DMAA Alternative

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  1. Quote Originally Posted by Kelt View Post
    Yes, police do profiling in Sweden as well. However, profiling takes time, and sometimes police do not have time. In these cases, police have the right to act, if they think something is fishy. I know it is weird, but it is how it works here. Also to be clear, I am not a police, I am just a Ph.D. student in a technical field.

    Also so we do not deviate from this thread, let me ask you Patrick. Do you have any idea what are the consequences if a substance have ability of binding to Estrogen Receptor alpha? I know it is probably dose dependent, but how bad can it be?

    You are misunderstanding the meaning of the word profiling as I meant it. Profiling in the context I am talking about means selectively pursuing a suspect based on characteristics such as race or religion or style of clothes they wear etc. Examples would be preferentially pulling a muslim aside at an airport for secondary screening or pulling a hispanic guy in a car over and asking for his identification because you suspect he may be illegal.
    Anabolicminds.com Featured Author


  2. Quote Originally Posted by Kelt View Post
    Yes, police do profiling in Sweden as well. However, profiling takes time, and sometimes police do not have time. In these cases, police have the right to act, if they think something is fishy. I know it is weird, but it is how it works here. Also to be clear, I am not a police, I am just a Ph.D. student in a technical field.

    Also so we do not deviate from this thread, let me ask you Patrick. Do you have any idea what are the consequences if a substance have ability of binding to Estrogen Receptor alpha? I know it is probably dose dependent, but how bad can it be?


    ERalpha I believe is the predominant subtype in the hypothalamus. Therefore, a binder should suppress the HPTA
    Anabolicminds.com Featured Author
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  3. Quote Originally Posted by Patrick Arnold View Post
    You are misunderstanding the meaning of the word profiling as I meant it. Profiling in the context I am talking about means selectively pursuing a suspect based on characteristics such as race or religion or style of clothes they wear etc. Examples would be preferentially pulling a muslim aside at an airport for secondary screening or pulling a hispanic guy in a car over and asking for his identification because you suspect he may be illegal.
    Ok, I understand now. Well here in Sweden our leaders like to “educate” us normal mortals in various “negative” activities (do not know how exactly call it). Therefore, it is very common practice to do something calls zero tolerance weeks. One week they pick for example driving under influence of alcohol. This means that the whole week, children in schools are “educated” how dangerous it is. Meanwhile police in the same week do extra alcohol controls on the roads. I have seen zero tolerance weeks on violence, racism, narcotics and also doping. Every time there is such a campaign the police are reinforcing it with targeted activities.

    Sweden is on other hand too much of humanistic, meaning, for example the convicts have quit a lot of rights. Therefore I am not surprised to read in newspaper that convicted pedophiles ware sending each other pictures of children over the mobile phones, since in Sweden, they are allowed to keep them.

    I do not want to make this thread to much of a political debate. So to make some sort of a conclusion the two biggest negative thinks (as I see them) are: 1 the state is trying to over protect its citizens and 2 on another hand they try to preserve the humanistic rights for everybody. And this in the end creates such weird situations.

  4. Quote Originally Posted by Kelt View Post
    Ok, I understand now. Well here in Sweden our leaders like to “educate” us normal mortals in various “negative” activities (do not know how exactly call it). Therefore, it is very common practice to do something calls zero tolerance weeks. One week they pick for example driving under influence of alcohol. This means that the whole week, children in schools are “educated” how dangerous it is. Meanwhile police in the same week do extra alcohol controls on the roads. I have seen zero tolerance weeks on violence, racism, narcotics and also doping. Every time there is such a campaign the police are reinforcing it with targeted activities.

    Sweden is on other hand too much of humanistic, meaning, for example the convicts have quit a lot of rights. Therefore I am not surprised to read in newspaper that convicted pedophiles ware sending each other pictures of children over the mobile phones, since in Sweden, they are allowed to keep them.

    I do not want to make this thread to much of a political debate. So to make some sort of a conclusion the two biggest negative thinks (as I see them) are: 1 the state is trying to over protect its citizens and 2 on another hand they try to preserve the humanistic rights for everybody. And this in the end creates such weird situations.

    Yikes is all i gotta say
    Anabolicminds.com Featured Author

  5. Quote Originally Posted by Patrick Arnold View Post
    Yikes is all i gotta say
    Yes, it is a mess. However, there are also many good things, but like I said, we should not make this tread into a political debating. These thinks are better to talk about person to person in a pub then on an internet forum.
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  6. Quote Originally Posted by Kelt View Post
    what are the consequences if a substance have ability of binding to Estrogen Receptor alpha? I know it is probably dose dependent, but how bad can it be?
    Binding to the receptor does not imply activation. It could be an inverse agonist, antagonist, or bind with such low affinity as to afford physiological insignificance.

  7. Quote Originally Posted by lronFist View Post
    Binding to the receptor does not imply activation. It could be an inverse agonist, antagonist, or bind with such low affinity as to afford physiological insignificance.

    good point
    Anabolicminds.com Featured Author

  8. So we can say, if the substance is binding to ERalpha as agonist it will extra stimulate HPTA and in case of an antagonist then it will suppress HPTA?

  9. Quote Originally Posted by Kelt View Post
    So we can say, if the substance is binding to ERalpha as agonist it will extra stimulate HPTA and in case of an antagonist then it will suppress HPTA?
    I suppose, unless there are other aspects of the compound that interfere with the HPTA
    Anabolicminds.com Featured Author

  10. Quote Originally Posted by Patrick Arnold View Post
    I suppose, unless there are other aspects of the compound that interfere with the HPTA
    Ok, interesting. However, purely theoretically, it could give problems in case the over/under stimulation would deviate outside the usual limits?

    A small clarification about the incident with convicted pedophiles. I meant that they could keep the mobile phones during serving their sentence. Not that they were able to keep the pictures of which they have been convicted for, as one could understand from my previously written text. Sweden have its weird moments, but not that severely creepy.

  11. The difference between a four star prison and a four star hotel is I can leave the latter at will the former not so much. I think I will not be visiting.



  12. Quote Originally Posted by pushinweightw View Post
    The difference between a four star prison and a four star hotel is I can leave the latter at will the former not so much. I think I will not be visiting.
    The difference can also be seen as, full accommodation in four star prison is paid for you with taxation money (free education included), while accommodation in four star hotel cost you $$$. Although, do not exactly know how it works with people from outside of Sweden. Most probable is the deportation, unless you claim you will be killed if deported.

  13. Quote Originally Posted by Kelt View Post
    So we can say, if the substance is binding to ERalpha as agonist it will extra stimulate HPTA and in case of an antagonist then it will suppress HPTA?
    Higenamine has absolutely no access to the CNS (if it did, it would be quite neurotoxic) so it is a moot point.

  14. Quote Originally Posted by lronFist View Post
    Higenamine has absolutely no access to the CNS (if it did, it would be quite neurotoxic) so it is a moot point.
    Yes, I found a rat study that higenamine is mostly metabolized through Catechol-O-methyl transferase (COMT) to coclaurine and isococlaurine. As I understand it also humans have COMT mechanism so it could be argued that even we do produce such metabolites? I also did prediction on coclaurine which show somewhat higher probability then higenamine that it is a week ERalpha binder. Prediction shows a good chance of coclaurine to cross BBB.

    EDIT: Predictions are done in ACD/I-lab.

  15. Quote Originally Posted by Kelt View Post
    Yes, I found a rat study that higenamine is mostly metabolized through Catechol-O-methyl transferase (COMT) to coclaurine and isococlaurine. As I understand it also humans have COMT mechanism so it could be argued that even we do produce such metabolites? I also did prediction on coclaurine which show somewhat higher probability then higenamine that it is a week ERalpha binder. Prediction shows a good chance of coclaurine to cross BBB.

    EDIT: Predictions are done in ACD/I-lab.
    Coclaurine is the main metabolite via COMT, and it is a peripheral anti-stimulant (1). It won't make it pass the human BBB either. The first point is important because higenamine, which is indeed stimulatory to adrenergic receptors, has an incredibly short half-life and its main metabolite is distinctly anti-stimulatory.

    (1) jstage. jst. go. jp/article/jphs1951/50/1/50_1_75/_pdf

  16. Quote Originally Posted by lronFist View Post
    Coclaurine is the main metabolite via COMT, and it is a peripheral anti-stimulant (1). It won't make it pass the human BBB either. The first point is important because higenamine, which is indeed stimulatory to adrenergic receptors, has an incredibly short half-life and its main metabolite is distinctly anti-stimulatory.

    (1) jstage. jst. go. jp/article/jphs1951/50/1/50_1_75/_pdf
    Great find!

    Note: a www. addition is mandatory for that link to open. Reading now.

    So it appears it might not only be anti-stimulatory but also ergolytic during exercise...

  17. Quote Originally Posted by mr.cooper69 View Post
    Great find!

    Note: a addition is mandatory for that link to open. Reading now.
    My post count needs to be 150 before I can post links.

  18. Quote Originally Posted by lronFist View Post
    Coclaurine is the main metabolite via COMT, and it is a peripheral anti-stimulant (1). It won't make it pass the human BBB either. The first point is important because higenamine, which is indeed stimulatory to adrenergic receptors, has an incredibly short half-life and its main metabolite is distinctly anti-stimulatory.

    (1) jstage. jst. go. jp/article/jphs1951/50/1/50_1_75/_pdf
    Yes, that article I have seen. Some comments on the ACD/I-Lab predictions for crossing BBB are unfortunately only on rodent model.

  19. Quote Originally Posted by lronFist View Post
    My post count needs to be 150 before I can post links.
    I have the same problem, and find it annoying.

  20. DMAA is irreplaceable!!
    Anabolicminds.com Featured Author

  21. Quote Originally Posted by lronFist View Post
    Coclaurine is the main metabolite via COMT, and it is a peripheral anti-stimulant (1). It won't make it pass the human BBB either. The first point is important because higenamine, which is indeed stimulatory to adrenergic receptors, has an incredibly short half-life and its main metabolite is distinctly anti-stimulatory.

    (1) jstage. jst. go. jp/article/jphs1951/50/1/50_1_75/_pdf
    So I reread the pointed out article. Now, biochemistry is only my hobby so I am sorry if my following speculation is totally wrong.

    The test in that article has been conducted on the heart muscle and I presume you ware referring to the results in influence of calcium ion channels by higenamine and coclaurine? I have reread numerous times the chapter 5 (pp. 65-77) in book called Voltage-Gated Ion Channels as Drug Targets (ISBN 3-527-31258-7) and also found well summarized info on wiki about different types of calcium channels. It appears that L-type channels are mostly concentrated in cardiac muscle (the tissue used in the article), while in brain there are mostly P-type, Q-type and N-type of channels. Is it therefore correct to judge the possible CNS activities of Higenamine and Coclaurine in the brain, based on the test performed on L-type of channels?

  22. Quote Originally Posted by Kelt View Post
    So I reread the pointed out article. Now, biochemistry is only my hobby so I am sorry if my following speculation is totally wrong.

    The test in that article has been conducted on the heart muscle and I presume you ware referring to the results in influence of calcium ion channels by higenamine and coclaurine? I have reread numerous times the chapter 5 (pp. 65-77) in book called Voltage-Gated Ion Channels as Drug Targets (ISBN 3-527-31258-7) and also found well summarized info on wiki about different types of calcium channels. It appears that L-type channels are mostly concentrated in cardiac muscle (the tissue used in the article), while in brain there are mostly P-type, Q-type and N-type of channels. Is it therefore correct to judge the possible CNS activities of Higenamine and Coclaurine in the brain, based on the test performed on L-type of channels?
    In cardiac tissue, activating the beta-1 receptor increases cAMP which enhances calcium release from the sarcoplasmic reticulum via PKA. This is why higenamine is an inotrope. The study cited above notes that the 6-OH on the tetrahydroisoquinoline is a necessary constituent for beta receptor activation. COMT removes this constituent by way of creating a methoxy group (i.e. creating coclaurine).

    cvpharmacology. com/cardiostimulatory/beta-receptors-Gs.gif <---(This image may help).

    As I have already mentioned, neither higenamine nor colclaurine have access to the CNS, and probably do not interact directly with calcium channels.

  23. Quote Originally Posted by lronFist View Post
    In cardiac tissue, activating the beta-1 receptor increases cAMP which enhances calcium release from the sarcoplasmic reticulum via PKA. This is why higenamine is an inotrope. The study cited above notes that the 6-OH on the tetrahydroisoquinoline is a necessary constituent for beta receptor activation. COMT removes this constituent by way of creating a methoxy group (i.e. creating coclaurine).

    cvpharmacology. com/cardiostimulatory/beta-receptors-Gs.gif <---(This image may help).

    As I have already mentioned, neither higenamine nor colclaurine have access to the CNS, and probably do not interact directly with calcium channels.
    Oh, I see, this is how it goes when I read something outside of my area after midnight.

    However, I cannot stop wondering that the prediction in ACD/I-Lab can be so wrong. They use predictions of LogPS (rate of brain penetration), LogPB/LogBB (extent of brain penetration) and Log(PS*fu, brain) (Brain/plasma equilibration rate) as a measure of “brain penetration sufficient for CNS activity”. There are numerous nicely writer articles about efforts on estimating accurate predictions of new compounds’ properties.

    Did you have a look at this tool?
    ilab.acdlabs.com/iLab2 (I use your trick )

  24. PA what led you to look for DMAA in the first place? Was it a quest to find an ephedrine alternative? Do you have an interest in finding an alternative to DMAA? If no what would it take to generate an interest in such?

    Thank you for your time.



  25. Quote Originally Posted by pushinweightw View Post
    PA what led you to look for DMAA in the first place? Was it a quest to find an ephedrine alternative? Do you have an interest in finding an alternative to DMAA? If no what would it take to generate an interest in such?

    Thank you for your time.
    +1
    These are really good questions.

  26. Quote Originally Posted by Patrick Arnold

    In Sweden u can be apprehended by police if they suspect you are using anabolic steroids. suspicion can be simply having extraordinary muscle mass. this happened to IFBB bodybuilders that were visiting sweden recently.
    At least one (Tony Freeman) was arrested and forced to submit urine if i recall
    The X-man had been to Holland a couple of days before going to Sweden. In Holland he smoked a joint, which explains the narcotics. He also had prescriptions for his aas, which cleared him from the drug use. I think he lost a contract with a supplement company because of his arrest.

    Norway is more strict than Sweden, but one is allowed to use aas.

  27. Quote Originally Posted by Patrick Arnold
    DMAA is irreplaceable!!
    Before a workout with ......?
    As a fatburner?

  28. Quote Originally Posted by HITFrank View Post
    Before a workout with ......?
    As a fatburner?
    both, Clear Shot, its all you need
    E-PHARM Nutrition Representative
    Better one ugly truth than a million pretty lies
    Check Out Ur-Spray and D-Serine at Prototype Nutrition




  29. Quote Originally Posted by pushinweightw View Post
    PA what led you to look for DMAA in the first place? Was it a quest to find an ephedrine alternative? Do you have an interest in finding an alternative to DMAA? If no what would it take to generate an interest in such?

    Thank you for your time.
    +1
    I've got an add-odd question for PA: How long did it take you to finally settle on DMAA and how many different substances did you research before deciding DMAA was the way to go?

  30. Quote Originally Posted by HITFrank View Post
    Norway is more strict than Sweden, but one is allowed to use aas.
    Interesting, is it not that essential amino acids in the free form are considered as pharmaceutics in Norway?
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