37 Questions
What does the term 'opium' mean in Greek?
Juice
In medicinal chemistry, what is the purpose of drug design strategies like extension and simplification of structure?
To develop various morphine analogues
What is the main focus of discussing the Stereochemistry of opioid analgesics?
Receptor binding specificity
Why are analogues like Morphinans and Benzomorphans considered important in the study of opioid analgesics?
To enhance receptor interaction
What key aspect of morphine's structure do medicinal chemists aim to understand?
Its structural features
What is the significance of rigidification in developing opioids like buprenorphine?
To increase receptor selectivity
What is the correct structural feature of morphine that enables it to bind through various interactions?
Functional groups capable of forming ionic, hydrogen bond, and van der Waals interactions
In the context of opioid analgesics, what is the significance of morphine being poorly absorbed orally?
It limits its potential clinical use
What are the common side effects associated with the use of morphine?
Respiratory depression and constipation
How does codeine differ from morphine in terms of its analgesic activity?
Codeine is less active when injected peripherally than when it crosses the blood-brain barrier
What distinguishes heroin from morphine in terms of crossing the blood-brain barrier?
Heroin can directly cross the blood-brain barrier
Why is it essential to test analogues for activity when studying structure-activity relationships?
To determine the importance of functional groups for activity
Which molecule is used as a substitute for morphine or heroin to treat addicts?
Methadone
Which form of methadone has 2 times the activity of morphine?
R form
Which molecule uses a flexible binding mode different from morphine?
Methadone
Which opioid displays properties of being an antagonist with agonist properties?
Buprenorphine
Which opioid has the property of dissociating slowly from the receptor?
Buprenorphine
What is the main advantage of simplifying drug analogues according to the text?
Decrease production cost
Which functional group is removed to create a series of tetracyclic compounds known as morphinans?
Phenol group
What change in the structure of N-methylmorphinan increased its potency compared to morphine?
Removal of ring D
Which compound has the same analgesic activity as morphine after removing both rings C and D?
Metazocine
What impact did replacing the N-methyl group of metazocine with a phenyl group have on phenazocine?
Increased potency without addiction properties
What is a key characteristic of pentazocine in terms of addiction potential?
Low addiction risk
What distinguishes bremazocine from pentazocine in terms of activity?
Higher potency than morphine
What is the main drawback of Pethidine compared to Methadone?
Greater dependence potential
What is the primary advantage of benzomorphans over morphine according to the text?
Rapid onset and long duration
What is an important clinical benefit of benzomorphans?
Balance analgesic benefits with lower addiction/tolerance risks
Which functional group is indicated as the most important for the analgesic activity of morphine in the given text?
Phenolic group
What effect is observed on the analgesic activity of analogues if the 3-OH group in morphine is modified?
Activity decreases significantly
Which receptor is identified as the main one for both analgesic effects and side effects of morphine in the text?
Mu (µ)
What is the biologically active enantiomer of morphine with regard to its stereochemistry?
(5R, 6S, 9R, 13S, 14R)
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?
Drug extension
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?
Decreases agonist activity to zero
Which type of drug antagonist binds to analgesic receptors without activating them and blocks morphine binding?
Pure antagonist
In drug extension at the N-atom of morphine, which additional groups lead to naloxone, naltrexone, and nalorphine?
Allyl or propyl groups
What is the main purpose of opioid drug design mentioned in the text?
To minimize side effects
Which group indicated in drug extension for morphine increases activity by 14-fold according to the text?
Phenethyl group
Test your knowledge on The Opioid Analgesics discussed in Lectures 4&5 of MSOP1016 - The Science of Medicine 3 at Medway School of Pharmacy. Explore topics related to the structural features of morphine and medicinal chemistry. Recommended reading from 'An introduction to medicinal chemistry' by Graham Patrick (5th Ed) available at the Drill Hall Library.
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