Endorphins are the body’s natural pain killers and mood boosters. Ever wonder why exercise can make even the toughest patient feel so great? It is partially due to the fact that the body releases endorphins which block pain signals and inhibit GABA release in the nervous system, which in turn increases dopamine release. Beta-endorphins (one of the main endorphins in the central and peripheral nervous system) are synthesized in the anterior pituitary gland from their precursor, proopiomelanocortin (POMC). POMC is created in the anterior pituitary gland via corticotropin-releasing hormone (CRH) stimulation from the hypothalamus. CRH also increases levels of cortisol, which is the body’s main stress hormone. Whenever the body encounters stress, it upregulates the production of endorphins via the CRH pathway . Exercise can directly increase CRH release . Thus, exercise can indirectly increase endorphin release.
Unfortunately, in today’s fast-paced society, most cannot afford to exercise for long periods of time in order manage pain and stabilize mood. One amino acid that has shown promise as an endorphin promotor is D-phenylalanine. L-phenylalanine is the precursor to tyrosine, which is the precursor to dopamine. L-phenylalanine is naturally occurring and is found in proteins, while D-phenylalanine must be formed in a laboratory . It is postulated that D-phenylalanine helps prevent the degradation of endorphins through inhibition of the enkephalinase enzyme, which is responsible for metabolizing certain endorphins. When enkephalinase is inhibited, some endorphins are left intact for longer periods of time. One study showed D-phenylalanine to lower plasma levels of enkephalinase in human subjects . Another study showed D-phenylalanine to produce analgesia in horses . Furthermore, one study observed greater compliance in patients taking Trexan (for rapidly detoxifying methadone usage) when D-phenylalanine and other amino acids were administered in conjunction with the medication, as opposed to Trexan monotherapy .
Taken together, these studies support the theory that D-phenylalanine can help prevent the breakdown of endogenous endorphins by inhibiting the enkephalinase enzyme. Consider supplementing D-phenylalanine to potentially assist in improving feelings of pain and depression. Procite-D, a Targeted Nutritional Therapy formula by Sanesco, contains 100 mg of DL-Phenylalanine. However, it is recommended to measure neurotransmitter levels before starting Procite-D, as it contains other ingredients for catecholamine support. If your patient’s catecholamine levels are high, it may be best to administer a supplement which contains only D-phenylalanine.
1. Sprouse-Blum, A. S., Smith, G., Sugai, D., & Parsa, F. (2010, March). Understanding Endorphins and Their Importance in Pain Management. Hawaii Med J, 69(3), 70-71.
2. Inder, W., Hellemans, J., Swanney, M., Prickett, T., & Donald, R. (1998, September). Prolonged exercise increases peripheral plasma ACTH, CRH, and AVP in male athletes. Journal of Applied Physiology, 85(3), 835-841.
3. Phenylalanine. (n.d.). University of Maryland Medical Center. Retrieved Dec. 5th 2016 , from http://umm.edu/health/medical/altmed/supplement/phenylalanine
4. Marcello, F., Grazia, S. M., Sergio, M., & Federigo, S. (1986). Pharmacological “Enkephalinase” Inhibition in Man [Abstract]. Adv Exp Med Biol, 198(Pt B), 153-160. doi:10.1007/978-1-4757-0154-8_19
5. McKibbin, L. S., & Cheng, R. S. S. (1982). Systemic D-Phenylalanine and D-Leucine for Effective Treatment of Pain in the Horse. The Canadian Veterinary Journal, 23(2), 39–40.
6. Chen, T., Blum, K., Payte, J. T., Schoolfield, J., Hopper, D., Stanford, M., & Braverman, E. R. (2004). Narcotic antagonists in drug dependence: Pilot study showing enhancement of compliance with SYN-10, amino-acid precursors and enkephalinase inhibition therapy. Medical Hypotheses, 63(3), 538-548. doi:10.1016/s0306-9877(04)00194-x