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Sazetidine A
Systematic (IUPAC) name
6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-ol
Identifiers
CAS number 820231-95-6
ATC code  ?
PubChem  ?
Chemical data
Formula C 15H20N2O2  
Mol. mass 260.331
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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. doi:10.1124/mol.106.027318. PMID 16857741.  
  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. doi:10.1124/mol.108.045104. PMID 18367540.  
  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. doi:10.1097/ALN.0b013e3181834490. PMID 18719450.  
  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-yl]hex-5-yn-1-ol (AMOP-H-OH) for possible use in depression". Chemmedchem 4 (8): 1279–91. doi:10.1002/cmdc.200900079. PMID 19569163.  
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