Chemistry:Sazetidine A
From HandWiki
Short description: Pharmaceutical drug
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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]
References
- ↑ "Divergent functional effects of sazetidine-a and varenicline during nicotine withdrawal". Neuropsychopharmacology 38 (10): 2035–2047. September 2013. doi:10.1038/npp.2013.105. PMID 23624742.
- ↑ "Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them". Molecular Pharmacology 70 (4): 1454–1460. October 2006. doi:10.1124/mol.106.027318. PMID 16857741.
- ↑ "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. June 2008. doi:10.1124/mol.108.045104. PMID 18367540.
- ↑ "Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug". Anesthesiology 109 (3): 512–519. September 2008. doi:10.1097/ALN.0b013e3181834490. PMID 18719450.
- ↑ "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): 1279–1291. August 2009. doi:10.1002/cmdc.200900079. PMID 19569163.
- ↑ "Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them". Molecular Pharmacology 70 (4): 1454–1460. October 2006. doi:10.1124/mol.106.027318. PMID 16857741.
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