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Pain control at brain
level
Content

– Our analegsic system
– Opioids :
a. Endrophin
b. Enkaphlin
– Receptors
– Mechanism
– Areas concerned
• pain has 2 components : perception &
reaction
• The degree to which a person reacts to
pain varies tremendously.
• This results partly from a capability of
the brain itself to suppress input of pain
signals to the nervous system by
activating a pain control system called
analgesia system
1.Opioids are the main analgesic system in
brain
2.They are of 2 types: endorphins & enkephlins
3.Drugs that mimic their effect are called opiates
4. Although the opioids have a broad range of
effects, their primary use is to relieve intense
pain, whether that pain is from surgery or a
result of injury or disease such as cancer
• Drugs that mimic action of opioids.
• The general term endorphins refers to some
endogenous morphine-like substances
whose activity has been defined by their
ability to bind to opiate receptors in the
brain.
• Endorphins(brain polypeptides with actions
like opiates) may function as synaptic
transmitters or modulators. Endorphins
appear to modulate the transmission of pain
signals within sensory pathways.
• When injected into animals, endorphins can
be analgesic
• Two closely related polypeptides (pentapeptides)
found in the brain that also bind to opiate receptors
are
• Methionine enkephalin (met-enkephalin) and
leucine enkephalin (leuenkephalin).
• The amino acid sequence of met-enkephalin has
been found in alpha-endorphin and beta-endorphin,
and that of beta-endorphin has been found in betalipotropin, a polypeptide secreted by the anterior
pituitary gland
• The major effects of the opioids are
mediated by three major receptor
families.
• These are designated by the Greek
letters μ (mu), κ (kappa), and δ
(delta).
• Each receptor family exhibits a
different specificity for the drug(s) it
binds.
Receptors
• The analgesic properties of the opioids
are primarily mediated by theμ
receptors
• .The enkephalins interact more
selectively with the δ receptors in the
periphery
• All three opioid receptors are
members of the G protein–coupled
receptor family and inhibit adenylyl
cyclase
• block neurotransmitter release by
A. inhibiting Ca2+ influx into the
presynaptic terminal,
B . open potassium channels, which
hyperpolarizes neurons and inhibits
spike activity.
They act on various receptors in the
brain and spinal cord..
• So, activation of the analgesia system
by nervous signals entering the
periaqueductal gray and
periventricular areas, or inactivation
of pain pathways by morphine-like
drugs, can almost totally suppress
many pain signals entering through
the peripheral nerves.
• PGA area: enkephalin
• Raphe magnus nucleus :serotonin
• Periventricular nuclei in hypothalamus
• Referneces
Guyton textbook of physiology
www.zuvin.com
www.bioscience.org
www.chemitryexplained.com

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Pain control at brain level

  • 1. Pain control at brain level
  • 2. Content – Our analegsic system – Opioids : a. Endrophin b. Enkaphlin – Receptors – Mechanism – Areas concerned
  • 3. • pain has 2 components : perception & reaction • The degree to which a person reacts to pain varies tremendously. • This results partly from a capability of the brain itself to suppress input of pain signals to the nervous system by activating a pain control system called analgesia system
  • 4.
  • 5.
  • 6.
  • 7. 1.Opioids are the main analgesic system in brain 2.They are of 2 types: endorphins & enkephlins 3.Drugs that mimic their effect are called opiates 4. Although the opioids have a broad range of effects, their primary use is to relieve intense pain, whether that pain is from surgery or a result of injury or disease such as cancer
  • 8. • Drugs that mimic action of opioids.
  • 9. • The general term endorphins refers to some endogenous morphine-like substances whose activity has been defined by their ability to bind to opiate receptors in the brain. • Endorphins(brain polypeptides with actions like opiates) may function as synaptic transmitters or modulators. Endorphins appear to modulate the transmission of pain signals within sensory pathways. • When injected into animals, endorphins can be analgesic
  • 10. • Two closely related polypeptides (pentapeptides) found in the brain that also bind to opiate receptors are • Methionine enkephalin (met-enkephalin) and leucine enkephalin (leuenkephalin). • The amino acid sequence of met-enkephalin has been found in alpha-endorphin and beta-endorphin, and that of beta-endorphin has been found in betalipotropin, a polypeptide secreted by the anterior pituitary gland
  • 11.
  • 12. • The major effects of the opioids are mediated by three major receptor families. • These are designated by the Greek letters μ (mu), κ (kappa), and δ (delta). • Each receptor family exhibits a different specificity for the drug(s) it binds.
  • 13.
  • 14. Receptors • The analgesic properties of the opioids are primarily mediated by theμ receptors • .The enkephalins interact more selectively with the δ receptors in the periphery • All three opioid receptors are members of the G protein–coupled receptor family and inhibit adenylyl cyclase
  • 15. • block neurotransmitter release by A. inhibiting Ca2+ influx into the presynaptic terminal, B . open potassium channels, which hyperpolarizes neurons and inhibits spike activity. They act on various receptors in the brain and spinal cord..
  • 16. • So, activation of the analgesia system by nervous signals entering the periaqueductal gray and periventricular areas, or inactivation of pain pathways by morphine-like drugs, can almost totally suppress many pain signals entering through the peripheral nerves.
  • 17. • PGA area: enkephalin • Raphe magnus nucleus :serotonin • Periventricular nuclei in hypothalamus
  • 18.
  • 19. • Referneces Guyton textbook of physiology www.zuvin.com www.bioscience.org www.chemitryexplained.com