Benefits of each Compound

What is Endorphinol®?

Endorphinol® refers to a blend of specialized amino acids which increase the levels of pain & mood modulating endorphins in laboratory animals and humans and thus provide an effective, non-addictive and natural substance for relief from pain, depression and anxiety. A lot of the pioneering work on these natural compounds was carried out in the early 1980’s by Dr. Ehrenpreis and his colleagues at Chicago Medical School. Much of this research focused on the pain-relieving properties of D-phenylalanine (DPA). Unlike narcotics such as morphine and codeine, DPA is not addictive and users don’t build up a tolerance to it. It also quells inflammation. 

Other endorphinols such as L-leucine and hydrocinnamic acid were discovered later on.  These natural sources of pain relief work together to confer greater pain-killing punch.  They also increase the effectiveness of other analgesics including anti-inflammatory drugs such as aspirin, Ibuprofen, Darvon, Codeine, acetaminophen, etc.

How does Endorphinol® work?

Endorphins are natural chemicals that improve mood, immune function, memory and physical endurance and reduce pain, anxiety and depression.  Two of the enzymes that are involved in the breakdown of endorphins and enkephalins are carboxypeptidase A and leucine aminopeptidase.   The enzymatic breakdown of endorphins and enkephalins results in a decrease in the time users experience pain relief.  However, the DPA in Endorphinol® keeps these enzymes from destroying these endorphins and enkephalins.  This blocking action keeps the pain and inflammation-modulating compounds around which translates into longer periods of being pain-free.  D- and DL-phenylalanine are among the most potent natural analgesics tested thus far, with D-phenylalanine being the more pure form. ¹ 

How effective are the ingredients in Endorphinol®?

In lab animals and patient use, the combination of DL-phenylalanine, DL-Leucine and hydrocinnamic acid provide greater pain relief benefits than did any one of these compounds by itself.  This combination also appeared to be as effective as morphine in some instances.

In Dr. Ehrenpreis’ research, both D- and DL-phenylalanine was administered to 47 subjects.  Four of these subjects suffered from acute pain and 43 suffered from chronic pain.   A pain-killing effect was observed in 28 (60%) of the subjects. 

It should be noted that DLPA also shown benefit in Parkinson’s Disease and depression. ¹

Are there side effects from the compounds in Endorphinol®? 

When 3 grams per kg (2.2. lbs) of body weight of DPA was given daily for several weeks to young or adult Swiss albino mice, there were no behavioral or adverse nervous system changes reported.  There were also no detectable microscopic changes in the animals’ heart, liver, kidney, pancreas or spleen.   In fact, no mice or rats ever died from doses up to 3 grams per kg of body weight. 

When 500 mg per kg of body weight of DPA was given intravenously to dogs and rabbits, there was no change in blood pressure or heart rate.  Two to four grams of DPA taken orally by human subjects also produced no symptoms of toxicity.  When 1 gram per day of DPA was given for 5 weeks to subjects with chronic pain, two out of 43 subjects showed rashes and less than 1% reported minor gastrointestinal tract disturbances, including nausea, diarrhea and constipation.    These reactions were quickly reversed by stopping the DPA. 

The researchers concluded that DPLA produced little or no toxic reactions, even in high doses, in people.¹

Additional Information on the compounds in Endorphinol®:

D- and DL-Phenylalanine

¹ Ehrenpreis, S.  D-Phenylalanine: Animal and Human Pharmacology, with Emphasis on Analgesic Activity.  Chicago Medical School, Chicago, Il.   (Case Studies)

1) Burning pain in right hand – partial relief with DPA and codeine for 4 weeks.

2) Pain in left face for 20 years – good to excellent relief in the 2^nd and 3^rd week with DPA 20 mg and 2 aspirin tablets.

3) Low back pain - DPA 200 mg diminished pain and can lower Dilaudid intake.

4) Low back pain with osteroarthritis – excellent results with DPA.  No longer takes Percodan.

Russell AL, McCarty MF.  DL-phenylalanine markedly potentiates opiate analgesia – an example of nutrient/pharmaceutical up-regulation of the endogenous analgesia system.  Med Hypotheses 2000, 55(4): 283-8.

Treatment with DL-phenylalanine (DLPA)  potentiates pain relief and eases depression in patients receiving opiates for chronic non-malignant pain.

Kitade T, Odahara Y, Shinohara S, Ikeuchi T, Sakai T, Morikawa K, Minamikawa M, Toyota S, Kawachi A, Hyodo M, et al.  Studies on the enhanced effect of acupuncture analgesia and acupuncture anesthesia by D-phenylalanine (2^nd report) – schedule of administration and clinical effects in low back pain and tooth extraction.  Acupunct Electrother Res 1990; 15(2): 121-35.

Thirty patients with chronic low back pain were 4 grams of DPA followed by 30 minutes of acupuncture.  Seven cases reported excellent results, 11 reported good results, 6 reported fair results and 6 reported poor results.  With 18 patients undergoing tooth extraction with 4 grams of DPA followed by acupuncture anesthesia, 8 subjects reported excellent results, 6 reported good results, 3 reported fair results and 1 reported poor results.  In a study comparing administering DPA one day before or 30 minutes before treatment, the one day before group showed better results.

Kitade T, Odahara Y, Shinohara S, Ikeuchi T, sakai T, Morikawa K, Minamikawa M, Toyota S, Kawachi A, Hyodo M, et al.  Studies on the enhanced effect of acupuncture analgesia and acupuncture anesthesia by D-phenylalanine (first report) – effect on pain threshold and inhibition by naloxone.  Acupunct Electrother Res 1998, 13(22-3): 87-97.

DPA enhances the analgesic effect of acupuncture by the “endorphin mechanism

Ehrenpreis, S.  D-phenylalanine and other enkephalinase inhibitors as pharmacological agents: implications for some important therapeutic application. Acupunct Electrother Res 1982, 7(2-3): 157-72.

D-phenylalanine has proven to be beneficial in many human patients with chronic, intractable pain.  Dr. Ehrenpreis proposes that enkephalinase inhibitors may be effective in a number of human “endorphin deficiency diseases” such as depression, schizophrenia, convulsive disorders and arthritis.  D-phenylalanine may also alleviate other conditions associated with decreased endorphin levels such as opiate withdrawal symptoms.

Fischer E, Heller B, Nachon M, Spatz H.  Therapy of depression by phenylalanine.  Preliminary note.  Arzneimittelforschung 1975, 25(1): 132.

Twenty-three subjects with endogenous depression had been treated unsuccessfully with antidepressive drugs.  D- or DL-phenylalanine was given in daily oral doses of 50 or 100 mg for 15 days.   The treatment was effective in 17 subjects between day one and day 13.  No significant adverse reactions were observed.

D- and DL-Leucine:

Cheng RS, Pomeranz B.  A combined treatment with D-amino acids and electroacupuncture produces a greater analgesia than either treatment alone: naloxone reverses these effects.  Pain 1980, 8(2): 231-6.

The D-amino acids D-phenylalanine and D-leucine produce analgesia.  Electroacupuncture also produces analgesia.  62% of mice showed analgesia by electroacupuncture, 53% showed analgesia by D-phenylalanine and D-leucine and 80% of the mice showed marked analgesia with both treatments.  Combining the two treatments produces an addictive effect, creating greater analgesia than that produced by either treatment given alone. 

Hydrocinnamic Acid:

Giusti P, Carrara M, Cima L, Borin G.  Antino-ciceptive effect of some carboxypeptidase A inhibitors in comparison with D-phenylalanine.  Eur J Pharmacol 1985, 116(3): 287-92.

D-phenylalanine and hydrocinnamic acid are two in vitro inhibitors of carboxypeptidase A and have analgesic action when injected i.p. in mice.