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MCDB 126/226 Pharmacology, Assignments of Pharmacology

Week 7 Homework Assignment- Questions about Opiorphin Reading

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2023/2024

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Week 7 HW Assignment: Questions about Opiorphin Reading
1. What is the three classes of endogenous compounds whose anti-nociceptive activity is
mimicked by opioid drugs?
Opiorphin, sialorphin, and spinorphin are the three types of endogenous substances whose pain-
relieving effects are comparable to those of opioid medications.These substances are all
endogenous enkephalinase inhibitors (EIs) The function of these three EIs is to physiologically
reduce zinc ectopeptidases, which deactivate enkephalins, hence boosting the actions of
enkephalins.
2. What is the biochemical nature of opiorphin, where was it isolated, and what is its mechanism
of action?
Opiorphin is a pentapeptide with the amino acid sequence QRFSR. It is an inhibitor of neutral
ectoendopeptidase and ecto-aminopeptidase enzymes.Human saliva is where it was initially
discovered.Opiorphin lessens the breakdown of enkephalins, which are naturally occurring
opioids. As a result, more enkephalins are available to attach to opioid receptors and provide
analgesic effects.
3. How were the anti-nociceptive actions of opinorphin evaluated in the Popik study?
The tail-flick test in mice was used in the Popik study to assess the pain-relieving effects of
opiorphin. This test determines how long it takes a mouse to remove its tail from a radiant heat
source.The researchers measured the mice's tail-flick latency at different periods following
injection after giving them opiorphin. The findings indicated that opiorphin dramatically
prolonged tail-flick latency, proving its analgesic effect.
4. What was the purpose of the naloxone that was used in some of the tail flick experiments?
Naloxone counteracts the effects of opioids by acting as an opioid receptor antagonist.To see if
opioid receptors were involved in the antinociceptive effects of opiorphin, naloxone was utilized
in the tail-flick studies. The implication would be that opiorphin was actually acting via opioid
receptors if naloxone suppressed its effects.
5. What other potentially useful behavioral effect was observed from the use of opiorphin on
mice? How was this determined?
In addition to its pain-relieving properties, the study also found that opiorphin had an
antidepressant-like impact on mice. The forced swim test, a behavioral experiment that gauges
how long a mouse stays motionless when submerged in a container of water, was used to ascertain
this impact. Mice given opiorphin exhibited considerably less immobility than control mice,
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Week 7 HW Assignment: Questions about Opiorphin Reading

  1. What is the three classes of endogenous compounds whose anti-nociceptive activity is mimicked by opioid drugs? Opiorphin, sialorphin, and spinorphin are the three types of endogenous substances whose pain- relieving effects are comparable to those of opioid medications.These substances are all endogenous enkephalinase inhibitors (EIs) The function of these three EIs is to physiologically reduce zinc ectopeptidases, which deactivate enkephalins, hence boosting the actions of enkephalins.
  2. What is the biochemical nature of opiorphin, where was it isolated, and what is its mechanism of action? Opiorphin is a pentapeptide with the amino acid sequence QRFSR. It is an inhibitor of neutral ectoendopeptidase and ecto-aminopeptidase enzymes.Human saliva is where it was initially discovered.Opiorphin lessens the breakdown of enkephalins, which are naturally occurring opioids. As a result, more enkephalins are available to attach to opioid receptors and provide analgesic effects.
  3. How were the anti-nociceptive actions of opinorphin evaluated in the Popik study? The tail-flick test in mice was used in the Popik study to assess the pain-relieving effects of opiorphin. This test determines how long it takes a mouse to remove its tail from a radiant heat source.The researchers measured the mice's tail-flick latency at different periods following injection after giving them opiorphin. The findings indicated that opiorphin dramatically prolonged tail-flick latency, proving its analgesic effect.
  4. What was the purpose of the naloxone that was used in some of the tail flick experiments? Naloxone counteracts the effects of opioids by acting as an opioid receptor antagonist.To see if opioid receptors were involved in the antinociceptive effects of opiorphin, naloxone was utilized in the tail-flick studies. The implication would be that opiorphin was actually acting via opioid receptors if naloxone suppressed its effects.
  5. What other potentially useful behavioral effect was observed from the use of opiorphin on mice? How was this determined? In addition to its pain-relieving properties, the study also found that opiorphin had an antidepressant-like impact on mice. The forced swim test, a behavioral experiment that gauges how long a mouse stays motionless when submerged in a container of water, was used to ascertain this impact. Mice given opiorphin exhibited considerably less immobility than control mice,

indicating that opiorphin may have antidepressant-like properties.

  1. What undesirable effect of opioids such as morphine was not observed at the lowest effective dose of opiorphin? Physiological dependence is an adverse effect of opioids like morphine that was not seen at the lowest effective dose of opiorphin. While repeated morphine administration at a dose of 30 mg/kg caused physiological dependence, as demonstrated by the naloxone-induced opioid withdrawal, opiorphin at a dose of 3 mg/kg did not have this effect. This supports the theory that opiorphin, in contrast to conventional opioids, does not result in physical dependence.