NORBOLETHONE

- Everything we could find out about it

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Created Sep 2020

NORBOLETHONE

  • [GENABOL]
  • [NORBOLETONE]

(13BETA,17ALPHA-DIETHYL-17BETA-HYDROXYGON-4-EN-3-ONE)

DEA CODE 4000: Schedule 3

Norboletone, or norbolethone, is an anabolic steroid that was never marketed. It was first developed in 1966 by Wyeth Laboratories, and tested for use as an agent to encourage weight gain and for the treatment of short stature, but was never marketed commercially because of fears that it might be toxic. Norboletone is on the World Anti-Doping Agency's list of prohibited substances, and is therefore banned from use in most major sports.

Norbolethone is an orally active derivative of nandrolone. Structurally, this steroid differs from normethandrolone (Orgasteron) only by the substitution of the 13-methyl group with an ethyl. As is common for a member of the nandrolone family, norbolethone is more anabolic than androgenic in nature. Early animal studies place the anabolic index of this agent at 20 as compared to oral methyltestosterone (the standard of comparison for oral anabolic/androgenic steroids), meaning that it has 20 times higher anabolic than androgenic activity. Although this figure may not translate perfectly to real-world human use, we can still expect a favorable balance of anabolic to androgenic effect. Comparisons to other commercially available agents would probably place norbolethone in a, similar category to norethandrolone, both being effective anabolic derivatives of nandrolone, but with some additional estrogenic and progestational activity that makes them somewhat dissimilar to more purely anabolic agents. Norbolethone is most appropriately considered a bodybuilding drug, and is less ideally suited for the needs of competitive athletes.

Genabol History:
Norbolethone was first described in 1963. The drug was developed by Wyeth (Genabol, 2.5 mg), and put into human clinical trials between 1964 and 1972. It was investigated as a potential medicine to treat low body weight and children with short stature. Effective doses used in the studies were as low as 1.25 mg per day in children, but generally included a common adult dose of 2.5 mg to 10 mg per day. A detailed series of investigations into the metabolic effects of norbolethone (using 2.5 mg to 10 mg per day for up to 6 weeks) in adult and elderly men and women recovering from surgery or illness in 1968 determined that optimal protein retention was achieved at 7.5 mg per day (10 mg per day was shown to offer no advantage in this study). Although the drug was deemed highly anabolic with minimal androgenic properties, and effective doses had been determined, norbolethone was ultimately never released as a commercial prescription agent. As such, after the clinical trials were published, little mention was made of this drug for approximately thirty years.

Norbolethone was thrown into headlines in mid-2002, when it was announced that Dr. Don Catlin of the UCLA Analytical Laboratories had discovered that athletes were using this drug to beat the drug screens being conducted at his facility. Because norbolethone was never sold as a commercial steroid, the athletic bodies were not looking for it during earlier tests. A private chemist (later identified as Patrick Arnold) realized this, and manufactured it for the specific purpose of beating the drug screen. Catlin was clued into its use after identifying several "negative" samples that had signs of endogenous steroid suppression (potentially indicating steroid use). The norbolethone doping scandal that resulted was the first modern appearance of the "designer steroid" phenomenon. These are non-commercial steroids that do not show up on a drug screen by virtue of their anonymity. For as long as they are not known to drug-testing facilities, they will not be detected. Drugs like norbolethone are highly valued commodities among competitive athletes.

Once Catlin identified norbolethone, he promptly devised and released a method for the detection of its metabolites in the urine. Several world-class athletes were ultimately suspended for using this drug during competition, including U.S. Olympic cyclist Tammy Thomas. With this press release, norbolethone immediately lost any value it formerly had as an undetectable designer steroid. It has been "discovered," so to speak, and is now actively screened for during any serious steroid urinalysis test. There is little doubt that most of the athletes that were using this compound have long since abandoned it and moved on to better things. Charlie Francis, the man who coached Ben Johnson when he tested positive for steroids at the 1988 Summer Games, would later comment that norbolethone was being widely used at the 2000 Sydney Games, two years before the IOC caught wind of its existence.

Norbolethone found its way into the competitive athlete market by a chemist named Patrick Arnold. It was a component of a steroid formulation called "The Clear," which was marketed as being undetectable. It was originally developed to promote weight gain and to treat stunted growth. Of course, eventually its active ingredient was discovered, showing up in urine tests of competitors in the early 2000s. This lead to The Clear's formulation being changed.

Fears about the drug's toxicity prevented it from being marketed commercially. Under the brand name Genabol, Norbolethone made its way through numerous clinical trials. However, it never reached commercial markets. This means that it was never circulated and thus it is not available for purchase from online suppliers. Although it was included in a designer steroid formulation, as mentioned above, these are long gone.

If you do happen to stumble upon generic norbolethone, it likely stems from an underground laboratory. These pills come in 2.5 mg, 5 mg, and 10 mg forms.

Take this advice: Avoid it at all costs.

Although it is known to have a low tendency for aromatization and estrogen conversion, its use is so rare that we don't know as much about it as we do other steroids. It is also a weaker derivative of Deca-Durabolin, meaning that it possesses similar actions and side effects.

Since its beneficial effects mirror that of Deca, you probably won't be surprised to find that its side effects are similar too. These include: Erectile dysfunction, Liver problems, Water retention, Enlarged prostate, Loss of appetite, Depression, Acne, Low sperm count.

Description:
Effective Dose (Men): 10-15 mg/day
Effective Dose (Women): 5 mg/day
Half-Life: Approx. 8-10 Hours
Detection Time: Unknown
Anabolic/Androgenic Ratio: 350/17

Genabol, a.k.a. norbolethone, is a slightly weaker oral derivative of the anabolic steroid Deca-Durabolin, but possesses very similar actions. Genabol was never officially manufactured as a prescription medication, but was used for clinical trials in 2.5 mg tablets. Allegedly used during the 2000 Sydney Olympics, Genabol is believed to be presently available within both designer and black market circles in 2.5, 5, and 10 mg tablets.

Indications/Purpose & Side Effects:
For the Indications/Purpose & Side Effects of Genabol see the Deca-Durabolin profile.

First Reported Designer Steroid, Norbolethone
In 2002, Dr. Catlin was the first to report the use of a designer anabolic steroid in sport. He identified norbolethone (or norboletone) for the first time in an athlete's urine sample. Norbolethone had been developed in the 1960s as a treatment for growth and weight gain but was deemed harmful and never brought to market. Patrick Arnold and Victor Conte introduced it to athletes through the Bay Area Laboratory Co-operative (BALCO). Dr. Catlin's discovery of the substance was a wake-up call that some athletes were abusing designer steroids. The Chicago Tribune named Catlin Sportsman of the Year for 2002.

Designed in 1964 by Wyeth Laboratories in Philadelphia, PA, it is one of the oldest steroids, and was also not manufactured after design. In fact, Norbolethone was given in clinical trials over 30 years ago and never given the green light. No supply was ever manufactured, and no test was ever developed to detect this substance, yet ironically, it was suspected of being used in the 2000 Olympics based on blood and urine assays done by the IOC. Still, by the time testing was ready, athletes suspected of doping with it, had moved on. So where was the supply coming from, anyhow?

The mystery of Norbolethone is simple: When a steroid doesn't appear on a banned list, but does appear in the PDR, and there is no test in existence to detect it because it isn't in commercial production, a market is born. Loopholes in the world of sport and performance are rare and few since Congress began banning anabolic steroids, and laws began tightening the loop behind the mandate with each passing year. But just as a market develops quickly, so too does a test and a the appearance of a governing body to administer the test.

March 8, 2003: Drug Testers Have Designs on New Steroid:
Don Catlin did not detect anabolic steroids in the urine sample of a female athlete he analyzed last spring. Yet he believed they were present. The sample struck him as odd. Catlin, the director of the UCLA Olympic Analytical Laboratory in Los Angeles, had examined the urine of athletes in Olympic sports for years. Though this one did not show evidence of any of the dozens of steroids Catlin had been trained to identify, the levels of several natural hormones in the sample were strikingly low, almost nil. Catlin knew that anabolic steroids tend to suppress a person's production of natural steroids. That fact alone strongly suggested that an anabolic steroid had been used.

But where was the steroid?
Catlin's curiosity led to the discovery of what drug-testing officials refer to as a designer steroid - a drug that cannot be detected by standard drug tests - and it set off a search for the producer of the drug that has homed in on the lab of a renowned U.S. chemist, raised questions about how long the drug may have been used to beat drug tests and attracted the interest of federal investigators. A combination of research and detective work led Catlin and officials of the U.S. Anti-Doping Agency to the identification of an obscure but powerful steroid - known as norbolethone - in two samples of the athlete's urine after obtaining a sample of it from the chemical library of Wyeth Laboratories in Philadelphia. Wyeth studied norbolethone during the 1960s, as interest in the medical uses of synthetic steroids peaked, but it eventually abandoned the research and never marketed the drug. Norbolethone had never been found in an athlete's urine prior to Catlin's discovery.

"Discovering an unmarketed steroid last known to have been given to humans in a clinical trial 30 years ago raises an interesting question," Catlin wrote in the scientific paper on the discovery that appeared in Rapid Communications in Mass Spectrometry last May. "What is the source of this steroid today? It is quite unlikely that a supply of norbolethone remains from the few clinical studies conducted between 1964 and 1972. Thus, someone or some organization with synthetic chemical expertise could be preparing norbolethone." - https://www.washingtonpost.com/archive/sports/2003/03/08/drug-testers-have-designs-on-new-steroid/

Norbolethone is a 19-nor anabolic steroid first synthesized in 1966. During the 1960s it was administered to humans in efficacy studies concerned with short stature and underweight conditions. It has never been reported by doping control laboratories prior to 2001. Norbolethone was identified in two urine samples from one athlete by matching the mass spectra and chromatographic retention times with those of a reference standard. The samples also contained at least one likely metabolite. The samples were also unusual because the concentrations of endogenous steroids were exceptionally low. Since norbolethone is not known to be marketed by any pharmaceutical company, a clandestine source of norbolethone may exist. Norbolethone matches the description for what is described as a "designer steroid." Androgenic anabolic steroids (AAS) are defined as natural, synthetic or semi-synthetic drugs chemicals derived from testosterone, used with the aim to improve physical performance by increasing both muscle strength and mass. Despite their reported toxicological effects on the cardiovascular, hepatic and neuro-endocrine systems, the AAS have been extensively used in sports activities.

A synthetic and orally active anabolic - androgenic steroid which was never marketed. Norboletone was found to have been brought to the market by the chemist Patrick Arnold, of the Bay Area Laboratory Co-operative (BALCO), an American nutritional supplement company. It is reputed to have been the active ingredient in the original formulation of the "undetectable" steroid formulation known as "The Clear" before being replaced by the more potent drug tetrahydrogestrinone. Norboletone is on the World Anti-Doping Agency's list of prohibited substances, and is therefore banned from use in most major sports.

  
Anabolic agents: recent strategies for their detection and protection from inadvertent doping - Zeranol has been prohibited according to the regulations of WADA as an anabolic agent and its formation from zearalenone has been observed in humans, representing an analytical challenge for doping ...
Thursday March 13, 2014 - bjsm.bmj.com

Mass Spectrometry and Illicit Drug Testing: Analytical Challenges of the Anti-doping Laboratories - At present, the recourse to LC/MS-MS is progressively increasing among the WADA-accredited laboratories for a number of reasons, and not only to face the new challenges of doping analysis.
Sunday March 13, 2022 - medscape.com

  
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