aced126
Bluelighter
- Joined
- May 18, 2015
- Messages
- 1,047
Pomzazed, could you expand in more detail on the SAR of CB1 ligands. More importantly, what is required for antagonist activity. Afaik CB1 spontaneously switches between active and inactive states; rimonabant stabilises the inactive state of CB1, and thus could be considered an inverse agonist.
https://en.m.wikipedia.org/wiki/Can...nist#/media/File:Rimonabant_Pharmacophore.png
Are the marked aa residues in the linked diagram also involved in active state agonist binding? Or are they completely different? If the latter is true, does this suggest an endogenous CB1 antagonist which enables more precise neuron signalling?
https://en.m.wikipedia.org/wiki/Can...nist#/media/File:Rimonabant_Pharmacophore.png
Are the marked aa residues in the linked diagram also involved in active state agonist binding? Or are they completely different? If the latter is true, does this suggest an endogenous CB1 antagonist which enables more precise neuron signalling?