presentation on Endorphin hormone


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Endorphin a natural analgesic and pleasant hormone

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  • Endorphin belong to class of enkephalin.
  • POMC processing in anterior pituitary gland
  • Heroin one thousand times more powerful and potent than morphine. It also used endorphin receptor site For binding.It caused drug addiction more than others.
  • presentation on Endorphin hormone

    2. 2. 2 Endorphins "endogenous morphine" Beta-endorphin the best in pain relief Endorphins production is hereditary, and due to this, its production level varies from one person to another. High concentrations of endorphins in the brain produce a sense of euphoria, enhance pleasure, and suppress pain, both emotionally and physically. Low concentrations of endorphins in the brain people feel anxious and they are also more aware of pain.
    3. 3. OVERVIEW OF PRESENTATION 1) History 2) What is Endorphin 3) Types of Endorphin 4) Control of Secretion 5) Transport and distribution 6) Receptors of endorphin 7) Binding: endorphin and receptor 8) Function as analgesic 9) Mode of action 10)Can we get endorphin ? 11)Abnormalities of endorphin receptors 12)Receptors used by exogenous opioid (morphine) 13)what is drug addiction ? 14)Can Methadone Fix to endorphin Receptors? 15)Future of endorphin’s and other’s receptors
    4. 4. HISTORY  In 1970’s that many research allowed us to understand how the exogenous opioid drugs work by studying the “endogenous opioid system”.  In 1973, H. Solomon Snyder and Johns hopkins discovered the “endogenous opioid system”. Researchers also determined the existence of opiate binding sites in the brain through the use of radioligand binding assays.  In 1974, Rabi Simantov and Solomon H. Snyder isolated endogenous opioid from the brain of a calf , and term is given "endorphin" (i.e. Endogenous morphine).  In 1975, an endogenous opiate-like factor called enkephalin was found and shortly after this two more classes of endogenous opiate peptides were isolated, the dynophorins and the “endorphins”.
    5. 5. WHAT IS ENDORPHIN? A peptide hormone named Endorphin produced in the brain and anterior pituitary. Endorphin inhibits pain perception. It is popularly called Body’s natural analgesic or opiate. Endorphin is produced at the time of physical or emotional stress, such as labor of child birth. Endorphin binds to the same receptors that binds exogenous opiates. “Endorphin Affect Your Mood And Emotions And May Be Responsible For Your Body Feeling Pleasure Even Euphoria For Your Body Feeling Pleasure”
    6. 6. alpha (α) endorphin - beta (β) endorphin Most powerful gamma (γ) endorphin - sigma (σ) endorphin - TYPES OF ENDORPHIN Human body produces at least 20 different endorphins ( benefits and uses are investigating) Special types are as follows: (made all by 16 to 31 amino acids )
    7. 7. β -ENDORPHIN • β -Endorphin is peptide hormones (consist of chains of amino acids) ----NH2 / NH3 + COOH • β -Endorphin is a 31 amino acid polypeptide • SEQUENCE: Ac - Tyr - Gly - Gly - Phe - Met - Thr - Ser - Glu - Lys - Ser - Gln - Thr - Pro - Leu - Val - Thr - Leu - Phe - Lys - Asn - Ala - Ile - Ile - Lys - Asn - Ala – His - Lys - Lys - Gly - Gln – OH • β-endorphin is released by pituitary (into blood ) and hypothalamus ( into the spinal cord and brain ) • β-endorphin is a cleavage product of pro- opiomelanocortin (POMC)
    8. 8. Hypothalamus Corticotropin releasing factor (CRF) Anterior Pituitary Pro-Opiomelanocortin (POMC) Endorphin Hormone (EP) Central Nervous System Environmental Cue “Stressor” ( pain) •Step 1: Cue perceived by CNS •Step 2: Signal sent to hypothalamus (in brain) •Step 3: Hypothalamus secretes CRF (peptide), travels to pituitary •Step 4: CRF causes protein pro-Opiomelanocortin hormone (POMC) to be cleaved, releases Beta lipotropin •Step 5: lipotropin gets convert into Endorphin. •Step 6: Endorphin binds to the nerve fiber. Brain Beta-lipotropin
    9. 9. ENDORPHIN HORMONE : AS CLEAVAGE PRODUCT pro-opiomelanocortin polypeptide (POMC) ACTH b-lipotropin g-MSH g-lipotropina-MSH CLIP b-endorphin b-MSH MET-enk
    10. 10. RECEPTORS OF ENDORPHIN • All of the endorphins bind to the opioid receptors in the brain. • These analgesia- producing receptors are located in your brain, spinal cord, and other nerve endings. Mu ( ) Receptor Analgesic (most important ) Delta( ) Receptor Analgesic (predominantly ) Kappa () Receptor Analgesic (hyper- analgesic )
    11. 11. TRANSPORT AND DISTRIBUTION  β-endorphin is released by : 1. Pituitary (into blood ) and 2. Hypothalamus ( into the spinal cord and brain )  Beta endorphin containing nerve fibres spread widely from neurones in the hypothalamus, to make inhibitory contacts with target neurones to reduce pain. Free hormones are rapidly eliminated from circulation through kidney or liver. Hypothalamus
    12. 12. An Easy Way to Think of Receptors and Endorphins binding • Is to think of the substance as a key and the receptor as a lock. • When the substance binds to the receptor it opens the lock. • This in turn sends another signal or causes the release of a substance. • When a lot of signals are sent a function happens like the release of a hormone.
    13. 13. BINDING OF ENDORPHIN & RECEPTOR  Portion of molecule Where ligand binds Is called binding site.  If the molecule Is a receptor (like in a cell membrane) the binding site is called receptor site.  The purpose of binding to target tissue is to elicit a response by the target cell.
    14. 14. FUNCTION AS ANALGESIC Pain impulse feel Pain impulse stop
    15. 15. Before endorphin release After endorphin release FUNCTION AS ANALGESIC PAIN IMPULSE STOP BY ENDORPHIN : MECHANISM hypothalamus
    17. 17. MODE OF ACTION The mu receptor is the strongest binding site of the body’s natural pain killer, the class of opioid peptides called the endorphin. The mu receptor is a G-protein linked receptor. When endorphin binds to the delta receptor is induces a conformational change that causes the activation of a specific G-protein. This G-protein inhibits the membrane bound enzyme adenylate cyclase and prevents the synthesis of cAMP.  The transmission of the pain signal requires cAMP to act as a secondary messenger, and so inhibition of this enzyme blocks the signal . (Pain-relieving effect by blocking the release of substance P) Adenylcyclase Endorphin ATP cAMP AMP
    18. 18. 18 Calcium channels closed Potassium channels open K+ AC Gi [cAMP] Calciumentry blocked [Ca2+] Decreased release of neurotransmitters Endorphin Receptor 2. Directaction on K channels (alpha & beta subunit) Net effects: K+ conductance hyperpolarize neurons Ca+ conductance neurotransmitter release 1. Couple to Gi & Go protein (neuronal excitability) Pain reduced MODE OF ACTION
    19. 19. CAN WE GET ENDORPHIN ? Yes we can get : BY Chili Runner’s high Exercise Music Laughing Meditation Acupuncture
    20. 20. ABNORMALITIES OF ENDORPHIN RECEPTORS However with some people : When the lock (receptor) is damaged. No matter how much Endorphins may be near the receptor because it does not function right the lock can not be opened. By Genetics/Birth Defect A person can be born with defective receptors. This can make an individual more susceptible to addiction By Exogenous drug And using opiates - not for pain - but when the brain is flooded over and over again – the receptors stop working normally.
    21. 21. ENDORPHIN RECEPTORS USED BY EXOGENOUS OPIOID (Morphine) Morphine Carbon Hydrogen Nitrogen Sulfur Oxygen Natural endorphin (a) Structures of endorphin and morphine. Natural endorphin Endorphin receptors Morphine Brain cell (b) Binding to endorphin receptors
    22. 22. ENDORPHIN MORPHINE Endogenous opioid. Exogenous opioid Powerful analgesic 18 to 500 times than morphine (Β-endorphin is 80 times) Less analgesic than endorphin similar Molecular structure & Different chemical properties. It also Non-addictive Addictive Does not cause addiction Side-effects : euphoria/ dysphoria, constipation, respiratory depression, nausea/ vomiting etc. Receptors are : mu, kappa, delta Receptors are : mu, kappa, sigma Metabolized quickly Metabolized slowly HOW DOES POTENCY DIFFER?
    23. 23. WHAT IS DRUG ADDICTION ? In the normal course Opiate Receptors and Endorphins are kept in balance with one another. When the brain is flooded with exogenous opiates, (heroin a morphine derivative) it mimic of endorphins so system gets confused. It thinks it is making too many endorphins and shuts that down, But it still has all this excess (heroin) and thinks that it also needs to make more receptors. Heroin addiction
    24. 24. What Happens Next…. • As more Opiate Receptors are made you need more heroin to get the same effect so you use more. • And more receptors are made to accommodate the extra what the brain thinks is endorphins. • For decreasing this effect- You need more substance to get the same effect.
    25. 25. Can Methadone Fix to endorphin Receptors? • Methadone does normalize the damage caused by drug use(heroin). • Synthetic. Long half-life Used to reduce withdrawal symptoms of heroin addicts • And there is some evidence that for persons who have not used drugs very long that methadone will stop the damage they are doing and over time can normalize the system. • But this is a small minority – 30%. 72-84 hr (Slow excretion) Half-life > 24 hr Half-life > 12 hr Methadone Heroin 2 hr ( fast excretion)
    26. 26. FUTURE OF ENDORPHIN’S AND OTHER’S RECEPTORS • The future of Opioid Analgesics seems to be linked to the study of the Kappa Receptor. The kappa receptor induces analgesia without the dangerous and unwanted side effects that the mu and delta receptors are associated with. • However there are not any selectively strong agonists to this receptor as of now. • Another area of research important to the future of opioid analgesics is the study of the endogenous opioid peptides.
    27. 27. FUTURE OF ENDORPHIN’S AND OTHER’S RECEPTORS • Because these peptides are endogenous, on metabolic degradation (unlike opiates) they break down to amino acids. Hence, the metabolites are nontoxic and to not cause kidney and liver damage • Also, because they are made from amino acid residues, a large number of analogs can be synthesized from a few basic building blocks and simple modifications may be attempted to develop analogs with a desired biological effect .
    28. 28. SUMMARY • Endorphin is best analgesic endogenous opioid. • For future research endorphin receptors are very important.
    29. 29. Thanks !!!