Sazetidin A

Sazetidin A
(IUPAC) ime
	6-[5-[(2S)-2-Azetidinilmetoksi]-3-piridinil]-5-heksin-1-ol
Klinički podaci
Identifikatori
CAS broj	820231-95-6
ATC kod	nije dodeljen
Hemijski podaci
Formula	C15H20N2O2
Mol. masa	260,331
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C15H20N2O2/c18-8-4-2-1-3-5-13-9-15(11-16-10-13)19-12-14-6-7-17-14/h9-11,14,17-18H,1-2,4,6-8,12H2 ; Key: WONBUILDJNKYCB-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

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 (October 2006). „Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them”. Molecular Pharmacology 70 (4): 1454–60. DOI:10.1124/mol.106.027318. PMID 16857741.
↑ 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. DOI:10.1124/mol.108.045104. PMID 18367540.
↑ 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. DOI:10.1097/ALN.0b013e3181834490. PMID 18719450.
↑ 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. DOI:10.1002/cmdc.200900079. PMC 2955514. PMID 19569163.

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