Selegiline HCL

Selegiline (chemical name: L-Deprenyl, Brandnames: Eldepryl , Jumex, Zelapar, or veterinairy Anipryl

I believe nootropics like by example Selegiline Cabergoline and Bromocriptine are very underrated bodybuilding drugs.

The enzyme monoamine oxidase has two main forms, type A and type B. They are coded by separate genes. MAO may be inhibited with agents that act reversibly or irreversibly; and selectively or unselectively. These categories are not absolute.

MAO type-A preferentially deaminates serotonin and noradrenaline, and also non-selectively dopamine. Type B metabolises dopamine, phenylethylamine (the chocolate amphetamine) and various trace amines.

Selegiline is a MAO-B inhibitor (in regular doses), it inhibits the enzyme monoamine oxidase type B that oxidizes dopamine, as a result the user keeps a higher level of dopamine. Dopamine is an effective inhibitor of prolactin secretion. High prolactin causes low testosterone, lethargy, weak sex drive and erectile dysfunction. Elevated prolactin is an unwanted side-effect of some steroids, especially nandrolone (Deca) and trenbolone are blamed. This is an obvious reason why bodybuilders and other steroids using induviuals use it.

A surge in the hormone prolactin after sexual orgasm is the reason why men need a refractory period before they can go again. Selegiline as prolactin inhibitor counteracts this, thus it is obvious that selegeline is also used as a pro-sexual drug. Later in this blogpost more on that.

A Happy Active Bodybuilder

Selegeline has broad array of effects and as far as we know is relatively safe to use. It elevates dopamine thus increasing our mood, libido and daily energy. It is also used as a smart drug, a pro-sexual drug, as an anti-depressant and also protects the brain. For the bodybuilder it is extremely useful to fight the notorious post cycle depression.

Selegiline has been intensively researched over the past 50 years, and many hundreds of research papers on Selegiline have been published. So this blogpost is far from complete.

Selegiline has immune-system-boosting and anti-neurodegenerative effects. Its use increases the level of tyrosine hydroxylase, growth hormone, cerebral nitric oxide and the production of key interleukins. Selegiline offers protection against DNA damage and oxidative stress by hydroxyl and peroxyl radical trapping; and against excitotoxic damage from glutamate. In addition, selegiline stimulates the release of superoxide dismutase (SOD). SOD is a key enzyme which helps to quench damaging free-radicals.

First of all I want you to read some studies that produced some interesting results for bodybuilders and other lifters, but also for the health conscious and the older individual. What you should know is that Selegeline boosts Dopamine levels in the brain. Increases in Dopamine lead to an increase in Growth Hormone levels.

Some studies on increases of GH:

Effects of L-Deprenyl on Human Growth Hormone Secretion. Koulu et al

“The effects of L-deprenyl on L-dopa-, apomorphine- and L-tryptophan induced growth hormone (GH) secretion were studied in thirteen healthy male volunteers. An acute 10 mg dose of L-deprenyl did not stimulate the basal GH secretion. Short-term L-deprenyl premedication significantly enhanced the L-dopa-stimulated GH release.”

Stimulation of Human-Growth-Hormone Secretion by L-Dopa. Boyd et al

“The effect of L-dopa, a precursor of Central-nervous-system catecholamines, on growth-hormone secretion was studied in a group of patients with Parkinson's disease undergoing treatment with the drug. Oral doses (0.5 g) caused a significant rise in plasma growth hormone in patients initially starting therapy or on chronic therapy for as long as 11 months. The rise in plasma growth hormone persisted for 120 minutes after the administration of the drug. Furthermore, patients with Parkinson's disease, on L-dopa therapy, appear to be under the influence of elevated plasma growth hormone for a substantial part of the day.”

Deprenyl treatment restores serum insulin-like growth factor-I (IGF-I) levels in aged rats to young rat level. De la Cruz et al

“We studied the effects of treatment with (-)-deprenyl, a monoamine oxidase B inhibitor, on plasma levels of insulin-like growth factor-I (IGF-I) (as indicator of growth hormone (GH) secretion), levels of monoamines and their metabolites, and the activity and content of tyrosine hydroxylase - the rate-limiting enzyme in the biosynthesis of catecholamines - in the hypothalamus and hypophysis of old male rats. Male Wistar rats (22 months old) were treated with 2 mg deprenyl/kg body weight s.c. three times a week for 2 months.

Deprenyl treatment restored the IGF-I plasma levels in old rats to a concentration similar to those found in young animals. Postulated anti-aging effects of (-)-deprenyl could hence be due to restoration of hypothalamic hormones such as GH.”

L-deprenyl: nitric oxide production and dilation of cerebral blood vessels. Thomas et al

The monoamine oxidase-B inhibitor L-deprenyl (Selegiline) is effective in treating Parkinson’s disease and possibly Alzheimer’s disease. The neuroprotective property of L-deprenyl may be unrelated to the inhibition of monoamine oxidase-B. Since nitric oxide (NO) modulates activities including cerebral blood flow and memory, we examined the effect of L-deprenyl on NO. L-Deprenyl induced rapid increases in NO production in brain tissue and cerebral vessels. Vasodilation was produced by endothelial NO-dependent as well as NO-independent mechanisms in cerebral vessels. The drug also protected the vascular endothelium from the toxic effects of amyloid-beta peptide. These novel actions of selegiline may protect neurons from ischemic or oxidative damage and suggest new therapeutic applications for L-deprenyl in vascular and neurodegenerative diseases.

Increases maximum life span

Selegiline, which also works primarily on the dopamine system in the brain, has been shown to significantly increase both sex drive and maximum life span in aging laboratory animals, and many people have verified that at least the elevation in sex drive carries over into the human species. In addition to its aphrodisiac and life-extending properties, Selegiline has been shown to have antidepressant and cognitive enhancement effects as well.

Perhaps most significantly, Selegiline is the first pharmaceutical treatment to ever demonstrate an increase in the maximum lifespan of laboratory animals. This means that Selegiline can increase what is commonly referred to as “normal life expectancy,” in at least in one species of laboratory animals.

In several unprecedented experiments, rats showed as much as a forty percent increase in their maximum lifespans from Selegiline treatments, which is approximately equivalent to a human being living to be one hundred and seventy years of age.

In fact, all members of the placebo group were dead several weeks before the very first Selegiline -treated rat died. Interestingly enough, it was those animals that had the highest sex drives which lived the longest.Selegiline (Deprenyl) is currently available in the United States by prescription, and it is prescribed primarily for the treatment of Parkinson’s disease, depression, and Alzheimer’s disease. There are some contraindications and precautions that one should be aware of before experimenting with this substance. Some drugs, such as MAO inhibitors, should never be used in combination with Selegiline, and too much Selegiline can cause unpleasant, amphetamine-like symptoms. It is worth noting that while most antidepressants (such as Prozac and Zoloft) appear to inhibit sexual function for many people, Selegiline actually enhances it. I think that alone would make me less depressed.


John Morgenthaler, reveals in his book “Better Sex Through Chemistry” how to safely enhance one's sex life through nutrients and a new class of pharmaceuticals which they call "prosexual drugs" .

Smart drugs and prosexual drugs have a lot in common. Some of the prosexual substances, such as Deprenyl (Selegiline) and Bromocriptine have also been shown to increase intelligence, booster attention, and benefit memory consolidation. According to gerontologist and life extension researcher Ward Dean, M.D., "...anything that improves brain function is probably going to improve sexual functioning."

Selegiline is also extremely safe, remarkably free of side-effects, non-addictive, and in general improve overall health. This would have to be the case with any substance that improved sexual vitality over an extended period of time, as sex and health are intimately linked. So great is their connection that a healthy sex life is one of the primary indicators of overall good physical health.

Just read the discussion forums and you will find out that those that already like polypharmacy and are not afraid to experiment and want to look for the extreme also combine Selegiline with substances such as Cialis and Viagra.


The precipitous declindopamine-containing neurons in the human brain after age 45 e of is a universal characteristic of the aging process. The nigrostriatal region of the brain is richest in dopamine and undergoes the most rapid aging of any brain area. People whose brain nigrostriatal regions age prematurely develop symptoms of Parkinson’s disease, formerly called the shaking palsy. Age-associated depletion of dopamine also accounts for less noticeable symptoms, like decline in drives, most notably male sex drive

Unique Pharmacology of Selegiline

Selegiline (Deprenyl) provides selective protection against the age-related degeneration of the dopaminergic nervous system. It protects sensitive dopamine-containing neurons from the age-associated increases in glial cells (non-neuron brain cells) and the monoamine oxidase (type B) that they contain. Selegiline is the first selective inhibitor of MAO-B ever discovered, it is the only one used in clinical practice, and it remains the scientific reference standard for B-type inhibition after more than 40 years.

Selegiline also competitively inhibits the uptake of dopamine, norepinephrine and epinephrine (collectively referred to as catecholamines) into neurons. This unique ability among the MAO inhibitors prevents the “cheese effect,” a dangerous hypertensive reaction caused by neural uptake of tyramine from tyramine-containing foods like aged cheeses, certain wines, yeast, beans, chicken liver and herring. Selegiline exhibits no significant cheese effect at therapeutic dosages, and only minimal effects at extremely high dosages.

Variable Aging in the Brain

The rate at which dopamine neurons age is apparently quite variable. Prior to age 45, dopamine levels remain fairly stable. Starting at age 45, average dopamine content in healthy individuals decreases linearly 13% per decade. When it reaches approximately 30%, Parkinson symptoms result (gray area). Below 10%, death results. Although the average decrease in dopamine is 13% per decade, some individuals exhibit more rapid decline and others less rapid decline. People experiencing rapid dopamine decline manifest with Parkinson’s disease. Those with normal or slow decline (see illustration) die before Parkinson symptoms become apparent.

This model of nigrostriatal aging and the development of Parkinson’s disease has been advanced by Dr. Jozsef Knoll, the world’s most prominent deprenyl researcher. He suggests that Parkinsonism may be a generic condition of the human species that does not currently manifest in very many people because of our limited average lifespan. He also suggests a general strategy of long-term Selegiline use for the prevention of nigrostriatal aging in the above-45-year-old population.

Selegiline and Antioxidant Defenses

The sensitivity of the dopaminergic nervous system to oxidizing free radicals is well established. Oxidative polymerization of aromatic amino acids (e.g., phenylalanine, tyrosine, dopa, tryptophan) and aromatic monoamine neurotransmitters (e.g., norepinephrine, epinephrine, dopamine and serotonin) lead to the formation of melanin, a black pigment which is a characterizing feature of the nigrostriatal (black-striped) neurons. Chronic deprenyl treatment lessens the rate of melanin production.

Two oxidized derivatives of dopa and dopamine (6-hydroxydopa and 6-hydroxydopamine, respectively) are potent neurotoxins. The protective effect of Selegiline in lessening the neurotoxic effect of these two chemicals appears to correlate with increased antioxidant enzyme levels, superoxide dismutase (SOD) [Knoll, 1989] and catalase [Carrillo, 1991]. The increase in antioxidant enzymes is proportional to the amount of Selegiline given. The protective influence of deprenyl is selective for dopaminergic neurons; increased SOD is not noted throughout the rest of the brain.

Life Extension and Cognitive Enhancement

Although the long-term use of Selegiline in normal people as a life-extension and cognitive-enhancing drug has yet to be definitively studied, animal research is extensive. Age-associated decrease in sexual performance and hunger drive in rodents (a dopaminergic function) is dramatically inhibited.

The lifespan studies of Selegiline in rodents is equally dramatic all of the control rats die before the first Selegiline -treated rat dies.

The life-extending influence of Selegiline is not mediated through a food-restriction mechanism. Selegiline -treated animals maintain body weight better than control animals.

Early research with Selegiline in humans (early diagnosed Parkinson patients) shows delayed development of symptoms and delayed need for L-dopa therapy. In combination with other drugs, Selegiline has significantly prolonged the survival of Parkinson patients.


Selegiline’s low level of toxicity, few side-effects, and unique spectrum of pharmacological activities make it ideal for prophylaxis against nigrostriatal aging and the secondary aging symptoms accompanying the decline of the dopaminergic nervous system. Selegiline is a drug of choice for Parkinson’s disease and is currently being established as a treatment for Alzheimer’s disease. Eventually, Selegiline may become recognized as a general treatment for aging in the above-45-year-old population.


There may be considerable individual variation in what dose is optimal. This is also depended on age, body weight etc.

As someone on a discussionboard wrote: “ I take 2.5mg three times a week. I am guided partly by the effect on my mood. If I take full 5mg pill, I can feel a little lightheadedness, like a sugar high. I don’t feel anything from 2.5mg.” Another one wrote: “Selegiline only needs 2.5mg ED (or EOD if you are sensitive) to create a pleasant lift in daily energy, mood, libido, etc.”

Some drugs, such as other MAO inhibitors, should never be used in combination with Selegiline, and too much Selegiline can cause unpleasant, amphetamine-like symptoms.

A Japanese study revealed that doses over 0.5 mg/kg in mice shortened life-span while at or below 0.5 mg increased life-span. To put this in context, there is lots of room between 0.5mg/kg and usual doses of Selegiline in humans. Typical doses used in the life extension community are 0.05 or 0.20 mg/kg of bodyweight, which are much smaller than the dose that causes shortened life span in mice.

Both Dr. Joseph Knoll and the Life Extension Foundation recommend a 10-15 mg weekly (i.e. 1.5 - 2 mg/day) oral Selegiline dosage for humans, starting around age 40, possibly even in the 30s. 10 mg/day is a relatively standard Selegiline dose for treatment of PD and AD, but this higher dose should only be used with medical supervision. Some Selegiline experts believe this dosage is excessive, and that with long term Selegiline use lower doses may still be effective and safer. Knoll has noted that the human MAO-B inhibiting Selegiline dose ranges from 0.05 to 0.20 mg/kg of bodyweight. Thus, even in those wishing to use Selegiline at an effective MAO-B inhibiting dose, it should not be necessary to use more than 3-5 mg/day. Because Selegiline is a potent and irreversible MAO-B inhibitor, it may even turn out in many individuals that the suggested 1.5-2 mg/day life extension Selegiline dose may achieve MAO-B inhibition with long term use.

Selegiline is reported in most human studies to be well tolerated. Typically, no abnormalities are noted in blood pressure, laboratory valves, ECG or EEG. The most common side effects reported for Selegiline are gastrointestinal symptoms, such as nausea, heartburn, upset stomach, etc. Some studies have found side effects such as irritability, hyper-excitability, psychomotor agitation, and insomnia. These effects are probably due to Selegilines catecholamine-enhancing effect, over-activating DA/NA neural systems at the expense of calming/sleep-inducing serotonergic systems, so taking magnesium and tryptophan or 5-HTP may suffice to counter these psychic effects.

Healthy individuals looking at Selegiline for life-extension purposes are advised moderate doses. Over the long term, proper dosage appears to be a crucial factor and research is underway to pin-point optimum dosage. Very high doses are not advised for healthy people. Life-extensionists have understandably had a difficult time trying to determine what dose would be optimal for a human seeking the life-extension and neuroprotective benefits of Selegiline.

Dosages in excess of 20-30 mg/day could create high blood pressure problems by MAO-A inhibition. Dosages in the 10 mg/day range would reduce the oxidation stress of the breakdown products of dopamine metabolized by MAO-B, but the resulting elevated dopamine levels might not be desirable. Selegiline binds to MAO-B irreversibly, and it takes 2 weeks for MAO-B levels to return to normal. A single 5 mg dose can cause 86% MAO-B inhibition within 2-4 hours. Inhibition remains at 90% for 5 days, and does not return to baseline for 2 weeks. Selegiline induction of enzyme synthesis (including, presumably, anti-oxidant enzymes) can take place at levels below those required for MAO-B inhibition [*21].

Therefore, a dose in the range of 1 mg/day might be optimal for a 40-year-old 170-pound person. Twice-weekly dosing has been based on the fact that Selegiline binds MAO-B irreversibly. But more frequent dosing might be better for steady induction of enzyme synthesis.

Aside from body weight, age is a very important consideration. As a person gets older, neurons decrease in number while glial cells (which synthesize MAO-B) increase — meaning that MAO-B levels increase with age. This may be the reason that dopamine content of the striatum (caudate nucleus) typically decreases by 13% per decade after age 45. A person over 45 would want to counteract the excessive MAO-B in a dose proportional to his or her age. This could mean up to 5 mg daily for an elderly person with no symptoms of Parkinson's Disease or Alzheimer's Disease. Selegiline has been shown to produce vasodilation by rapid increase in nitric oxide production and to protect the vascular endothelium from the toxic effects of amyloid-beta peptide.

Whether or not Selegiline can extend maximum lifespan, there is reason to believe that it can extend mean lifespan and protect from neurodegenerative disease.