Sazetidine A
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Pharmaceutical drug
Pharmaceutical compound
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| Formula | C15H20N2O2 |
| Molar mass | 260.337 g·mol−1 |
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Sazetidine A (AMOP-H-OH) is a drug which acts as a subtype selective partial agonist[1] 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.[2][3] It has potent analgesic effects in animal studies comparable to those of epibatidine, but with less toxicity,[4] and also has antidepressant action.[5][6]
- ↑ Turner JR, Wilkinson DS, Poole RL, Gould TJ, Carlson GC, Blendy JA (September 2013). "Divergent functional effects of sazetidine-a and varenicline during nicotine withdrawal". Neuropsychopharmacology. 38 (10): 2035–2047. doi:10.1038/npp.2013.105. PMC 3746688. PMID 23624742.
- ↑ Xiao Y, Fan H, Musachio JL, Wei ZL, Chellappan SK, Kozikowski AP, et al. (October 2006). "Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them". Molecular Pharmacology. 70 (4): 1454–1460. doi:10.1124/mol.106.027318. PMID 16857741. S2CID 6599272.
- ↑ Zwart R, Carbone AL, Moroni M, Bermudez I, Mogg AJ, Folly EA, et al. (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): 1838–1843. doi:10.1124/mol.108.045104. PMID 18367540. S2CID 24632914.
- ↑ Cucchiaro G, Xiao Y, Gonzalez-Sulser A, Kellar KJ (September 2008). "Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug". Anesthesiology. 109 (3): 512–519. doi:10.1097/ALN.0b013e3181834490. PMID 18719450. S2CID 22185882.
- ↑ Kozikowski AP, Eaton JB, Bajjuri KM, Chellappan SK, Chen Y, Karadi S, et al. (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): 1279–1291. doi:10.1002/cmdc.200900079. PMC 2955514. PMID 19569163.
- ↑ Xiao Y, Fan H, Musachio JL, Wei ZL, Chellappan SK, Kozikowski AP, et al. (October 2006). "Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them". Molecular Pharmacology. 70 (4): 1454–1460. doi:10.1124/mol.106.027318. PMID 16857741.
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| nAChRsTooltip Nicotinic acetylcholine receptors |
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