Sazetidine A

Sazetidine A
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
Formula C15H20N2O2
Molar mass 260.331
3D model (JSmol)
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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. PMID 16857741. doi:10.1124/mol.106.027318.
  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. PMID 18367540. doi:10.1124/mol.108.045104.
  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. PMID 18719450. doi:10.1097/ALN.0b013e3181834490.
  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. PMC 2955514 Freely accessible. PMID 19569163. doi:10.1002/cmdc.200900079.

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