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7 Cards in this Set

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What is the SAR of a miscarinic agonist?
Must have a group that accepts an H-bond (usually O) the correct distance away from a nitrogen that can hold a negative charge (basic or quat amine). Optimal distance is 2C, although can be 3.
For greates potency, you want small groups on the N (no more than 2 ethyls or it becomes antagonist). Propyl kills activity. Also antagonist if anything large like phenyl is on the ester.

A methyl in the alpha position (next to N) of ACh makes it selective for nicotinic receptor, but a methyl in beta position makes it selective for muscarinic receptor.
What is the SAR of a muscarinic antagonist?
Need nitrogen, then chain (2-3 C), then an ester (optional), then R1, R2, and R3 attached to tert carbon. R1 and R2 tend to be bulky rings (usually one aromatic but not the other). R3 usually small.
What are conformationally restricted analogs?
Controling conformation of a substance in order to see how it reacts and learn what the active isomer is.
What is the SAR of a reversible AChEI?
Looks like ACh except has carbamate instead of ester. This causes the enzyme to be regenerated more slowly.
What is the SAR of an irreversible AChEI?
Contains phosphate on =O instead of carbon: i.e. -P(=O)-O- instead of -C(=O)-O-. This means the enzyme will get the phosphate, which will cause alkoxides to be irreversibly kicked off (aging) and ruin the enzyme. The halogens will cause mucus membrane destruction, but can be neutralized w/ base. The fewer alkoxide (O-R) groups on phophate, the faster aging will take place.
2-PAM will reverse the process if aging has not yet taken place.
What is the SAR of an alpha receptor agonist?
2-N heterocycle attached to aromatic ring; need ortho substitution for alpha activity. If meta or para substitution, it is alpha1 selective. If not (ortho substituted only), it is alpha2 selective.
What is the SAR of an alpha receptor antagonist?
same N ring and aromatic as agonist, but w/ no ortho ring substituents.