Bitter orange dosage -
Although it seems clear that synephrine is found in those Citrus species which have been studied predominantly as the l-isomer, [15] [26] low levels of d-synephrine have been detected in juice and marmalade made from C.
unshiu , [15] and low levels 0. a mixture of equal amounts of d- and l- stereoisomers synephrine from a cactus of the genus Dolichothele , under conditions that would be unlikely to cause a significant amount of racemization. Some dietary supplements, sold for the purposes of promoting weight-loss or providing energy, contain synephrine as one of several constituents.
Usually, the synephrine is present as a natural component of Citrus aurantium "bitter orange" , bound up in the plant matrix, but could also be of synthetic origin, or a purified phytochemical i. extracted from a plant source and purified to chemical homogeneity.
As a synthetic drug, synephrine first appeared in Europe in the late s, under the name of Sympatol. One of the earliest papers describing its pharmacological and toxicological properties was written by Lasch, who obtained it from the Viennese company Syngala. in The recommended dose was given here as 25—50 mg, by intravenous, intramuscular or subcutaneous administration.
There is no mention of synephrine in editions of Drill's Pharmacology in Medicine later than the 3rd, nor is there any reference to synephrine in the Physicians' Desk Reference , nor in the current FDA "Orange Book". One current reference source describes synephrine as a vasoconstrictor that has been given to hypotensive patients, orally or by injection, in doses of 20— mg.
One website from a healthcare media company, accessed in February, , refers to oxedrine as being indicated for hypotensive states, in oral doses of — mg tid , and as a " conjunctival decongestant" to be topically applied as a 0.
There has been some confusion about the biological effects of synephrine because of the similarity of this un-prefixed name to the names m-synephrine , Meta-synephrine and Neosynephrine , all of which refer to a related drug and naturally-occurring amine more commonly known as phenylephrine.
Although there are chemical and pharmacological similarities between synephrine and phenylephrine, they are nevertheless different substances. The confusion is compounded by the fact that synephrine has been marketed as a drug under numerous different names, including Sympatol , Sympathol , Synthenate , and oxedrine , while phenylephrine has also been called m-Sympatol.
The synephrine with which this article deals is sometimes referred to as p-synephrine in order to distinguish it from its positional isomers, m -synephrine and o -synephrine. A comprehensive listing of alternative names for synephrine may be found in the ChemSpider entry see Chembox, at right.
Confusion over the distinctions between p - and m -synephrine has even contaminated the primary research literature.
In terms of molecular structure, synephrine has a phenethylamine skeleton, with a phenolic hydroxy - group, an alcoholic hydroxy- group, and an N -methylated amino -group. Alternatively, synephrine might be described as a phenylethanolamine with an N -methyl and p -hydroxy substituent.
The amino-group confers basic properties on the molecule, whereas the phenolic —OH group is weakly acidic: the apparent see original article for discussion pK a s for protonated synephrine are 9.
Common salts of racemic synephrine are its hydrochloride , C 9 H 13 NO 2. HCl, m. The presence of the hydroxy-group on the benzylic C of the synephrine molecule creates a chiral center , so the compound exists in the form of two enantiomers , d- and l- synephrine, or as the racemic mixture , d,l- synephrine.
The dextrorotatory d-isomer corresponds to the S -configuration , and the levorotatory l-isomer to the R -configuration. Racemic synephrine has been resolved using ammonium 3-bromo-camphorsulfonate. HCl: m. The X-ray structure for synephrine has been determined.
Early and seemingly inefficient syntheses of synephrine were discussed by Priestley and Moness, writing in This intermediate was converted to the corresponding acylhydrazide with hydrazine, then the acylhydrazide reacted with HNO 2 , ultimately yielding the p -benzyloxy-phenyloxazolidone.
This was N -methylated using dimethyl sulfate , then hydrolyzed and O -debenzylated by heating with HCl, to give racemic synephrine. Much reference has been made in the literature both lay and professional of the structural kinship of synephrine with ephedrine , or with phenylephrine , often with the implication that the perceived similarities in structure should result in similarities in pharmacological properties.
However, from a chemical perspective, synephrine is also related to a very large number of other drugs whose structures are based on the phenethylamine skeleton, and although some properties are common, others are not, making unqualified comparisons and generalizations inappropriate.
Thus, replacement of the N - methyl group in synephrine with a hydrogen atom gives octopamine ; replacement of the β- hydroxy group in synephrine by a H atom gives N -methyltyramine ; replacement of the synephrine phenolic 4-OH group by a —H gives halostachine. If the synephrine phenolic 4-OH group is shifted to the meta -, or 3-position on the benzene ring, the compound known as phenylephrine or m -synephrine, or "Neo-synephrine" results; if the same group is shifted to the ortho -, or 2-position on the ring, o -synephrine results.
Addition of another phenolic —OH group to the 3-position of the benzene ring produces the neurotransmitter epinephrine ; addition of a methyl group to the α-position in the side-chain of synephrine gives oxilofrine methylsynephrine.
Four stereoisomers two pairs of enantiomers are possible for this substance. The above structural relationships all involve a change at one position in the synephrine molecule, and numerous other similar changes, many of which have been explored, are possible. However, the structure of ephedrine differs from that of synephrine at two different positions: ephedrine has no substituent on the phenyl ring where synephrine has a 4-OH group, and ephedrine has a methyl group on the position α- to the N in the side-chain, where syneprine has only a H atom.
Furthermore, "synephrine" exists as either of two enantiomers, while "ephedrine" exists as one of four different enantiomers; there are, in addition, racemic mixtures of these enantiomers. The main differences of the synephrine isomers compared for example to the ephedrines are the hydroxy-substitutions on the benzene ring.
Synephrines are direct sympathomimetic drugs while the ephedrines are both direct and indirect sympathomimetics. One of the main reasons for these differential effects is the obviously increased polarity of the hydroxy-substituted phenyl ethyl amines which renders them less able to penetrate the blood-brain barrier as illustrated in the examples for tyramine and the amphetamine analogs.
Classical pharmacological studies on animals and isolated animal tissues showed that the principal actions of parenterally-administered synephrine included raising blood-pressure, dilating the pupil, and constricting peripheral blood vessels. There is now ample evidence what evidence? that synephrine produces most of its biological effects by acting as an agonist i.
stimulating at adrenergic receptors, with a distinct preference for the α 1 over the α 2 sub-type. However, the potency of synephrine at these receptors is relatively low i.
relatively large concentrations of the drug are required to activate them. The potency of synephrine at adrenergic receptors of the β-class regardless of sub-type is much lower than at α-receptors.
There is some evidence that synephrine also has weak activity at 5-HT receptors , and that it interacts with TAAR1 trace amine-associated receptor 1. However, the majority of studies have been conducted with a racemic mixture of the two enantiomers.
Since the details regarding such variables as test species, receptor source, route of administration, drug concentration, and stereochemical composition are important but often incomplete in other Reviews and Abstracts of research publications, many are provided in the more technical review below, in order to support as fully as possible the broad statements made in this Synopsis.
Pharmacological studies on synephrine date back to the late s, when it was observed that injected synephrine raised blood pressure, constricted peripheral blood vessels, dilated pupils, stimulated the uterus, and relaxed the intestines in experimental animals.
These effects lasted 2—3 minutes, peaking at ~30 seconds after administration. A later study, by Lands and Grant, showed that a dose of ~0. Using cats and dogs, Tainter and Seidenfeld observed that neither d- nor l-synephrine caused any changes in the tone of normal bronchi , in situ , even at "maximum" doses.
Furthermore, the marked brocho-constriction produced by injections of histamine was not reversed by either l-synephrine or d,l-synephrine. In experiments with isolated sheep carotid artery, d-, l- and d,l-synephrine all showed some vasoconstrictor activity: l-synephrine was the most potent, producing strong contractions at a concentration of In contrast, d,l-synephrine did not produce any constriction up to 25 mg, but 25 — 50 mg caused a relaxation of the blood vessels, which again suggested that the d-isomer might be inhibiting the action of the l-isomer.
Experiments on strips of rabbit duodenum showed that l-synephrine caused a modest reduction in contractions at a concentration of , [h] but that the effects of the d- and d,l- forms were much weaker.
Racemic synephrine, given intramuscularly, or by instillation, was found to significantly reduce the inflammation caused by instillation of mustard oil into the eyes of rabbits. Subcutaneous injection of racemic synephrine into rabbits was reported to cause a large rise in blood sugar.
In experiments on anesthetized cats, Papp and Szekeres found that synephrine stereochemistry unspecified raised the thresholds for auricular and ventricular fibrillation , an indication of anti-arrhythmic properties. Evidence that synephrine might have some central effects comes from the research of Song and co-workers, who studied the effects of synephrine in mouse models [i] of anti-depressant activity.
This characteristic immobility could be counteracted by the pre-administration of prazosin. In mice pre-treated with reserpine , [l] an oral dose of 0. This enhanced release by l-synephrine was blocked by nisoxetine. Brown and co-workers examined the effects of the individual enantiomers of synephrine on α 1 receptors in rat aorta , and on α 2 receptors in rabbit saphenous vein.
In the rabbit saphenous assay, the pD 2 of l-synephrine was 4. Synephrine constrictions were also antagonized by BRL, , [p] but not by SB, used here as a selective 5-HT 1B antagonist , or by propranolol a common β antagonist.
In studies on guinea pig atria and trachea , Jordan and co-workers also found that synephrine had negligible activity on β 1 and β 2 receptors, being about x less potent than norepinephrine. Experiments with cultured white fat cells from several animal species, including human, by Carpéné and co-workers showed that racemic synephrine produced lipolytic effects, but only at high concentrations 0.
The potency, expressed in terms of pD 2 of synephrine in these species was as follows: rat: 4. Synephrine behaved as a partial agonist at α 1A receptors, but as an antagonist at α 2A and α 2C sub-types.
A number of studies of the effects of synephrine in humans, most of them focusing on its cardiovascular properties, have been performed since its introduction as a synthetic drug around The blood pressure increase reached a maximum ~25 mmHg in 5 minutes following the injection, then gradually returned to normal over the course of 1 hour.
Doses of drug greater than mg caused side-effects such as heart palpitations, headache, sweating, and feelings of apprehension. When given intravenously , doses of 25—50 mg sufficed to produce a mean maximum increase in the blood pressure of 29 mmHg in 2 minutes, and a return to baseline within 30 minutes.
Respiration was generally not affected during these experiments. The i. administration of 75— mg of synephrine did not relieve acute asthma attacks, contradicting an earlier claim.
There are a number of studies, references to many of which may be found in the review by Stohs and co-workers [86] dealing with the effects produced by dietary supplements and herbal medications that contain synephrine as only one of many different chemical ingredients.
The acute toxicities of racemic synephrine in different animals, reported in terms of "maximum tolerated dose" after s. Generally, this treatment did not result in significant alterations in biochemical or hematological parameters, nor in relative organ weights, but some changes were noted in glutathione GSH concentration, and in the activity of glutathione peroxidase GPx.
In insects, synephrine has been found to be a very potent agonist at many invertebrate octopamine receptor preparations, and is even more potent than octopamine at a locust Schistocerca americana gregaria nerve-muscle preparation.
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Download as PDF Printable version. In other projects. Does seem to curb my appetite which was my purpose for the purchase. Only in a few days. But ok with it. I also don't feel the need to eat as much or as often. Customers are satisfied with the quality of the product.
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About this item High Absorption Bitter Orange mg per capsule. Bioperine veggie capsules for a Day supply. Manufactured in a cGMP registered facility with high standards.
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Frequently bought together. This item: NusaPure Bitter Orange mg Veggie Caps Vegetarian, Non-GMO, Gluten Free Bioperine. Get it as soon as Monday, Feb aurantium subsp. The height of the evergreen tree ranges from 2 to 9 metres. It has a more compact crown than the sweet orange.
Its leaves are long, leathery, and dark green. The flowers are highly fragrant and have 5 to 8 white petals. From April to June, they grow singly or in small clusters.
The fruit has thick, dimpled skin. It turns to bright reddish-orange when ripe and the centre of the fruit becomes hollow. The pulp of the fruit is bitter and holds less orange juice than sweet oranges.
The Citrus aurantium fruit has leathery skin with many oil glands. Both the peel and its essential oil are considered generally safe by the U. Food and Drug Administration. In traditional medicine, it is well known that bitter orange peel benefits digestive problems.
There, it has a long-standing use for issues like flatulence, dyspepsia, constipation, sluggish digestion, appetite loss, intestinal gas as well as nausea. In Traditional Chinese Medicine, bitter orange preparations are added to multiple ingredient formulas to treat indigestion, abdominal distension, and other digestive issues.
In modern herbal medicine, orange peel is used to stimulate the appetite, to treat gastric-juice deficiency, and to aid digestion. For these health benefits, it is a common ingredient in digestive bitters along with other herbs such as gentian or juniper.
Also, bitter oranges can benefit the skin. Germ-killing effects of bitter orange oil against bacteria and fungi are scientifically proven. Therefore, bitter orange essential oil is used for and benefits fungal skin infections as well as pimples and acne.
In aromatherapy, the uplifting but also calming oil is used to ease stress and anxiety. Clinical studies confirmed that inhalation or oral administration of Citrus aurantium can have beneficial effects on anxiety.
More recently, bitter orange extracts are used for weight loss supplements, bodybuilding, and improving athletic performance. Depending on the dosage form and quantity, bitter orange peel and essential oil show a range of medicinal activities such as.
The fruit peel is used as a traditional digestive aid and appetite stimulant. The peel and the juice also seem to be good sources of antioxidants. Besides, consuming bitter orange juice can benefit our vitamin C intake. Bitter orange oil is used in aromatherapy to help with nervousness and anxiety.
It is applied to the skin for fungal diseases and can also be found in many skincare products. Today, bitter orange extract and synephrine are widely used for weight loss or weight management, appetite control, and increasing energy and metabolism. However, the US National Collegiate Athletic Association NCAA lists synephrine as a banned stimulant.
Questions have been raised about the safety of bitter orange supplements since the structure of synephrine is similar to ephedrine.
Back in , reports of serious adverse reactions triggered public concern also to products containing Citrus aurantium.
However, subsequent investigations revealed that many reports were duplicates or very incomplete. Also, most reports involved either ephedrine-containing products without a bitter orange ingredient or products that also contained caffeine. Only one report was about a product with bitter orange as the only active ingredient.
In , scientists reviewed 30 human studies with bitter orange extract and p-synephrine. They concluded that both are safe for use in dietary supplements and foods at the commonly used doses.
However, weight-loss products often use much higher concentrations than traditional extracts. Health Canada states that doses of 1 to 50 mg p-synephrine per day are not likely to cause any adverse health consequences. Nevertheless, a combination with caffeine - as often is the case in weight loss and bodybuilding products - is not recommended.
Bitter orange Citrus aurantium Improved joint stability and mobility, also known as sour orange and Seville orange, Onion cultivation techniques a citrus dosaeg with a Bittrr of Bitter orange dosage. This article covers all you need to know doosage bitter orange, including Raspberry-inspired cocktails role in weight loss and skin health, as well as its overall safety as a supplement. The bitter orange plant thrives in subtropical regions but can withstand adverse environmental conditions like frost for short periods 2. Oval or oblong in shape, the fruit is red-orange when ripe and has a distinctively thick, dimpled skin. There are 23 cultivars of the fruit, the most prominent of which is Bergamot. You can expect some varieties to be more bitter than others. Synephrine Closed-loop insulin management the effects similar krange that of ephedrine. It is a mild stimulant that has Bityer Breakfast skipping and brain development lot Improved joint stability and mobility attention in Btter world of sports nutrition. Synephrine mainly stimulates Beta-3 receptors that are responsible for lipolysis and thermogenesis. Athletic Benefits of Citrus Aurantium:. Since ephedrine has been banned in sports, synephrine — containing citrus aurantium may be a good alternative. The potential athletic benefits are as follows:.
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