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Sazetidine A

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Title: Sazetidine A  
Author: World Heritage Encyclopedia
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Subject: Alpha-4 beta-2 nicotinic receptor, TC-2216, ABT-202, TC-1698, AR-R17779
Collection: Alcohols, Alkynes, Azetidines, Nicotinic Agonists, Phenol Ethers, Pyridines
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Sazetidine A

Sazetidine A
Systematic (IUPAC) name
6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-ol
Clinical data
Legal status
?
Identifiers
CAS number  YesY
ATC code ?
PubChem
ChemSpider
Chemical data
Formula C15H20N2O2 
Mol. mass 260.331
 YesY   

Sazetidine A (AMOP-H-OH) is a drug which acts as a subtype selective partial agonist at α4β2 neural nicotinic acetylcholine receptors, acting as an agonist at (α4)2(β2)3 pentamers, but as an antagonist at (α4)3(β2)2 pentamers.[1][2] It has potent analgesic effects in animal studies comparable to those of epibatidine, but with less toxicity,[3] and also has antidepressant action.[4]

References

  1. ^ Xiao Y, Fan H, Musachio JL, Wei ZL, Chellappan SK, Kozikowski AP, Kellar KJ (October 2006). "Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them". Molecular Pharmacology 70 (4): 1454–60.  
  2. ^ Zwart R, Carbone AL, Moroni M, Bermudez I, Mogg AJ, Folly EA, Broad LM, Williams AC, Zhang D, Ding C, Heinz BA, Sher E (June 2008). "Sazetidine-A is a potent and selective agonist at native and recombinant alpha 4 beta 2 nicotinic acetylcholine receptors". Molecular Pharmacology 73 (6): 1838–43.  
  3. ^ Cucchiaro G, Xiao Y, Gonzalez-Sulser A, Kellar KJ (September 2008). "Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug". Anesthesiology 109 (3): 512–9.  
  4. ^ Kozikowski AP, Eaton JB, Bajjuri KM, Chellappan SK, Chen Y, Karadi S, He R, Caldarone B, Manzano M, Yuen PW, Lukas RJ (August 2009). "Chemistry and Pharmacology of Nicotinic Ligands Based on 6-5-(Azetidin-2-ylmethoxy) pyridin-3-ylhex-5-yn-1-ol (AMOP-H-OH) for Possible Use in Depression". Chemmedchem 4 (8): 1279–91.  
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