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.