2,4-Dinitrophenol (DNP),is a cellular metabolic poison. It uncouples oxidative phosphorylation by carrying protons across the mitochondrial membrane, leading to a rapid consumption of energy without generation of ATP.
Dinitrophenols as a class of compounds, of which there are six members, do not occur naturally but are all manufactured compounds.

2,4-DNP is a yellow solid with no smell. It is used in making dyes, wood preservatives, explosives, insect control substances, and other chemicals, and as a photographic developer.
It was used in diet pills in the 1930s but was banned for this use in 1938. It may be sold under several trade names, including Caswell No. 392, Sulfo Black B, and Nitro Kleenup. Use of trade names is for identification only and does not imply endorsement by the Agency for Toxic Substances and Disease Registry, the Public Health Service, or the U.S. Department of Health and Human Services.

Hystory of 2,4-DNP

Competitive bodybuilders and many others are continually on a quest for leanness. Used by the hardcore since Dan Duchaine’s reporting of it a couple years ago, DNP (2,4-Dinitrophenol) has managed to steadily gain popularity as a powerful tool for weight loss. Interestingly, DNP was first used to ignite TNT in the early 1900’s. In 1931 a study released by Stanford University declared that DNP was able to cause amazing weight loss; subsequently it found its way into many diet potions and medications; regulation was much less strict during this time than the present, and many of these products were available over the counter. Two years later DNP was banned by the FDA as a dieting agent due to its inclusion in many OTC dietary supplements. The FDA was a new organization at this time and acted in a rather brazen manner, with the absence of any set procedures for taking substances off the market. Granted, there was only a 1% incidence of cataracts over a large population (around 100,000); nonetheless it happened (although interestingly, exclusively women). However, there are now ways to counter this which will be covered thoroughly.
The comparisons to the current drugs used for dieting are astounding, at least in terms of thermogenesis. While the ECA stack has been shown to provide approximately a 3% increase in metabolic rate, DNP can deliver a relatively controlled 50% elevation in resting metabolic rate. The thermogenic aspect of clenbuterol, while sometimes overestimated due to the high CNS stimulation that yields a “wired” feeling, can vary according to prior exposure to various amphetamine-like compounds and certainly is not much greater than that of ECA. DNP does not have the anorectic effects of ephedrine or other thermogenic agents; rather, it tends to increase hunger, particularly appetite for carbohydrates. This problem is easily solved with appetite suppressants, and one may even use ECA itself for this purpose while on DNP.

Pharmacological action of 2,4-DNP

DNP accomplishes the astounding boost in metabolic rate via inhibition of the F0F1 ATP synthase molecule, located in the inner wall of each mitochondrion. While the electron transport chain still functions to pump hydrogen ions into the intermembrane space, the coupling of the proton gradient to ATP production is rendered impossible by DNP. As a result, ATP production is dramatically reduced, and the energy is instead thrown off as heat. This results in an astounding production of heat; when using dinitrophenol, the athlete will radiate so much heat that it is uncomfortable to be within any proximity of them. Luckily, this heat does not fully contribute to body temperature increases, and is instead thrown off from the entire body surface, particularly the head. As a result, adequate doses of DNP will usually only elevate body temperature by about 1-1.5ºC. This is a good thing for your central nervous system and other delicate tissues; if the heat produced by ATP contributed in a more direct matter to body temperature, effective doses for fat loss would cause supraphysiological body temperature increases on a level unwitnessed at this time. Nonetheless, overheating is a very real danger; this and other side effects shall be addressed.
Concerns about dangerous side-effects and rapidly developing cataracts resulted in DNP being discontinued in the United States by the end of 1938. DNP, however, continues to be used by some bodybuilders and athletes to rapidly lose body fat. Fatal overdoses are rare, but are still reported on occasion.
While DNP itself is considered by many to be too risky for human use, its mechanism of action remains under investigation as a potential approach for treating obesity. Currently, research is being conducted on uncoupling proteins naturally found in humans.

Risks and Side Effects of using 2,4-DNP

Hearing all of these wonderful things probably has you wondering what the side effects and risks are. They are quite formidable and contribute to making DNP one of the most intolerable (though effective) drugs used in bodybuilding. Starting with the most significant, and descending in importance, are the following risks and side effects of DNP use.

Risks:

  1. Overheating - There is no upper limit to DNP’s body temperature increase, meaning that one may literally “cook from the inside” if they take too much. Dosage considerations will be given later, but even an overdose of 4-6 times the recommended dosage may be lethal. Much smaller overdoses may result in damage to the brain and/or other body systems.
  2. Carcinogenesis - Phenols in general are reputed to be carcinogenic. Although 2,4-dinitrophenol has never been implicated in a cancer diagnosis, some are nonetheless concerned, and understandably so. In addition to the inherent carcinogenic potential caused by its status as a phenol, production of free radicals and the release of various compounds stored in adipose tissue stores during DNP’s rapid oxidation of fat may also potentially be harmful.
  3. Death - This is self-explanatory and has occurred with several bodybuilders who chose to use this compound.

Side Effects:

  1. Discomfort and sweating - This is the single most noticeable effect of DNP use, both by the user and those around him/her. Even in the winter, while indoors at ambient temperatures, one may expect his or her shirt to be completely soaked through with sweat. Those with jobs requiring formal or semi-formal apparel are advised to consider other means of fat loss (or a new job, if preferred). Other obvious considerations lie in the areas of social life, personal appearance, etc. and the user must prioritize.
  2. Insomnia - Second in frequency of reports to sweating and discomfort is insomnia; this may be at least partially attributed to discomfort. Possible means of countering this include such supplements as Valerian root or melatonin. Alternatively, one may deal with this via prescription or OTC sleep medications or GHB-A precursors. However, these may be addictive if used on a regular basis and if their use may be avoided, by all means abstain from using them.
  3. Yellow bodily fluids - Some don’t notice this, but others find that all of their bodily fluids take on a yellowish appearance. Urine is a darker yellow, and even semen and vaginal secretions may be affected. According to current knowledge, this is not known to be harmful in and of itself.
  4. Muscle Soreness - This is yet another thing that may be minimized via cerebral function. Dan Duchaine has recommended using a weight such as to allow no fewer than 15 reps per set of any weight training workout; judging from anecdotal reports and personal experience, this seems to be good advice. Low levels of ATP are a cause of muscle soreness in and of itself; the additional factor of encumbered recovery mechanisms make extreme soreness (and if not careful, catabolism) quite possible.
  5. Allergic Reactions – These are highly individualized but may be summarily discussed. Various reactions are common with DNP use, and approximately 10% of users will be extremely allergic to it. Allergic reactions can include hives, blisters, and/or inexplicable rashes. If you suffer any of these side effects, and they are extremely bothersome, it is the recommendation of the author to cease usage immediately. If so desired, another trial may be made at a later date with a lower dosage, but do not attempt to continue the drug cycle at that point.
  6. Carbohydrate Cravings - To counter this, some methods will be touched on later. As with most diets, willpower is sometimes the single most important factor.

Sources and emissions

Sources

Sources of 2,4-dinitrophenol include manufacturing plants, mines, foundries, metal, petroleum, and dye manufacturing plants which use 2,4-dinitrophenol. It is used as a wood preservative, indicator, reagent, chemical intermediate for production of azo dyes, and in the manufacturing of photographic developers (HSDB, 1991). 2,4-Dinitrophenol is also found in motor vehicle exhaust. It also may form as a result of photochemical reaction between benzene and nitrogen monoxide in polluted air (Howard, 1990).
2,4-Dinitrophenol was registered for use as a pesticide, however as of December 31, 1991, it is no longer registered for pesticidal use in California (DPR, 1996).

Emissions

No emissions of 2,4-dinitrophenol from stationary sources in California were reported, based on data obtained from the Air Toxics “Hot Spots” Program (AB 2588) (ARB, 1997b).

Natural Occurrence

No information about the natural occurrence of 2,4-dinitrophenol was found in the readily-available literature.

Ambient concentrations

No Air Resources Board data exist for ambient measurements of 2,4-dinitrophenol.

Indoor sources and concentrations

No information about the indoor sources and concentrations of 2,4-dinitrophenol was found in the readily-available literature.

Atmospheric persistence

In the atmosphere, 2,4-dinitrophenol may exist in the gaseous or particulate form. It may be removed by direct photolysis, by settling or washout in precipitation, or it may react in the gas-phase with photochemically-produced hydroxyl radicals (Howard, 1990). Based on the hydroxyl radical rate constant for 2-nitrophenol, the calculated half-life of 2-nitrophenol, due to reaction with hydroxyl radicals, is estimated to be 11 days. 2,4-Dinitrophenol is expected to be less reactive than 2-nitrophenol. 2,4-Dinitrophenol is therefore expected to be removed from the atmosphere by direct photolysis and/or wet and dry deposition (Atkinson, 1995).
2,4-Dinitrophenol emissions are not reported from stationary sources in California under the AB 2588 program. It is also not listed in the California Air Pollution Control Officers Association Air Toxics “Hot Spots” Program Revised 1992 Risk Assessment Guidelines as having health values (cancer or non-cancer) for use in risk assessments (CAPCOA, 1993).

How can dinitrophenols affect my health if I don’t use?

Most of the information on the health effects of dinitrophenols comes from old studies of patients who were prescribed diet pills containing dinitrophenol before it was banned.
Deaths have occurred in people who ingested 3-46 milligrams of dinitrophenols per kilogram of body weight per day (3-46 mg/kg/day) for short periods, or 1-4 mg/kg/day for long periods. Also, people who breathed air containing 40 mg dinitrophenols per cubic meter of air (40 mg/m3) for long periods have died.
The amount of dinitrophenols ingested that causes harmful effects varies among people. Increased basal metabolic rate (the rate that you use energy at complete rest), increased sweating, a feeling of warmth, weight loss, and increased heart rate, breathing rate, and body temperature have been observed in people who swallowed as little as 1 mg/kg/day or as much as 46 mg/kg/day for short or long periods of time.
Ingesting 2-4 mg/kg/day DNP for short or long periods has caused cataracts in some people, while ingesting 1-4 mg/kg/day for short or long periods has caused skin rashes and decreases in white blood cells.

How likely are dinitrophenols to cause cancer?

The Department of Health and Human Services (DHHS), the International Agency for Research on Cancer (IARC), and the EPA have not classified dinitrophenols for carcinogenicity.
There are no studies available in people or animals on the carcinogenic effects of dinitrophenols.

Sources: wikipedia, mesomorphosis, agency for toxic substances and disease registry

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