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  #1  
Unread 01-30-2017, 01:15 PM
keentoblean keentoblean is offline
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Default Berberine HCL as a possible alpha-2 antagonist

Hello All,

I wish to follow the Stubborn Fat Solution, but in my country (UK) Yohimbine HCL is currently banned.

I know I can import it from the USA, but for various reasons I do not want to attract the attention of UK customs/authorities. Also, because of the need to import, it is quite expensive.

In researching about a blood sugar lowering supplement (Berberine), I came across an interested pubmed abstract. It states that in the presence L-epinephrine (adrenaline), which should be raised by the caffeine & HIIT in the Stubborn Fat Protocol, that Berberine acts as alpha-2 adrenoceptor antagonist, similar to Yohimbine. Does anybody know, if Berberine could be used as a replacement for Yomimbine, even if its effects are weaker?

"Berberine, an alkaloid, has been found to have a myriad of pharmacological effects including hypotensive, antisecretory, sedative, and antimicrobial effects, some of which are similar to those of clonidine, an alpha 2 adrenoceptor partial agonist. The interaction of berberine with human platelet alpha 2 adrenoceptor was investigated in this study. Berberine was found to inhibit competitively the specific binding of [3H]-yohimbine. The displacement curve was parallel to those of clonidine, epinephrine, norepinephrine, with the rank order of potency (IC50) being clonidine (0.4 microM) greater than epinephrine (7.5 microM) greater than norepinephrine (14.5 microM) = berberine (16.6 microM). Increasing concentrations of berberine from 0.1 microM to 10 microM inhibited [3H]-yohimbine binding, shifting the saturation binding curve to the right without decreasing the maximum binding capacity. In platelet cyclic AMP accumulation experiments, berberine at concentrations of 0.1 microM to 0.1 mM inhibited the cAMP accumulation induced by 10 microM prostaglandin E1 in a dose dependent manner, acting as an alpha 2 adrenoceptor agonist. In the presence of L-epinephrine, berberine blocked the inhibitory effect of L-epinephrine behaving as an alpha 2 adrenoceptor antagonist. These properties are similar to those of clonidine on human platelets, suggesting that berberine is a partial agonist of platelet alpha 2 adrenoceptors. These findings may provide potential mechanisms for the hypotensive, antisecretory, and sedative effects of berberine."

https://www.ncbi.nlm.nih.gov/pubmed/1649363
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  #2  
Unread 01-31-2017, 05:24 AM
tellurium's Avatar
tellurium tellurium is offline
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Join Date: Aug 2016
Location: United Kingdom
Posts: 210
Default

Quote:
Originally Posted by keentoblean View Post
Hello All,

I wish to follow the Stubborn Fat Solution, but in my country (UK) Yohimbine HCL is currently banned.

I know I can import it from the USA, but for various reasons I do not want to attract the attention of UK customs/authorities. Also, because of the need to import, it is quite expensive.

In researching about a blood sugar lowering supplement (Berberine), I came across an interested pubmed abstract. It states that in the presence L-epinephrine (adrenaline), which should be raised by the caffeine & HIIT in the Stubborn Fat Protocol, that Berberine acts as alpha-2 adrenoceptor antagonist, similar to Yohimbine. Does anybody know, if Berberine could be used as a replacement for Yomimbine, even if its effects are weaker?

"Berberine, an alkaloid, has been found to have a myriad of pharmacological effects including hypotensive, antisecretory, sedative, and antimicrobial effects, some of which are similar to those of clonidine, an alpha 2 adrenoceptor partial agonist. The interaction of berberine with human platelet alpha 2 adrenoceptor was investigated in this study. Berberine was found to inhibit competitively the specific binding of [3H]-yohimbine. The displacement curve was parallel to those of clonidine, epinephrine, norepinephrine, with the rank order of potency (IC50) being clonidine (0.4 microM) greater than epinephrine (7.5 microM) greater than norepinephrine (14.5 microM) = berberine (16.6 microM). Increasing concentrations of berberine from 0.1 microM to 10 microM inhibited [3H]-yohimbine binding, shifting the saturation binding curve to the right without decreasing the maximum binding capacity. In platelet cyclic AMP accumulation experiments, berberine at concentrations of 0.1 microM to 0.1 mM inhibited the cAMP accumulation induced by 10 microM prostaglandin E1 in a dose dependent manner, acting as an alpha 2 adrenoceptor agonist. In the presence of L-epinephrine, berberine blocked the inhibitory effect of L-epinephrine behaving as an alpha 2 adrenoceptor antagonist. These properties are similar to those of clonidine on human platelets, suggesting that berberine is a partial agonist of platelet alpha 2 adrenoceptors. These findings may provide potential mechanisms for the hypotensive, antisecretory, and sedative effects of berberine."

https://www.ncbi.nlm.nih.gov/pubmed/1649363
I am in the UK and have had no trouble getting hold of yohimbine from online stores. Secondly it is important to note that it is illegal to sell it (over the counter) but it is legal to buy and possess it.
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