A little more help.

Sldge

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Ok, I could use a little help again, I am still really busy and was just looking through some stuff, can someone do a search and see what info you can come up with on Bolasterone (17beta-Hydroxy-7alpha,17-dimethylandrost-4-en-3-one) CAS# 1605-89-6

Thanks for any help.
 

phatbody

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Bolasterone (myagen)
This was originally a popular oral steroid being used in Europe. It had functions similar to dianabol, but it has long since been discontinued. Several years ago bolasterone became the first big name counterfeit steroid to be internationally marked.
Belonging to a group of steroids titled the DDR compounds, inferring they came from East Germany, this steroid was billed as the best drug ever made. It became very popular partially because several respected steroid experts were in on the production of it, and gave it rave reviews in their publications. Thousands of 30 cc vials of this injectable steroid were sold at a price of over 200 dollars a piece.
It was said to contain ten miligram of the drug per cc, but it actually contained a low dosage of several domestic steroids mixed together. In the spring of 1986 the makers of this drug were busted. There are still at least three other counterfeiters using the bolasterone name: UCLA bolasterone, available in a 10 cc vail; new bolasterone, available in a 10 cc vial, and bolasterone depot available in a 50 cc vial. All of these items are the worst kind of counterfeit steroids made. They are worthless and dangerous. Many athletes are still taking these drugs. It is obvious that any item carrying a bolasterone or GDR label should be avoided.
 

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Bolasterone

Bolasterone is an anabolic steroid implicit in Schedule III classification by PL 101-647, but not explicitly named therein.
 

Sldge

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Thanks phatbody, that was quick, if you come up with anything else let me know. I am pretty sure it is a scheduled drug but I am going to check a few other things also when I get some time.
 

x_muscle

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its scduled in canada

Bolasterone
Structure: 3.23.5. Merck: 1326, Bolasterone, anabolic.
"Bolasterone" was placed on the schedule to part G of the FDR and exempted from the general category of "Sex Hormones" on the prescription drug schedule by P.C. 1992-1295(SOR/92-386). It was simultaneously made a controlled drug by P.C. 1992-1296(SOR/92-387).
"Bolasterone (17-beta-Hydroxy-7-alpha,17-dimethylandrost-4-en-3-one)" is listed on schedule III of the CDSA
 

phatbody

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I just did some quick searches on google and yahoo and pulled up whatever looked promising. I'm just getting repeats of the EXACT same paragraph as above. So I don't think I will be able to find more at this time. Of course now is about the time Bobo pulls out a thesis paper on Bolasterone.

Oh and apparently Thermolife makes "Bolasterone"
 

Sldge

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Well maybe Bobo can find something else. It dosent say what the compound in Thermolife's crap is.

If anyone has the Vida text nearby and can look up the ratios that would be helpful also. I assume it should be a pretty strong compound and I assume there will be some conversion to estrogen but I havent had a chance to look up very much on it.

And if you can find anything on MENT, there should be some studies showing what doses are being tested as a male contraceptive and I believe they are using a transdermal application for it.
 

phatbody

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MENT®
Several promising male methods are under development at the Population Council that rely on MENT®, a synthetic steroid that resembles testosterone. In contrast to testosterone, however, MENT does not have the effect of enlarging the prostate, a drawback that occurs with testosterone administered for therapy. A MENT implant and MENT transdermal gel and patch formulations are being developed for contraception and hormone therapy.
(More information)

Implants
Delivering MENT acetate (MENT Ac) via one or more implants placed under the skin of the upper arm, this contraceptive aims to suppress sperm cell development without impairing sexual drive (libido). Early developmental work on the MENT Ac implant indicated that it might be appropriate both as a contraceptive in normal men and as hormone therapy in men with male-hormone deficiency (hypogonadal men). A recently completed one-year dose-finding study in normal men has shown that four implants suppress gonadotrophin levels completely, leading to profoundly reduced sperm count. Eight of eleven men with 4 implants had zero sperm count which lasted in many subjects for several months until the implants were removed. In hypogonadal men, two MENT Ac implants were found to be adequate as therapy, and the men in the study preferred the implants to the standard therapy involving multiple injections of a testosterone derivative.

Other studies that combine MENT Ac implants with a synthetic progestin are underway. Long-term toxicology studies of MENT are also ongoing.

Transdermal gels and patches
Laboratory tests show that MENT readily penetrates the skin. The delivery of a potent androgen through the skin into the blood stream is an effective way to avoid metabolism by the liver, thereby decreasing side effects of the hormone. Early studies in men indicated that MENT delivered via transdermal gel suppressed steroid sex hormones over a seven-day treatment period, and that the effect was reversible when the treatment ended. Preliminary studies conducted in hypogonadal men also show the gel to be safe for further development as a method of hormone therapy.

Publications/Resources
Council researchers' names appear in boldface type.

2003
Lui, WY, WM Lee and CY Cheng. "Sertoli-germ cell adherens junction dynamics in the testis are regulated by RhoB GTPase via the ROCK/LIMK signaling pathway," Biology of Reproduction 68:2189--2206.

Siu, MKY, DD Mruk, WM Lee and CY Cheng. "Adhering junction dynamics in the testis are regulated by an interplay of ß-integrin and focal adhesion complex-associated proteins," Endocrinology 114:2141-2163.

2002
Cheng, CY, and DD Mruk. "Cell junction dynamics in the testis: Sertoli-germ cell interactions and male contraceptive development," Physiological Reviews 82:825-874.

Mruk, DD, B Silvestrini, MY Mo and CY Cheng. "Antioxidant superoxide dismutase - a review: its function, regulation in the testis, and role in male fertility," Contraception 65:305-311.

2001
Cheng, CY, B Silvestrini, J Grima, MY Mo, LJ Zhu, E Johansson, L Saso, MG Leone, M Palmery and DD Mruk. "Two new male contraceptives exert their effects by depleting germ cells prematurely from the testis," Biology of Reproduction 65:449-461.
 

phatbody

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Product Development
Contraceptives - Male
MENT®, Not Method-Specific
Two animal studies were planned to address issues related to the development of MENT® implants. A clinical trial is underway comparing MENT alone with three groups of various MENT-plus-levonorgestrel dose combinations.


In a rat model, however, a combination of MENT and levonorgestrel did not inhibit sperm production because testosterone has a direct stimulatory effect on spermatogenesis in rats, even when gonadotropins have been suppressed.

Hence, it was decided to investigate the effect of MENT alone and in combination with levonorgestrel on luteinizing hormone (LH) secretion from pituitary cells in culture. A rat pituitary cell culture assay system was established. The pituitary cells have been treated with MENT or levonorgestrel at different concentrations. The media have been collected for LH assays, and the assays are being validated to measure the LH content in the culture media obtained from the treatment of pituitary cells.

This research also includes radioimmunoassay of serum samples for MENT for clinical trials involving the Population Council's International Committee for Contraception Research.

Location: United States
Population Council researchers: Narender Kumar, Kalyan Sundaram
 

phatbody

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Product Development
Contraceptives - Male
Transdermal Delivery Systems
MENT® is permeable through animal skin at three times the rate of testosterone and has been shown to readily penetrate the skin and suppress production of the gonadotropins required for spermatogenesis. A transdermal gel formulation of MENT was compared to gel formulations containing two other androgens, 17 methyl testosterone and 17-a methyl testosterone.

Results indicate that MENT permeates the skin significantly better than the two other androgens. A clinical trial of MENT gel for use in hormone therapy in elderly men was completed, indicating some improvement in well-being among men using the gel. The study shows the gel to be safe for further development as a hormone therapy method.

Location: Chile, United States
Population Council researcher: Yun-yen Tsong
 

phatbody

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Clinical Trial of 7-Methyl-19-Nortestosterone Implants for Possible Use as a Long-Acting Contraceptive for Men

Sigrid von Eckardstein, Gabriela Noe, Vivian Brache, Eberhard Nieschlag, Horacio Croxatto, Francisco Alvarez, Alfred Moo-Young, Irving Sivin, Narender Kumar, Margaret Small and Kalyan Sundaram
Institute of Reproductive Medicine, University of Munster (S.v.E., E.N.), Munster, Germany; Instituto de Medicina Reproductiva (G.N., H.C.), Correo 22, Casilla 96 Santiago, Chile; PROFAMILIA (V.B., F.A.), Apartado Postal 1053, Santo Domingo, Dominican Republic; and The Population Council (A.M.-Y., N.K., M.S., I.S., K.S.), New York, New York 10021
Address all correspondence and requests for reprints to: Dr. Kalyan Sundaram, Center for Biomedical Research, Population Council, 1230 York Avenue, New York, New York 10021. E-mail: kalyan@popcbr. rockefeller.edu.

Several preparations of testosterone and its esters are being investigated alone or in combination with other gonadotropin-suppressing agents as possible antifertility agents for men. We studied the effectiveness of 7-methyl-19-nortestosterone (MENT) as an antispermatogenic agent in men. MENT has been shown to be more potent than testosterone and to be resistant to 5-reduction. For sustained delivery of MENT, we used a system consisting of ethylene vinyl acetate implants containing MENT acetate (Ac), administered subdermally. Thirty-five normal volunteers were recruited in 3 clinics and were randomly assigned to 1 of 3 doses: 1 (12 men), 2 (11 men), or 4 (12 men) MENT Ac implants. The initial average in vitro release rate of MENT Ac from each implant was approximately 400 µg/day. Implants were inserted subdermally in the medial aspect of the upper arm under local anesthesia. The duration of treatment was initially designed to be 6 months. However, in 2 clinics the duration of treatment was extended to 9 months for the 2-implant group and to 12 months for the 4-implant group. Dose-related increases in serum MENT levels and decreases in testosterone, LH, and FSH levels were observed. Effects on sperm counts were also dose related. None of the subjects in the 1-implant group exhibited oligozoospermia (sperm count, <3 million/ml). Four subjects in the 2-implant group became oligozoospermic, 2 of whom reached azoospermia. Eight subjects in the 4-implant group reached azoospermia, with 1 exhibiting oligozoospermia, whereas 2 were nonresponders. Side effects generally seen with androgen administration, such as increases in erythrocyte count, hematocrit, and hemoglobin and a decrease in SHBG, were also seen in this study and were reversible. Changes in lipid parameters were moderate and transient. Liver enzymes showed small changes. This study demonstrates that MENT Ac, when administered in a sustained release fashion via subdermal implants, can inhibit spermatogenesis over a prolonged period after a single administration and has the potential to be used as a male contraceptive.

This work was supported by the U.S. Agency for International Development (Cooperative Agreement HRN-A-00-99-00010-00), the United Nations Population Fund, the NIH (Center Grant U54-HD-29990), the Andrew W. Mellon Foundation, the Bingham Trust, the Educational Foundation of America, the Lila Annenberg Hazen Foundation, the George Hecht Family Trust, and the William and Flora Hewlett Foundation.

Preliminary results of this study were presented in abstract form at the VIIth International Congress of Andrology, Montreal, Canada, 2001.

Abbreviations: Ac, Acetate; BP, blood pressure; CV, coefficient of variation; MENT, 7-methyl-19-nortestosterone; PSA, prostate-specific antigen; T, testosterone; TE, testosterone enanthate; TU, testosterone undecanoate.
 

phatbody

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Male hormonal contraception

Research on hormonal methods of male contraception has been completed (2), and this approach will likely yield a marketable product in the next few years [33]. Investigated strategies include weekly or long-acting intramuscular (IM) injections, and implantable, oral, or transdermal testosterone delivery systems. In an effort to boost the rates of azoospermia, combination regimens involving gonad-otropin-releasing hormone (GnRH) analogues and progestins have also been studied.

Normal spermatogenesis occurs in the testes of sexually mature males in response to GnRH stimulation of the pituitary gonadotropins (luteinizing hormone [LH] and smaller amounts of follicle-stimulating hormone [FSH]) [33]. Testosterone and other androgens produced by testicular Leydig's cells, and inhibin B, produced by testicular Sertoli's cells, send negative feedback to the hypothalamus and pituitary. Interference with this normal feedback results in impaired spermatogenesis in males in a manner analogous to the interruption of ovulation in women [34,35].

The efficacy of male hormonal methods depends on the degree of suppression of spermatogenesis. Two large studies investigated the safety and efficacy of testosterone enanthate (TE), administered weekly in 200-mg IM injections. A 1990 World Health Organization (WHO) study found that 157 (58%) of 271 men who completed a 6-month induction phase of weekly injections became azoospermic (mean time: 120 days). Only one pregnancy occurred during 1486 months of exposure (0.8 conceptions per 100 person-years) during a 12-month efficacy study [36]. A subsequent WHO study investigated the efficacy of the approach in men who did, and men who did not, achieve azoospermia [37]. After the 6-month induction phase, adequate suppression of spermatogenesis (oligospermia 3 million) occurred in 391 (98%) of 399 men enrolled in the study. No pregnancies occurred among partners of men with azoospermia, but four pregnancies (8.1 per 100 person-years) occurred in partners of men with oligo-azoospermia (0.1 to 3 × 106/mL) [37]. A small contraceptive trial of testosterone implants at a dose of 800 to 1200 mg every 3 months up to 15 months found no pregnancies in partners of men achieving azoospermia [38].

The use of long-acting testosterone formulations such as testosterone undecanoate (TU) may improve acceptability of a male hormonal method by eliminating the need for weekly IM injections. Injection of 1000 mg TU IM every 6 weeks produces rates of oligo- and azoospermia similar to that obtained with weekly TE [39]. Implantation of testosterone pellets at a dose of 1200 mg provides stable testosterone levels for 4 to 6 months, and suppression of sperm counts to levels seen with weekly TE [42]. Testosterone encapsulated in biodegradable polylactide-glycolide microspheres and injected subcutaneously provides sustained stable levels, but contraceptive trials of this formulation are not yet available [43].

Concerns regarding hepatotoxicity and short half-life limit the potential use of currently available oral testosterone as a contraceptive [44]. Testosterone patches cannot deliver doses adequate for suppression of spermatogenesis [44]. Analogues of 7-apha-methyl-19-nortestosterone (MENT), an androgen resistant to 5alpha-reductase activity, may emerge as the ideal androgen for a male contraceptive [45]. MENT resists enzymatic conversion of 5alpha-reductase to dihydrotestosterone, the primary androgen involved in stimulating prostate growth, balding, and acne. Studies in rhesus macaques report that MENT effectively suppresses gonadotropins with comparatively little effects on prostate growth [46]. MENT has a short serum half-life because it does not bind to sex-hormone-binding globulin, but stable levels capable of suppressing gonad-otropins are obtained with implant delivery systems [47].

Combining a GnRH antagonist with testosterone induces azoospermia more rapidly and reliably than testosterone alone. A recent study [48] showed that 14 of 15 men treated with daily subcutaneous injections of the GnRH antagonist Nal-Glu and weekly IM injections of 100 mg of TE for 12 weeks had sperm counts less than 3 million/mL, and 10 subjects had complete azoospermia. Suppression of spermatogenesis was maintained in this study for an additional 20 weeks with TE alone at 100 mg per week, half the customary dose.

Oral or transdermal administrations of synthetic progestins suppress gonadotropins in men just as they do in women. Randomized trials demonstrate the superiority of the combined approach to testosterone alone. The most promising combinations include IM TE, and oral levonor-gestrel [39,49] or desogestrel [50,51]. Long-acting injections and implants of testosterone in combination with injections of medroxyprogesterone acetate or norethi-s-terone enanthate also produce azoospermia or severe oligospermia in most subjects [41,52].

The primary side effects of high-dose testosterone enanthate therapy observed in the WHO trials are weight gain (2.5-3 kg) and suppression of serum high-density lipoprotein (10%-15%) [37]. These effects appear in all subsequent long-term studies. Other side effects include increased erythrocytes, hemoglobin, and hematocrit, and decreased high-density lipoprotein cholesterol and alkaline phosphatase. Oral administration of some testosterone and progestin preparations may increase liver enzymes. The impact of these changes on long-term health is unknown, but the potential effect of adverse lipid changes on a male's lifetime risk of cardiovascular disease requires additional study. The effect of androgen stimulation on the risk of prostate cancer also requires study. Although significant changes in prostate volume or prostate-specific antigen levels have not been seen in contraceptive studies, additional long-term observations are necessary.
 

phatbody

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Hope some of these articles help out. Very interesting stuff this MENT.
 

Sldge

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yeah there is also a study showing it to be the only NON toxic methyl. :D I am looking for some dosing schemes. so we will see.
 

Onslaught

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It is such a tease when you do this!

"We will see." What will we see damnit?
 

nsruffryder34

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To my knowledge it isnt schedulaed but thats just off the top of my head. I have it written down at home, Im not sure if it was bolasterone or a derivative but I know one wasnt schedualed....
 

Sldge

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Well this 7a-17a-Dimethyl-4-AD should be the precursor of Bolasterone, and I dont think that is scheduled. 7a-methyl-19nordiol would be the precursor to MENT and that isnt scheduled either. I am getting a small amount of PROMENT in soon, so hopefully we will be able to extend the ban slightly to try some of these out.

Please no one email me I dont need beta testers, I just dont have enough of it.
 

nsruffryder34

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This is off the top of my head again, but the bolasterone precursor you listed, I believe is really hard on the liver. THeres so many compunds i have written down I get some mixed up at times though. Just a heads up..
 

Sldge

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It may be, I havent done tons of research on it. I dont have any plans for it yet, just becuase I dont think Ill have the time but you never know. although M1T is really rough so it would be nice to see a comparison.
 
custom

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I was looking into MENT awhile back after I read a nice piece on it by Bruce Kneller, but the only reputable source was the patent holder, and needless to say they were not willing to deal.
 

nsruffryder34

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I cant cehck on it right now, but I will check at home, I wrote down quite a bir of info on it. I think BK was thinking about realeasing it (maybe still is).
 

nsruffryder34

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I dont think they hold the patent on the precursor though
 

Sldge

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No they dont hold the patent on the precursor, it would need to be made, and mine is on its way to me. ;)
 

trd277

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BK is Bruce Kneller. He writes for MD and puts out a few supps.
 

jjjd

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Bruce Kneller also writes/wrote for Testosterone mag under the pseudonym "Brock Strasser"
 

Sldge

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No, he is doing them through other companies, like Gaspari. Nothing that isnt already out.
 

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