Sazetidine A
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Sazetidine A (AMOP-H-OH) is a drug which acts as a subtype selective
partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonis ...
at α4β2 neural
nicotinic acetylcholine receptor Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral ner ...
s, acting as an agonist at (α4)2(β2)3 pentamers, but as an antagonist at (α4)3(β2)2 pentamers. It has potent analgesic effects in animal studies comparable to those of
epibatidine Epibatidine is a chlorinated alkaloid that is secreted by the Ecuadoran frog ''Epipedobates anthonyi'' and poison dart frogs from the Ameerega genus. It was discovered by John W. Daly in 1974, but its structure was not fully elucidated until 19 ...
, but with less toxicity, and also has antidepressant action.


References

{{Nicotinic acetylcholine receptor modulators Nicotinic agonists Azetidines Phenol ethers Pyridines Alkyne derivatives Primary alcohols