Halostachine, mild sympathomimetic agent

Published: admin | Format: 2017-02-24

Halostachine (N-methylphenylethanolamine), mild sympathomimetic agent that partially binds to adrenergic potential.

Halostachine (also known as N-methylphenylethanolamine) is a natural product of an alkaloid from Asia, a shrub, for the first time isolated from salt-wood (Halostachys), the structure of β-hydroxy-phenylethylamine Phenylethanolamine) related to its more widely known "parent" biogenic amines, phenylethanolamine, epinephrine to epinephrine drugs, and  the alkaloids of ephedrine. The pharmacological properties of methotrexate have some similarity with the structure-related compounds, and the salt-ear wood extract has been listed as a component of some OTC dietary supplements [1] but methotrexate has never been developed as prescription. Although it is found in nature to be a single stereoisomer, methamidol is more commonly used in its formation as a synthetic product of racemates. 

In vitro pharmacodynamic studies and structural activity relationships (SAR) of various epinephrine - like compounds, halostachine have been shown to be 19% efficient in adrenergic - activated beta2 receptors. As a comparison, symplectic proved to be 24% effective. Significantly reduced Halostachine is thought to have the ability to activate intracellular cAMP then all other compounds, including deoxyadrenaline.

 

Weight loss function

Ephedrine alkaloids are members of a large family of dobutamine and amphetamines that include sympathomimetic compounds. The members of this family increase the blood pressure and heart rate bound to the alpha-adrenergic receptor and appear in many parts of the body, including the heart and blood vessels. These compounds are known to be sympathomimetic because they mimic the effects of epinephrine and norepinephrine that the body naturally occurs.

Usually weight-loss drugs like beta-adrenergic receptor agonists of ephedrine and clenbuterol. This stimulus causes fat to be released as a source of energy. A paper that studied the structure of epinephrine and compounds similar to adrenaline indicates that Halostachine is indeed a beta adrenergic receptor agonist with properties similar to adrenaline. In addition, Halostachine was found to be about 19% as effective as adrenaline stimulating camps due to beta-agonism.( Davis, 1983)

Halostachine was first introduced to replenish the market because of their fat burning function. Researchers claim Halostachine works since the burning of fats similar to ephedrine Halostachine has a similar structure and ephedrine.(Yao, 2006)

Infiltration into the central nervous system will also be due to beta-OH limitation, and due to a lack of alpha-CH3 (amphipathism). The most likely effective target molecule alpha receptor, demonstrated in the above studies in dogs. Intravenous injection produces pupillary dilatation (a), tachycardia (beta1), elevated body temperature, and possible stress due to excessive vasoconstriction. This reflex - activated response increases arterial pressure in the absence of beta2 - vasodilatation. In the above pharmacodynamic studies, it has been clearly demonstrated that halostachine has little ability to activate beta2 receptors, and therefore very different ephedrine. Because it is almost incapable of inducing the camp elevation formula to lose weight without purpose, there is no supplement due to its extremely fast metabolism. Likewise, since it is a partial stimulant, it will reduce the epinephrine signal in the presence of endogenous epinephrine, or exogenous ephedrine. ( Liapakis,2004)

All of this evidence suggests that Halostachine HCl is a good plant adrenergic receptor agonist. Get more lean quality and burn fat, Halostachine HCl from Summary Capsica is really a nice gift.

Adrenaline is the main hormone in body fat burning, and beta agitation is a typical and effective way to increase fat. Halostachine may be a good alternative to fat-burning materials like ephedrine, so look for more fat burning products in the future, including this new ingredient as part of a blend.( Liapakis,2004)


Safety:

LD50 mice oral intake 500 mg / kg.

In a study using dogs, intravenous administration of halostachine resulted in an increase in pupil diameter, initial tachycardia followed by bradycardia, and elevated body temperature (2). In another study, oral halostachine produced only a slight effect because of guinea pigs and sheep 100 - 200 mg / kg.(Shannon, 1982)(Aasen, 1969)

 

 Ref:

Aasen A J, Culvenor C C J, Finnie E P, et al. Alkaloids as a possible cause of ryegrass staggers in grazing livestock.[J]. Australian Journal of Agricultural Research, 1969, 20(1):71-86.

Armstrong J, Barlow R B. The ionization of phenolic amines, including apomorphine, dopamine and catecholamines and an assessment of zwitterion constants.[J]. British Journal of Pharmacology, 1976, 57(4):501–516.

Davis C B, Camp B J. The vasoactive potential of halostachine, an alkaloid of tall fescue (Festuca arundinaceae, Schreb) in cattle.[J]. Veterinary & Human Toxicology, 1983, 25(6):408-11.

Durden D A, Juorio A V, Davis B A. Thin-layer chromatographic and high resolution mass spectrometric determination of beta-hydroxyphenylethylamines in tissues as dansyl-acetyl derivatives.[J]. Analytical Chemistry, 1980, 52(12):1815-1820.

Liapakis G, Chan W C, Papadokostaki M, et al. Synergistic contributions of the functional groups of epinephrine to its affinity and efficacy at the beta2 adrenergic receptor.[J]. Molecular Pharmacology, 2004, 65(5):1181-1190.

Lyle G G. Rotatory Dispersion Studies. I. Aralkylamines and Alcohols1[J]. Journal of Organic Chemistry, 2002, 25(10):1779-1784.

R. Lukeš, V. Dienstbierová, J. Kovář, et al. Über die konfiguration stickstoffhaltiger verbindungen XII. Konfiguration des (-)-halostachins[J]. Collection of Czechoslovak Chemical Communications, 1961, 26(2):466-470.

Shannon H E, Cone E J, Yousefnejad D. Physiologic effects and plasma kinetics of beta-phenylethylamine and its N-methyl homolog in the dog.[J]. Journal of Pharmacology & Experimental Therapeutics, 1982, 223(1):379-85.

Yao X, Parnot C, Deupi X, et al. Coupling ligand structure to specific conformational switches in the beta2-adrenoceptor.[J]. Nature Chemical Biology, 2006, 2(8):417-22.






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