Podcast
Questions and Answers
What does the term 'opium' mean in Greek?
What does the term 'opium' mean in Greek?
In medicinal chemistry, what is the purpose of drug design strategies like extension and simplification of structure?
In medicinal chemistry, what is the purpose of drug design strategies like extension and simplification of structure?
What is the main focus of discussing the Stereochemistry of opioid analgesics?
What is the main focus of discussing the Stereochemistry of opioid analgesics?
Why are analogues like Morphinans and Benzomorphans considered important in the study of opioid analgesics?
Why are analogues like Morphinans and Benzomorphans considered important in the study of opioid analgesics?
Signup and view all the answers
What key aspect of morphine's structure do medicinal chemists aim to understand?
What key aspect of morphine's structure do medicinal chemists aim to understand?
Signup and view all the answers
What is the significance of rigidification in developing opioids like buprenorphine?
What is the significance of rigidification in developing opioids like buprenorphine?
Signup and view all the answers
What is the correct structural feature of morphine that enables it to bind through various interactions?
What is the correct structural feature of morphine that enables it to bind through various interactions?
Signup and view all the answers
In the context of opioid analgesics, what is the significance of morphine being poorly absorbed orally?
In the context of opioid analgesics, what is the significance of morphine being poorly absorbed orally?
Signup and view all the answers
What are the common side effects associated with the use of morphine?
What are the common side effects associated with the use of morphine?
Signup and view all the answers
How does codeine differ from morphine in terms of its analgesic activity?
How does codeine differ from morphine in terms of its analgesic activity?
Signup and view all the answers
What distinguishes heroin from morphine in terms of crossing the blood-brain barrier?
What distinguishes heroin from morphine in terms of crossing the blood-brain barrier?
Signup and view all the answers
Why is it essential to test analogues for activity when studying structure-activity relationships?
Why is it essential to test analogues for activity when studying structure-activity relationships?
Signup and view all the answers
Which molecule is used as a substitute for morphine or heroin to treat addicts?
Which molecule is used as a substitute for morphine or heroin to treat addicts?
Signup and view all the answers
Which form of methadone has 2 times the activity of morphine?
Which form of methadone has 2 times the activity of morphine?
Signup and view all the answers
Which molecule uses a flexible binding mode different from morphine?
Which molecule uses a flexible binding mode different from morphine?
Signup and view all the answers
Which opioid displays properties of being an antagonist with agonist properties?
Which opioid displays properties of being an antagonist with agonist properties?
Signup and view all the answers
Which opioid has the property of dissociating slowly from the receptor?
Which opioid has the property of dissociating slowly from the receptor?
Signup and view all the answers
What is the main advantage of simplifying drug analogues according to the text?
What is the main advantage of simplifying drug analogues according to the text?
Signup and view all the answers
Which functional group is removed to create a series of tetracyclic compounds known as morphinans?
Which functional group is removed to create a series of tetracyclic compounds known as morphinans?
Signup and view all the answers
What change in the structure of N-methylmorphinan increased its potency compared to morphine?
What change in the structure of N-methylmorphinan increased its potency compared to morphine?
Signup and view all the answers
Which compound has the same analgesic activity as morphine after removing both rings C and D?
Which compound has the same analgesic activity as morphine after removing both rings C and D?
Signup and view all the answers
What impact did replacing the N-methyl group of metazocine with a phenyl group have on phenazocine?
What impact did replacing the N-methyl group of metazocine with a phenyl group have on phenazocine?
Signup and view all the answers
What is a key characteristic of pentazocine in terms of addiction potential?
What is a key characteristic of pentazocine in terms of addiction potential?
Signup and view all the answers
What distinguishes bremazocine from pentazocine in terms of activity?
What distinguishes bremazocine from pentazocine in terms of activity?
Signup and view all the answers
What is the main drawback of Pethidine compared to Methadone?
What is the main drawback of Pethidine compared to Methadone?
Signup and view all the answers
What is the primary advantage of benzomorphans over morphine according to the text?
What is the primary advantage of benzomorphans over morphine according to the text?
Signup and view all the answers
What is an important clinical benefit of benzomorphans?
What is an important clinical benefit of benzomorphans?
Signup and view all the answers
Which functional group is indicated as the most important for the analgesic activity of morphine in the given text?
Which functional group is indicated as the most important for the analgesic activity of morphine in the given text?
Signup and view all the answers
What effect is observed on the analgesic activity of analogues if the 3-OH group in morphine is modified?
What effect is observed on the analgesic activity of analogues if the 3-OH group in morphine is modified?
Signup and view all the answers
Which receptor is identified as the main one for both analgesic effects and side effects of morphine in the text?
Which receptor is identified as the main one for both analgesic effects and side effects of morphine in the text?
Signup and view all the answers
What is the biologically active enantiomer of morphine with regard to its stereochemistry?
What is the biologically active enantiomer of morphine with regard to its stereochemistry?
Signup and view all the answers
What is the strategy involved in drug design focused on extending a lead compound by adding extra functional groups to probe for additional binding regions?
What is the strategy involved in drug design focused on extending a lead compound by adding extra functional groups to probe for additional binding regions?
Signup and view all the answers
What effect does increasing the alkyl group size attached to the nitrogen atom from methyl to butyl have on agonist activity according to the text?
What effect does increasing the alkyl group size attached to the nitrogen atom from methyl to butyl have on agonist activity according to the text?
Signup and view all the answers
Which type of drug antagonist binds to analgesic receptors without activating them and blocks morphine binding?
Which type of drug antagonist binds to analgesic receptors without activating them and blocks morphine binding?
Signup and view all the answers
In drug extension at the N-atom of morphine, which additional groups lead to naloxone, naltrexone, and nalorphine?
In drug extension at the N-atom of morphine, which additional groups lead to naloxone, naltrexone, and nalorphine?
Signup and view all the answers
What is the main purpose of opioid drug design mentioned in the text?
What is the main purpose of opioid drug design mentioned in the text?
Signup and view all the answers
Which group indicated in drug extension for morphine increases activity by 14-fold according to the text?
Which group indicated in drug extension for morphine increases activity by 14-fold according to the text?
Signup and view all the answers