Medicinal Chemistry Of Opioid Analgesics 2

Question 1

What happens to the activity of morphine is the n group is changed to a quaternary salt and what can we tell if it is injected into the CNS?

Answer 1

Inactive however if Injected into CNS it is active so therefore this shows nitrogen must be charged when interacting with the receptor

Question 2

What happens to the activity and polarity if the methyl group from the nitrogen is removed?

Answer 2

Activity decreases and polarity increases

Question 3

Do the aromatic ring and ether group effect activity?

Answer 3

Removal of Ring leads to loss of activity

Ether has no effect on analgesia

Question 4

Is morphines enantiomer inactive?

Answer 4

Yes

Question 5

What is pharmacophore?

Answer 5

The 3D positioning of the key functional groups with respect to each other

Question 6

Does the activity of morphine change when it undergoes hydrogenation to become dihydromorphine?

Answer 6

No