Sazetidin A

Sazetidin A
IUPAC ime
	6-[5-[(2S)-2-Azetidinilmetoksi]-3-piridinil]-5-heksin-1-ol
Identifikatori
CAS broj	820231-95-6
ATC kod	None
Hemijski podaci
Formula	C15H20N2O2
Molarna masa	260,331
	SMILES OCCCCC#Cc1cc(cnc1)OCC2CCN2; ;

Sazetidin A (AMOP-H-OH) je lek koji deluje kao selektivni parcijalni agonist za α4β2 tip neuronskih nikotinskih acetilholinskih receptora. On je agonist na (α4)2(β2)3 pentamerima, a antagonist na (α4)3(β2)2 pentamerima.^[1]^[2] On ima potentne analgetske efekte u životinjskim studijama, slično epibatidinu, ali je manje toksičan,^[3] a takođe ima antidepresivno dejstvo.^[4]

Reference

^ Xiao Y, Fan H, Musachio JL, Wei ZL, Chellappan SK, Kozikowski AP, Kellar KJ (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.
^ Zwart R, Carbone AL, Moroni M, Bermudez I, Mogg AJ, Folly EA, Broad LM, Williams AC, Zhang D, Ding C, Heinz BA, Sher E (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.
^ Cucchiaro G, Xiao Y, Gonzalez-Sulser A, Kellar KJ (2008). . „Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug”. Anesthesiology. 109 (3): 512—9. PMID 18719450. doi:10.1097/ALN.0b013e3181834490.
^ Kozikowski AP, Eaton JB, Bajjuri KM, Chellappan SK, Chen Y, Karadi S, He R, Caldarone B, Manzano M, Yuen PW, Lukas RJ (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 . PMID 19569163. doi:10.1002/cmdc.200900079.