wk8: Synthetic opioids
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24 Terms
What are the three main families of endogenous opioid peptides?
Endorphins, enkephalins, dynorphins
What is the precursor of β-endorphin?
POMC (pro-opiomelanocortin)
What is the precursor of enkephalins?
Proenkephalin
What is the precursor of dynorphin?
Prodynorphin
Which opioid receptor do enkephalins prefer?
DOR (delta)
Which opioid receptor does dynorphin prefer?
KOR (kappa)
Who discovered enkephalins and when?
Kosterlitz in 1975
Why are peptide drugs difficult to use orally?
Broken down by peptidases, poor oral bioavailability, don't cross BBB
What is one strategy to make peptide drugs more stable?
Integrate unnatural amino acids (e.g., D-alanine)
Why does D-alanine make peptides more stable?
Peptidases don't recognise it – steric hindrance blocks breakdown
What is another strategy to improve peptide drugs?
Use peptidase inhibitors to block breakdown
What is a prodrug strategy for peptides?
Make an inactive derivative that is converted to active drug in the body
What are the 4 main classes of synthetic opioids?
4-Phenylpiperidines, morphinans, benzomorphans, diphenylpropylamines
What are examples of 4-phenylpiperidines?
Pethidine, fentanyl
How potent is fentanyl compared to morphine?
Approximately 100x more potent
What is fentanyl used for?
Anaesthesia and severe pain
What is a major problem with fentanyl?
High abuse potential
What class does methadone belong to?
Diphenylpropylamines
What is special about methadone's duration of action?
Long-acting (slow elimination)
What is methadone used for?
Opioid addiction treatment (maintenance therapy)
What does the Portuguese binding theory propose?
The opioid receptor has a flexible binding site that can accommodate different shapes
What is the ring removal strategy?
Simplifying morphine structure (removing rings) while keeping activity
What is an example of a ring removal product?
Morphinans (4 rings instead of 5)
What modification makes an enkephalin orally active?
Integrating unnatural amino acids like D-Ala and N-methylation