiane. AU - Cappellari, Charles B.. AU - Barnett, Arthur L.. AU - Albright, Allen. AU - Nurnberger, John I.. AU - Gershon, Elliot S.. PY - 1987/12. Y1 - 1987/12. N2 - Beta-adrenergic receptor function was assessed in cultured skin fibroblasts obtained from bipolar patients and normal volunteers by measurement of the cyclic adenosine monophosphate (cAMP) response to isoproterenol. No group differences were observed. To assess regulation of receptor desensitization, fibroblasts were incubated for 24 hr with isoproterenol, and then the cAMP response to isoproterenol was determined. Subsensitivity to rechallenge with isoproterenol did not distinguish bipolar patients from controls.. AB - Beta-adrenergic receptor function was assessed in cultured skin fibroblasts obtained from bipolar patients and normal volunteers by measurement of the cyclic adenosine ...
Desipramine-yohimbine combination treatment of refractory depression. Implications for the beta-adrenergic receptor hypothesis of antidepressant action ...
RecName: Full=Adenylate cyclase type 6; EC=4.6.1.1;AltName: Full=Adenylate cyclase type VI;AltName: Full=ATP pyrophosphate-lyase 6;AltName: Full=Adenylyl cyclase 6;AltName: Full=Ca(2+)-inhibitable adenylyl ...
RecName: Full=Adenylate cyclase type 2; EC=4.6.1.1;AltName: Full=Adenylate cyclase type II;AltName: Full=ATP pyrophosphate-lyase 2;AltName: Full=Adenylyl cyclase ...
Timolol is a nonselective beta-adrenergic antagonist given in an eye drop solution to reduce intraocular pressure, or buy cialis - http://ci
TY - JOUR. T1 - Multiple forms of brain adenylate cyclase. T2 - Stimulation by Mn2+. AU - Malamuda, Daniel F.. AU - DiRusso, Concetta C.. AU - Aprille, June R.. PY - 1977/11/23. Y1 - 1977/11/23. N2 - Mn2+-stimulated adenylate cyclase (ATP pyrophosphate-lyase-(cyclizing), EC 4.6.1.1) activity in detergent solubilized preparations from mouse brain. While NaF-stimulated activity was decreased by both solubilization and storage at 0-4°C, the ability of the enzyme to be stimulated by Mn2+ was maintained for up to one week. By including Mn+ in the assay of adenylate cyclase in gel fractions after isoelectric focusing, two distinct peaks of enzyme activity (pI1 = 5.8, pI2 = 6.4) were detected, suggesting the existence of more than one type of catalytic subunit in mouse brain cell membranes.. AB - Mn2+-stimulated adenylate cyclase (ATP pyrophosphate-lyase-(cyclizing), EC 4.6.1.1) activity in detergent solubilized preparations from mouse brain. While NaF-stimulated activity was decreased by both ...
RECONSTITUTION OF BETA-ADRENERGIC RECEPTORS INTO LIPID VESICLES - AFFINITY-CHROMATOGRAPHY PURIFIED RECEPTORS CONVEY CATECHOLAMINE RESPONSIVENESS TO A HETEROLOGOUS ADENYLATE-CYCLASE SYSTEM
A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor ...
Cardivas is a brand name for Carvedilol, which is a vasodilating non-selective beta-blocking agent with antioxidant properties. Carvedilol reduces the peripheral vascular resistance through...
Adrenergic beta-blocking agents were given to 7 patients with advanced congestive cardiomyopathy who had tachycardia at rest (98 plus or minus 13 beats/min). The patients were on beta-adrenergic receptor blockade for 2 to 12 months (average 5-4 months). One patient was given alprenolol 50 mg twice daily and the other patients were given practolol 50 to 400 mg twice daily. Virus infection had occurred in 6 of the patients before the onset of symptoms of cardiac disease. All patients were in a steady state or were progressively deteriorating at the start of beta-adrenergic receptor blockade. Conventional treatment with digitalis and diuretics was unaltered or reduced during treatment with beta-blocking agents. An improvement was seen in their clinical condition shortly after administration of the drugs. Continued treatment resulted in an increase in physical working capacity and a reduction of heart size. Noninvasive investigations including phonocardiogram, carotid pulse curve, apex cardiogram, ...
It is a prodrug to alprenolol. Prokai L, Wu WM, Somogyi G, Bodor N (May 1995). "Ocular delivery of the beta-adrenergic ... antagonist alprenolol by sequential bioactivation of its methoxime analogue". Journal of Medicinal Chemistry. 38 (11): 2018-20 ...
... alprenolol binding". The Journal of Clinical Investigation. 57 (1): 149-155. doi:10.1172/JCI108254. PMC 436634. PMID 1245597. ...
When the extra hydrogen atoms are tritium, it is a radiolabeled form of alprenolol, which is used to label beta-adrenergic ... Dihydroalprenolol (DHA) is a hydrogenated alprenolol derivative that acts as a beta-adrenergic blocker. ...
... alprenolol (INN) alprostadil (INN) alrestatin (INN) Alrex alsactide (INN) Altace (Pfizer/Sanofi-Aventis) Altamist altanserin ( ...
The molecular formula C15H23NO2 (molar mass : 249.34 g/mol) may refer to: Alprenolol Castoramine, an alkaloid found in ...
Solabegron Terbutaline Tretoquinol Tulobuterol Xamoterol Zilpaterol Zinterol Acebutolol Adaprolol Adimolol Afurolol Alprenolol ...
Beta blockers Non-selective agents Alprenolol Bucindolol Carteolol Carvedilol (has additional α-blocking activity) Labetalol ( ...
ERK1/2 preferring agonist Alprenolol AV-965 Binospirone (postsynaptic 5-HT1A) BMY-7,378 Cannabigerol Cyanopindolol ...
C07AA01 Alprenolol C07AA02 Oxprenolol C07AA03 Pindolol C07AA05 Propranolol C07AA06 Timolol C07AA07 Sotalol C07AA12 Nadolol ...
The molecular formula C15H22N2O2 may refer to: Alprenoxime, a beta blocker and prodrug to alprenolol Mepindolol, a non- ...
Hickie JB (1970). "Alprenolol ("aptin") in angina pectoris. A double-blind multicentre trial". Med. J. Aust. 2 (6): 268-72. doi ... Alprenolol, or alfeprol, alpheprol, and alprenololum (Gubernal, Regletin, Yobir, Apllobal, Aptine, Aptol Duriles), is a non- ...
Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ...
... is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker[1][2] . ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor.[3][4] The compound was developed by Imperial Chemical Industries, which was acquired by AkzoNobel in 2008. ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β2 adrenergic receptor, as few other specific antagonists for this receptor are known.[5] ICI-118,551 has been used in pre-clinical studies using murine models.[6][7][8] When dissolved in saline, the compound crosses the blood-brain barrier. Common systemic doses used in rodent research are 0.5 or 1 mg/kg although efficacy has been demonstrated at doses as low as 0.0001 mg/kg in rhesus monkeys.[9] Doses up to 20 mg/kg have been used without toxicity. At room temperature in saline, the ICI 118,551 hydrochloride is soluble to ...
There are a variety of clinically useful ergoline derivatives for the purpose of vasoconstriction, the treatment of migraines, and treatment of Parkinson's disease. Ergoline alkaloids found their place in pharmacology long before modern medicine as preparations of ergot were often used by midwives in the 12th century to stimulate childbirth.[10] Following Arthur Stoll's isolation of ergometrine, the therapeutic use of ergoline derivatives became well explored. The induction of uterine contractions via the preparation of ergot was attributed to ergonovine, an ergoline derivative found in ergot, which is a powerful oxytocic. From this, methergine, a synthetic derivative, was elucidated.[7] While used to facilitate child birth, ergoline derivatives can pass into breast milk and should not be used during breastfeeding.[11] They are uterine contractors that can increase the risk of miscarriage during pregnancy.[3] Another example of medically relevant ergoline alkaloids is ergotamine, an alkaloid ...
The most common side effect is eye irritation felt as stinging or burning, which occurs in up to a third of patients. Blepharoconjunctivitis occurs in up to 5% of patients. Rarer adverse effects include keratitis, edema and increased lacrimation.[2][3] Allergies are rare, but seem to be more common than under the related drug timolol.[1] If the substance reaches the nasal mucosa via the tear duct, it can be absorbed into the bloodstream and cause systemic side effects. These include orthostatic hypotension (low blood pressure) and other effects on the heart and circulatory system, breathing problems in people with asthma, and skin symptoms such as itching and aggravation of psoriasis.[1] ...
InChI=1S/C23H40N2O4/c1-5-6-7-8-9-10-11-23(27)25-15-19-12-13-21(22(14-19)28-4)29-17-20(26)16-24-18(2)3/h12-14,18,20,24,26H,5-11,15-17H2,1-4H3,(H,25,27 ...
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... (INN) is a drug which is used in scientific research. It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor.[1][2] Idazoxan has been under investigation as an antidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment in schizophrenia. Due to its alpha-2 receptor antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area thought to be involved in the pathogenesis of schizophrenia. ...
... , also known as eformoterol, is a long-acting β2 agonist (LABA) used as a bronchodilator in the management of asthma and chronic obstructive pulmonary disease (COPD). Formoterol has an extended duration of action (up to 12 h) compared to short-acting β2 agonists such as salbutamol (albuterol), which are effective for 4 h to 6 h. LABAs such as formoterol are used as "symptom controllers" to supplement prophylactic corticosteroid therapy. A "reliever" short-acting β2 agonist (e.g., salbutamol) is still required, since LABAs are not recommended for the treatment of acute asthma. It was patented in 1972 and came into medical use in 1998.[2] It is also marketed in the combination formulations budesonide/formoterol and mometasone/formoterol. ...
Since silodosin has high affinity for the α1A adrenergic receptor, it causes practically no orthostatic hypotension (in contrast to other α1 blockers). On the other side, the high selectivity seems to be the cause of silodosin's typical side effect of loss of seminal emission.[3] As α1A adrenoceptor antagonists are being investigated as a means to male birth control due to their ability to inhibit ejaculation but not orgasm, a trial with 15 male volunteers was conducted. While silodosin was completely efficacious in preventing the release of semen in all subjects, 12 out of the 15 patients reported mild discomfort upon orgasm. The men also reported the psychosexual side effect of being strongly dissatisfied by their lack of ejaculation.[4] ...
... (MDPPP) is a stimulant designer drug. It was sold in Germany in the late 1990s and early 2000s as an ingredient in imitation ecstasy (MDMA) pills.[1] It shares a similar chemical structure with α-PPP and MDPV,[2][3][4] and has been shown to have reinforcing effects in rats.[5] ...
... (marketed as Hytrin or Zayasel) is a selective alpha-1 antagonist used for treatment of symptoms of an enlarged prostate (BPH). It also acts to lower the blood pressure, and is therefore a drug of choice for men with hypertension and prostate enlargement. It is available in 1 mg, 2 mg, 5 mg or 10 mg doses.[1] It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls. Most common side effects include dizziness, drowsiness, headache, constipation, loss of appetite, fatigue, nasal congestion or dry eyes, but they generally go away after only a few days of use. Therapy should always be started with a low dose to avoid first dose phenomenon.[2] Sexual side effects are rare, but may include priapism or erectile dysfunction. ...
... eye drops may cause blurred vision, eye irritation and dilated pupils.[6] Tetryzoline is not suitable for prolonged use as its vasoconstrictive effects within the eye eventually decrease or stop. When body is accustomed to tetryzoline, ceasing its use may cause redness of the eyes.[7] Intranasal use of tetryzoline may cause transient burning, stinging, or dryness of the mucosa and sneezing. Prolonged intranasal use often causes opposite effects in the form of rebound congestion with effects such as chronic redness, swelling and rhinitis. Prolonged use thus may result in overuse of the drug.[6] Overdose most often causes slow heart rate. Respiratory depression, low blood pressure, constricted pupils, hypothermia, brief episodes of high blood pressure,[8] drowsiness, headaches and vomiting may also occur.[9] In serious cases some of these effects may result in circulatory shock.[6] Most often overdoses occur in children who have ingested the drug.[8] There is no antidote for ...
InChI=1S/C19H26N2O4S/c1-19(2,12-14-7-5-4-6-8-14)20-13-18(23)15-9-10-17(22)16(11-15)21-26(3,24)25/h4-11,18,20-23H,12-13H2,1-3H3 ...
The drug works by stimulating adrenergic receptors on the lamina propria of blood vessels in the nose. The decongestant effect is due to constriction of large veins in the nose which swell up during the inflammation of any infection or allergy of the nose. The smaller arteries are also constricted and this causes the colour of the nasal epithelium to be visibly paler after dosage. Xylometazoline is an imidazole derivative which is designed to mimic the molecular shape of adrenaline. It binds to α1 and α2 adrenergic receptors[8] in the nasal mucosa. Due to its sympathomimetic effects, it should not be used by people with high blood pressure, or other heart problems. Extended usage of xylometazoline can result in decreased effectiveness or a buildup of tolerance against the drug.[9] The number of receptors decreases, and when the administration of the drug is ceased, chronic congestion can occur; this is called rhinitis medicamentosa, commonly referred to as rebound congestion. Moreover, ...
Ipratropium/salbutamol, sold under the brand name Combivent among others, is a combination medication used to treat chronic obstructive pulmonary disease (COPD).[2][3] It contains ipratropium (an anticholinergic) and salbutamol (albuterol, a β2-adrenergic agonist).[2] It is taken by inhalation.[4] Common side effects include sore throat, muscle cramps, and nausea.[2] Other side effects may include bronchospasm, allergic reactions, and upper respiratory tract infections.[2] Safety in pregnancy is unclear.[1] Each medication typically decreases bronchospasm and does so via different mechanisms.[2] The combination was approved for medical use in the United States in 1996.[4] It is available as a generic medication.[3] Sixty doses in the United Kingdom costs the NHS about 18 £ as of 2019.[3] In the United States the wholesale cost of this amount is about US$9.50.[5] In 2016 it was the 166th most prescribed medication in the United States with more than 3 million prescriptions.[6] ...
... means "related to catecholamines". The catecholamine neurotransmitters include dopamine, epinephrine (adrenaline), and norepinephrine (noradrenaline). A catecholaminergic agent (or drug) is a chemical which functions to directly modulate the catecholamine systems in the body or brain. Examples include adrenergics and dopaminergics. ...
Haddad, S; Poulin, P; Funk, C (2010). "Extrapolating in vitro metabolic interactions to isolated perfused liver: Predictions of metabolic interactions between R-bufuralol, bunitrolol, and debrisoquine". Journal of Pharmaceutical Sciences. 99 (10): 4406-26. doi:10.1002/jps.22136. PMID 20310018 ...
... is an intermediate-acting[citation needed] β2 adrenoreceptor agonist used for the treatment of asthma. It has never been filed for FDA evaluation in the United States, where it is not marketed. The drug is readily oxidized in the presence of moisture and air, making it unsuitable for therapeutic use by inhalation.[1] Pharmaceutical company Parke-Davis/Warner-Lambert researched a stabilizer to prevent oxidation, but an effective one was never developed.[1] It was patented in 1974 and came into medical use in 1980.[2] ...
Adverse drug reactions associated with the use of beta blockers include: nausea, diarrhea, bronchospasm, dyspnea, cold extremities, exacerbation of Raynaud's syndrome, bradycardia, hypotension, heart failure, heart block, fatigue, dizziness, alopecia (hair loss), abnormal vision, hallucinations, insomnia, nightmares, sexual dysfunction, erectile dysfunction and/or alteration of glucose and lipid metabolism. Mixed α1/β-antagonist therapy is also commonly associated with orthostatic hypotension. Carvedilol therapy is commonly associated with edema.[44] Due to the high penetration across the blood-brain barrier, lipophilic beta blockers, such as propranolol and metoprolol, are more likely than other less lipophilic beta blockers to cause sleep disturbances, such as insomnia, vivid dreams and nightmares.[45] Adverse effects associated with β2-adrenergic receptor antagonist activity (bronchospasm, peripheral vasoconstriction, alteration of glucose and lipid metabolism) are less common with ...
Hickie JB (1970). "Alprenolol ("aptin") in angina pectoris. A double-blind multicentre trial". Med. J. Aust. 2 (6): 268-72. doi ... Alprenolol, or alfeprol, alpheprol, and alprenololum (Gubernal, Regletin, Yobir, Apllobal, Aptine, Aptol Duriles), is a non- ...
β-Blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivation. Il-Man Kim, Douglas G. Tilley, Juhsien ... β-Blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivation. Il-Man Kim, Douglas G. Tilley, Juhsien ... β-Blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivation. Il-Man Kim, Douglas G. Tilley, Juhsien ... β-Blockers alprenolol and carvedilol stimulate β-arrestin-mediated EGFR transactivation Message Subject (Your Name) has sent ...
Alprenolol: Search drug information, interaction, images & medical diagnosis. The most comprehensive database of medicines ... Disclaimer: This information is independently developed by MIMS based on Alprenolol from various references and is provided for ... Buckingham R (ed). Alprenolol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www. ...
alprenolol ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs. ...
Alprenolol on Lux 5µm Cellulose-1 by SFC. Column used: Lux® 5 µm Cellulose-1, LC Column 250 x 4.6 mm, Ea Part#: 00G-4459-E0 ...
Monoamine metabolites in cerebrospinal fluid during treatment with clonidine or alprenolol ... Patients on alprenolol showed no change in the levels of these metabolites in CSF. .StripeElement { box-sizing: border-box; ... Monoamine metabolites in cerebrospinal fluid during treatment with clonidine or alprenolol. Monoamine metabolites in ... were measured before and during the administration of clonidine or alprenolol to hypertensive patients. The noradrenaline ...
Alprenolol. Binding Sites. Epinephrine. Humans. Isoproterenol. Lymphocytes. Norepinephrine. Propranolol. Receptors, Adrenergic ... 3H] alprenolol binding to human mononuclear leukocyte preparations was almost entirely accounted for by binding to small ... Binding of (-) [3H] alprenolol to these sites demonstrated the kinetics, affinity, and stereospecificity expected of binding to ... Identification of beta-adrenergic receptors in human lymphocytes by (-) (3H) alprenolol binding. ...
Literature References: b-Adrenergic blocker. Prepn: Brandstrom et al., Acta Pharm. Suec. 3, 303 (1966); NL 6605692 (1966 to AB Hassle), C.A. 66, 46214p (1967); NL 6612958 (1967 to ICI), C.A. 67, 99851w (1967). Pharmacology: Marmo, Clin. Ter. 56, 121-176 (1971). Series of articles on clinical effect in myocardial infarction: Acta Med. Scand. 1984, Suppl. 680, 1-64. ...
... alprenolol should be greatly taken at least two hours before or four hours shortly after trans - 2 - phenylcyclopropylamine. ... If concurrent antibiotic use can when not be avoided, alprenolol should be greatly taken at least two hours before or four ... lornoxicam hcl is requiring something I have gradually tried instead of alprenolol a silent couple of times, I generally prefer ...
Alprenolol is an antagonist for ß1 and ß2 adrenergic receptors. This biotin-alprenolol conjugate is first designed and ... Alprenolol is derivatized with a cysteamine linkage first at a position that is known to not interfere with the receptor ... Click the button below to add the Biotin-Alprenolol Conjugate to your wish list. ...
Both (+) and (±)-alprenolol (5 x 10 -6 and 10 -5 mol.litre -1) decreased action potential amplitude and V̇max in Purkinje ... Electrophysiological effects of alprenolol on depressed canine myocardium. Paul A. Guse, Marion S. Gaide, Robert J. Myerburg, ... Electrophysiological effects of alprenolol on depressed canine myocardium. / Guse, Paul A.; Gaide, Marion S.; Myerburg, Robert ... Both (+) and (±)-alprenolol (5 x 10 -6 and 10 -5 mol.litre -1) decreased action potential amplitude and {\.V}max in Purkinje ...
Alprenolol Pharmacology. Alprenolol impairs the conduction of AV node and decreases the rate of sinus. It may also be capable ... Alprenolol is a non-selective beta (β)-locker and a 5-HT1A receptor antagonist. This drug is used for treating angina pectoris- ... Alprenolol IUPAC Name. The IUPAC (The International Union of Pure and Applied Chemistry) name for this drug is 1- (propan-2- ... Alprenolol Uses. This drug can cause selective β1-adrenoceptor blockade as it functions as a partial agonist. The pharmacology ...
Alprenolol treatment of angina pectoris. JAMA : the Journal of the American Medical Association ... Effect of beta adrenergic blocking agents (alprenolol and propranolol) in essential hypertension. (opens in new tab) ...
Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist. - Mechanism of Action & ... Alprenolol hydrochloride (Synonyms: (RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochloride). Cat. No.: HY-B1517A Purity: ... Alprenolol(RS)-Alprenololdl-Alprenolol5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit ... Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist. The reference for ...
... filtration rate and renal plasma flow in patients with essential hypertension before and after tratment with alprenolol.. ...
Alprenolol on Lux 5µm Cellulose-4 in NP. Column used: Lux® 5 µm Cellulose-4, LC Column 250 x 4.6 mm, Ea Part#: 00G-4491-E0 ...
This indicates induction of the first-pass extraction of alprenolol in man. ... but there was no change in the plasma half-life of alprenolol. ... range in steady-state plasma concentrations on oral alprenolol ... Combined pharmacokinetic and pharmacodynamic studies on alprenolol and 4-hydroxy-alprenolol in man.. *B Ablad. , K O Borg. , G ... Steady-state plasma concentrations of alprenolol in man. *M. D. Rawlins. , P. Collste. , Marianne Frisk-Holmberg. , Margareta ...
alcohol secundario (es); 第2級アルコール (ja); Alcool secondaire (fr); alkohol drugorzędowy (pl); вторичный спирт (ru); 仲醇 (lzh); 이차 알코올 (ko); secondary alcohol (en); sekundara alkoholo (eo); sekundární alkohol (cs); 仲醇 (zh) każdy alkohol, w którym grupa hydroksylowa przyłączona jest do drugorzędowego atomu węgla (pl) вторичные спирты (ru); Alcool Secondaire (fr); 2차 알코올 (ko); secondary alcohols (en); alkohole drugorzędowe (pl ...
beta bloqueador (es); Béta receptor blokkolók (hu); betablokeatzaile (eu); Beta blocker (ms); Betablocker (de); Beta blocker (pam); بلوک کننده بتا (fa); Β受体阻断药 (zh); Dagirên bêta-wergirên adrênalînê (ku); Beta-blocant (ro); 交感神経β受容体遮断薬 (ja); betablockerare (sv); Бета-блокатор (uk); Dagirên bêta-wergirên adrênalînê (ku-latn); Beetasalpaaja (fi); Beta-blokátor (cs); Beta blokator (bs); Betabloccanti (it); বিটা ব্লকার (bn); bêta-bloquant (fr); Beetablokaatorid (et); 베타 차단제 (ko); חוסמי בטא (he); blocador dadrenoreceptors beta (ca); Бета блокатор (mk); Beta blokator (sr-el); Бета блокатор (sr-ec); Bēta adrenoblokatori (lv); bloqueador beta-adrenérgico (pt); бета блокатор (sr); Бета-адреноблокаторы (ru); Beta-blokker (da); Bètablokker (nl); Leki beta-adrenolityczne (pl); Beta blocker (id); betablokkar (nn); betablokker (nb); Beta ...
Phenoxybenzamine may cause some people to become dizzy, drowsy, or less alert than they are normally. This is more likely to happen when you begin to take it or when you increase the amount of medicine you are taking. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy or not alert.. Dizziness, lightheadedness, or fainting may occur, especially when you get up from a lying or sitting position. Getting up slowly may help, but if the problem continues or gets worse, check with your doctor.. The dizziness, lightheadedness, or fainting is also more likely to occur if you drink alcohol, stand for a long time, exercise, or if the weather is hot. While you are taking this medicine, be careful in the amount of alcohol you drink. Also, use extra care during exercise or hot weather or if you must stand for a long time.. Before having any kind of surgery (including dental surgery) or emergency treatment, tell the ...
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are receiving this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.. Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.. ...
Detailed drug Information for Uroxatral. Includes common brand names, drug descriptions, warnings, side effects and dosing information.
Os betablocantes são as medicamentações que são usadas principalmente para tratar várias condições de coração, geralmente diminuindo a actividade do coração
Alprenolol (major, theoretical). *Amiodarone (contraindicated, theoretical). *Amitriptyline (major, theoretical). *Amoxapine ( ...
Hay algo de evidencia de que los bloqueadores beta (específicamente el propanolol, metoprolol y alprenolol) podrían dañar la ...
For antagonists, the rank order is yohimbine , chlorpromazine , phentolamine , mianserine , spiperone , prazosin , alprenolol ...
F → N: 350-fold reduced affinity for alpha-2 antagonist yohimbine, 3000-fold increase for beta-antagonist alprenolol. 1 ... alprenolol = pindolol.1 Publication. ,p>Manually curated information for which there is published experimental evidence.,/p> ,p ...
Antagonist: alprenolol (Sigma) Hoechst™ 33342 (Molecular Probes) Poly-D-lysine, 5 mg (Sigma) 96-well assay plate (Greiner Bio- ... alprenolol, each diluted in 0.01% DMSO. DMSO at ≤1% was demonstrated to have no detectable adverse effect on the cells or the ...
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  • En un estudio, los suplementos de CoQ 10 redujeron los efectos secundarios causados por el bloqueador beta propranolol. (empowher.com)
  • Promega synthesized alprenolol-TAMRA and CellAura provided propranolol-BY630. (news-medical.net)
  • Cardiosseletivos Nao seletivos Drogas com atividade al antagonista adicional Acebutolol * Alprenolol * Bucindolol Atenolol Carteolol * Carvedilol Betaxolol Nadolol Labetalol Bevantolol Oxprenolol * Bisoprolol Penbutolol * Celiprolol Pindolol * Esmolol Propranolol Metoprolol Sotalol Practolol * Timolol Quadro 4: Criterios usados na selecao e forma de obtencao dos dados. (thefreedictionary.com)
  • To identify directly and to quantitate these beta-adenergic receptors in human lymphocytes, (-) [3H] alprenolol, a potent beta-adrenergic antagonist, was used to label binding sites in homogenates of human mononuclear leukocytes. (duke.edu)
  • Alprenolol is an antagonist for ß1 and ß2 adrenergic receptors. (cellmosaic.com)
  • The electrophysiological effects of the β-adrenergic antagonist, alprenolol, were compared in normal and depressed canine myocardium. (elsevier.com)
  • Alprenolol is a non-selective beta (β)-locker and a 5-HT 1A receptor antagonist. (chemistrylearner.com)
  • Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist. (medchemexpress.com)
  • Twelve replicate wells contained a known agonist, isoproterenol, and four replicate wells contai ned a known antagonist, alprenolol, each diluted in 0.01% DMSO. (bio-medicine.org)
  • A) TEVC recordings showing antagonist effect of 5 µM alprenolol during addition of 0.5 µM isoproterenol on β2-K0-25, β2-K-62-25 and β2-K-72-25. (xenbase.org)
  • Here we show that only alprenolol (Alp) and carvedilol (Car) induce β 1 AR-mediated transactivation of the EGFR and downstream ERK activation. (pnas.org)
  • B) Change in whole-cell currents evoked by isoproterenol before and after addition of 5 µM alprenolol. (xenbase.org)
  • Similar depressant actions were noted in Purkinje fibres depolarised by exposure to 9 mmol.litre -1 K + . Depolarised and diseased myocardium is more sensitive to alprenolol and the drug's membrane depressant actions may be significant in terminating arrhythmias in such tissue. (elsevier.com)
  • Alprenolol has very low intrinsic sympathomimetic activity as well as little direct myocardial depressant activity. (chemistrylearner.com)
  • Glomerular filtration rate and renal plasma flow in patients with essential hypertension before and after tratment with alprenolol. (au.dk)
  • Disclaimer: This information is independently developed by MIMS based on Alprenolol from various references and is provided for your reference only. (mims.com)
  • Binding was rapid (t1/2 less than 30 s) and rapidly reversible (t1/2 less than 3 min) at 37 degrees C. Binding was a saturable process with 75 +/- 12 fmol (-) [3H] alprenolol bound/mg protein (mean +/- SEM) at saturation, corresponding to about 2,000 sites/cell. (duke.edu)
  • Half-maximal saturation occurred at 10 nM (-) [3H] alprenolol, which provides an estimate of the dissociation constant of (-) [3H] alprenolol for the beta-adrenergic receptor. (duke.edu)
  • The saturation binding experiments with alprenolol-TAMRA were then performed by adding serially diluted alprenolol-TAMRA to the wells, with or without 10μM alprenolol, and incubating the plate at room temperature for 120 minutes. (news-medical.net)
  • The saturation binding experiments with alprenolol- TAMRA were performed by operating the CLARIOstar plate reader in endpoint mode. (news-medical.net)
  • Lumbar cerebrospinal fluid (CSF) concentrations of the major metabolites of noradrenaline (4-hydroxy-3-methoxyphenyl glycol, HMPG), serotonin (5-hydroxyindoleacetic acid) and dopamine (homovanillic acid) were measured before and during the administration of clonidine or alprenolol to hypertensive patients. (eurekamag.com)
  • Patients on alprenolol showed no change in the levels of these metabolites in CSF. (eurekamag.com)
  • Alprenolol is derivatized with a cysteamine linkage first at a position that is known to not interfere with the receptor binding, then reacts with biotin NHS ester to form the conjugate. (cellmosaic.com)
  • Stereospecific 3 H (-)-alprenolol binding sites, beta-adrenergic receptor and adenylate cyclase. (springer.com)
  • After pentobarbital treatment, the area under the plasma concentration curve of the 200 mg dose was decreased to 32% and 59% of the pretreatment values in two subjects, but there was no change in the plasma half-life of alprenolol. (semanticscholar.org)
  • Seven healthy volunteers showing a fourteenfold range in steady-state plasma concentrations on oral alprenolol (200 mg b.i.d.) were investigated by administration of 5 mg of the drug intravenously and then 50, 100, 150, and 200 mg as single oral doses. (semanticscholar.org)
  • If concurrent antibiotic use can when not be avoided, alprenolol should be greatly taken at least two hours before or four hours shortly after trans - 2 - phenylcyclopropylamine. (aktuelle-kamera.org)
  • Click the button below to add the Biotin-Alprenolol Conjugate to your wish list. (cellmosaic.com)