Dugga 3 - Opiates

Question 1

What is morphinans?

Answer 1

Compounds where the D ring is removed from morphine.

N-methylmorphinan and levorphanol are two morphinans.

Question 2

Why is E-ring not removed from morphine in simplification?

Answer 2

Removing E leads to complete loss of activity

Question 3

What is benzomorphans?

Answer 3

Compounds where the D and C rings are removed from morphine.

Metazocine - same potency

Phenazocine 4x more potent (antagonist at the u-receptor and full agonist at the k-receptor)

Bremazocine - 200x more potent, non/low addictivity and doesn’t depress breathing

Question 4

What is nalorphine an example of?

Answer 4

Drug extension leading to antagonistic effects, blocking morphine.

Nalorphine acts as an antagonist and an agonist depending on what opiod receptor.

Question 5

What compound is used in an spray against morphine overdose?

Answer 5

Naloxene which is a antagonist created by ring extension by alkyl substiuents on the nitrogen atom.

Question 6

What is 4-anilinopiperidines?

Answer 6

Compounds where the b,C and D rings are removed from morphine.

Most potent one is fentanyl, one of the most potent agonist of the u-receptor.

Question 7

What is Oxycontin?

Question 8

What is tramadol?

Answer 8

A morphin analogue. The metabolite of tramadol is active:

• receptor agonist, leads to uphoria
• seratonin-NA reuptake inhibitor ==> Antidepressant

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Question 9

What is special with methadone?

Answer 9

Oraly active.
Removal of B,C,D, E rings.

Important to have the right position between nitrogen and phenalon. This is done by ring E.

Methadone is the simplest morphine analogue.

Question 10

Four opiod receptors

Answer 10

mu, kappa, delta and ORL1

Question 11

How does the different opiod receptor work?

Answer 11

Mu receptor is a potasium ion channel, morphine opens the channel ==> create down stream effect

Kappa, calcium ion channel, morphine will close the ion channel ==>

Delta receptor, G-protein receptor. The morphine will inhibit the co-enzyme and stop c-AMP

Question 12

What are endogenous compound in opiate receptors?

Answer 12

The endogenous substrate for opium receptors are peptide like structures, neuropeptides. These are formed in the brain in the CNS

One example of a neuropeptide is endorphine

Question 13

What drug mimics the neuropeptides?

Answer 13

Met-enkephalin, a penta peptide.

The phenyl in enkephalin may do the same thing as the phenyl in fentanyl