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Old 07-12-2008, 06:52 PM   #21
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Quote:
Originally Posted by Ironhead View Post
Check out this aricle Stereochemistry of the functional group determines the mechanism of aromatase inhibition by 6-bromoandrostenedione -- Osawa et al. 121 (3): 1010 -- Endocrinology

especially, "We have found that 6 alpha-bromoandrostenedione (6 alpha-BrA) is a competitive inhibitor of human placental aromatase with respect to androstenedione..."

Also, http://pubs.acs.org/cgi-bin/abstract...?sessid=6006l3

The end of the 2nd paragraph, "Furthermore,
both 6a- and 6b-bromoandrostenedione are competitive
inhibitors of androstenedione aromatization, as determined
by a Lineweaver-Burk plot, and 6a-bromoandrostenedione
gives the same type I cytochrome P-450 binding
spectrum with placental microsomes as androstenedione. These
data suggest that 6a-bromoandrostenedione is effective as an
active-site-directed inhibitor of placental microsomal aromatase"
Not only was the last article mentioned in vitro studies which I regard as a waste of time reading let alone citing, but this was stated from full text:

"Although 6a-bromoandrostenedione is the most active
compound examined, the aromatase inactivation appears to
be incomplete since 10 to 12% of the enzyme activity remains
after 17 h incubations with 260 and 520 nmol amounts of the
bromoandrogen. We sought to determine if this residual activity
represents a portion of microsomal aromatase that is
protected in some way from the inactivating effect or if some
other microsomal enzyme activity becomes apparent in the
aromatase assay when microsomal aromatase is completely
inactivated.....
.....The amount of [14C]estrone and [I4C]-
17P-estradiol produced during the incubation was measured
after organic solvent extraction and purification by thin-layer
chromatography (Bellino and Osawa, 1974) and countercurrent
distribution analysis (Spaeth and Osawa, 1974). [3H]-
Estrone and [3H]-17P-estradiol were added to the incubation
mixture before organic extraction to correct for the loss in the
procedures. The aromatase specific activity measured by
[ 14C]estrogen production agreed with the tritiated water
measurement. Therefore, the tritiated water production in the
aromatase assay using microsomes preincubated at 4 O C with
260 or 520 nmol of 6a-bromoandrostenedione for 17 h is due
to residual aromatase activity."

Also, a lot of these enzymes and BS were incubated at 4 degrees C which is far from human body temps, another reason to disregard this study. However, if you do want to talk about in vitro studies as being valid, this is of interesting 'merit' then:

"A stereospecificity of the inactivation is suggested by the inability
of 6b-bromoandrostenedione to inactivate the enzyme even
though it competitively inhibits androstenedione aromatization
in phosphate buffer and in “S” buffer to an extent equal to that
of the 6a isomer.
However, as discussed later, this stereospecificity
of inactivation may be due, at least in part, to the
relative instability of the 6b isomer in “S” buffer."

Moreover another reason to discredit this study....
But wait, it gets better:

"Furthermore, the extent of aromatase inactivation in a mixture of the two isomers,
6-bromoandrostenedione, was intermediate to that found
when the two isomers were incubated individually. This finding
probably reflects a partial protection of aromatase by the 6b
component since this component apparently is capable of reversibly
binding to the active site and it is present in significant,
though greatly reduced, amounts throughout the 17-h incubation.
"

Quote:
PA just wants you to believe that 6-OXO is the ONLY solid OTC AI...Oh wait does Ergopharm make that product??
I can think on my own, thank you very much.

Quote:
Originally Posted by mmowry View Post
No he wouldnt do that would he? That would be unethical!
The IBE vs. PA mentality still lingers I sea
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Old 07-12-2008, 08:09 PM   #22
 
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Nothing to do with Pat and IBE.Whats done is done and i dont live in the past .It just has to do with how PA treats people thats all.

But thanks for looking deeper into things than you need to......reminds me of my ex wife.(my counter attempt at being witty.lol) So lets act like adults and move on shall we.

Lets be honest, do you really think hes out to save the bbing world from themselves or does he have a vested interest most times? Hes a very intellegent man I admit but his delivery has alot to be desired if hes earnestly trying to help.

.
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Last edited by mmowry; 07-12-2008 at 08:24 PM.
Old 07-12-2008, 08:33 PM   #23
 
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I see some puppets had their stings clipped lol
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Old 07-13-2008, 12:09 AM   #24
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Quote:
Originally Posted by Beejis60 View Post
Not only was the last article mentioned in vitro studies which I regard as a waste of time reading let alone citing, but this was stated from full text:

"Although 6a-bromoandrostenedione is the most active
compound examined, the aromatase inactivation appears to
be incomplete since 10 to 12% of the enzyme activity remains
after 17 h incubations with 260 and 520 nmol amounts of the
bromoandrogen. We sought to determine if this residual activity
represents a portion of microsomal aromatase that is
protected in some way from the inactivating effect or if some
other microsomal enzyme activity becomes apparent in the
aromatase assay when microsomal aromatase is completely
inactivated.....
.....The amount of [14C]estrone and [I4C]-
17P-estradiol produced during the incubation was measured
after organic solvent extraction and purification by thin-layer
chromatography (Bellino and Osawa, 1974) and countercurrent
distribution analysis (Spaeth and Osawa, 1974). [3H]-
Estrone and [3H]-17P-estradiol were added to the incubation
mixture before organic extraction to correct for the loss in the
procedures. The aromatase specific activity measured by
[ 14C]estrogen production agreed with the tritiated water
measurement. Therefore, the tritiated water production in the
aromatase assay using microsomes preincubated at 4 O C with
260 or 520 nmol of 6a-bromoandrostenedione for 17 h is due
to residual aromatase activity."

Also, a lot of these enzymes and BS were incubated at 4 degrees C which is far from human body temps, another reason to disregard this study. However, if you do want to talk about in vitro studies as being valid, this is of interesting 'merit' then:

"A stereospecificity of the inactivation is suggested by the inability
of 6b-bromoandrostenedione to inactivate the enzyme even
though it competitively inhibits androstenedione aromatization
in phosphate buffer and in “S” buffer to an extent equal to that
of the 6a isomer.
However, as discussed later, this stereospecificity
of inactivation may be due, at least in part, to the
relative instability of the 6b isomer in “S” buffer."

Moreover another reason to discredit this study....
But wait, it gets better:

"Furthermore, the extent of aromatase inactivation in a mixture of the two isomers,
6-bromoandrostenedione, was intermediate to that found
when the two isomers were incubated individually. This finding
probably reflects a partial protection of aromatase by the 6b
component since this component apparently is capable of reversibly
binding to the active site and it is present in significant,
though greatly reduced, amounts throughout the 17-h incubation.
"



I can think on my own, thank you very much.



The IBE vs. PA mentality still lingers I sea
First of all Ergopharm is not a bad company, so I'm not dissing who you rep (lets be honest).

Second, your post means nothing because your original rebuttal was that 6-Bromo was no good because of the alpha isomer being anabolic and not an inhibitor. I gave you information asserting that both isomers are indeed inhibitors and you retort with empty rhetoric merely stating that the A isomer was found to incomplete aromatase inactivation 10-12% and some sideshow about "in vitro tests." Your reply doesn't negate the fact that "both 6a- and 6b-bromoandrostenedione are competitive inhibitors of androstenedione aromatization."

Stay on track dude. Let's move on.

Good day
Old 07-13-2008, 09:46 AM   #25
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Quote:
Originally Posted by mmowry View Post
Lets be honest, do you really think hes out to save the bbing world from themselves or does he have a vested interest most times? Hes a very intellegent man I admit but his delivery has alot to be desired if hes earnestly trying to help.
He's said numerous times he's no salesman, so ya, I guess he's like me or vice versa.

Quote:
Originally Posted by Ironhead View Post
First of all Ergopharm is not a bad company, so I'm not dissing who you rep (lets be honest).
I've stated before and most people know that your statement is true; I was asked by a mod (I think) to remove it since we are not a sponsor.

Quote:
Second, your post means nothing because your original rebuttal was that 6-Bromo was no good because of the alpha isomer being anabolic and not an inhibitor. I gave you information asserting that both isomers are indeed inhibitors and you retort with empty rhetoric merely stating that the A isomer was found to incomplete aromatase inactivation 10-12% and some sideshow about "in vitro tests." Your reply doesn't negate the fact that "both 6a- and 6b-bromoandrostenedione are competitive inhibitors of androstenedione aromatization."
I said it was not a good idea. I don't know at what time frame it was found about the alpha/beta isomer metabolite with respect to this study.
In vitro studies really hold no merit, to me, when reading any journal articles for my own Ph.D. research (organic synthesis); also these were incubated at 4 degrees, the human body is 37 degrees. That is far from realistic, don't you think?
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Old 07-13-2008, 09:50 AM   #27
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In what respect? ATD has a greater IC50 than 6-OXO, so if that's solely your basis of claim, then I would agree with you, though an incomplete argument.
PS- Those studies are done in eugonadal men.
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Last edited by Beejis60; 07-13-2008 at 09:58 AM.
Old 07-13-2008, 10:13 AM   #28
 
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Quote:
Originally Posted by xjsynx View Post
DR P for PCT, hmmmmm




Or do you mean Dr D or Dr C, or the resident doc dinoiii (who is not Dr D).
lol

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Old 07-13-2008, 01:57 PM   #29
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Quote:
Originally Posted by Beejis60 View Post
In what respect? ATD has a greater IC50 than 6-OXO, so if that's solely your basis of claim, then I would agree with you, though an incomplete argument.
PS- Those studies are done in eugonadal men.
Yes, I am aware. Eugonadal.

To copy and paste:

"Novedex XT resulted in average increases of 283%, 625%, 566%, and 438% for total testosterone (P=0.001), free testosterone (P=0.001), dihydrotestosterone (P=0.001), and the testosterone:estrogen ratio (P=0.001), respectively, whereas fat mass decreased 3.5% (P=0.026) during supplementation."

"Compared to baseline, free testosterone underwent overall increases of 90% for 300 mg 6-OXO and 84% for 600 mg, respectively (p < 0.05). DHT underwent significant overall increases (p < 0.05) of 192% and 265% with 300 mg and 600 mg, respectively. T/E increased 53% and 67% for 300 mg and 600 mg 6-OXO, respectively. For estrone, 300 mg produced an overall increase of 22%, whereas 600 mg caused a 52% increase (p < 0.05).Body composition did not change with supplementation (p > 0.05) and clinical safety markers were not adversely affected with ingestion of either supplement dose (p > 0.05)."

So lets see (now I admit the sentence structure in the first study is a bit annoying but):
....