A251
A-85380 dihydrochloride
solid
Sinonimo/i:
3-((2S)-Azetidinylmethoxy)pyridine dihydrochloride
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About This Item
Forma fisica
solid
Attività ottica
[α]20/D −5.2°, c = 0.5 in methanol(lit.)
Colore
off-white
Solubilità
H2O: 10 mg/mL
Stringa SMILE
Cl[H].Cl[H].C1C[C@H](COc2cccnc2)N1
Applicazioni
The 5-125I-analog has been used as a selective radioligand for the α4β2 nAChR subtype. Fluorinated analogs have been used for PET imaging of nAChRs.
Azioni biochim/fisiol
Potent and selective neuronal nicotinic acetylcholine receptor (nAChR) agonist.
Avvertenza
Hygroscopic
Note legali
Manufactured and sold under exclusive license from Abbott Laboratories.
Codice della classe di stoccaggio
13 - Non Combustible Solids
Classe di pericolosità dell'acqua (WGK)
WGK 3
Punto d’infiammabilità (°F)
Not applicable
Punto d’infiammabilità (°C)
Not applicable
Dispositivi di protezione individuale
Eyeshields, Gloves, type N95 (US)
Certificati d'analisi (COA)
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Nuclear medicine and biology, 25(7), 599-603 (1998-11-06)
The in vivo brain regional distribution of 2-[18F]fluoro-A-85380, a novel tracer for positron emission tomographic (PET) studies, followed the regional densities of brain nAChRs reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in
Neuropharmacology, 35(6), 725-734 (1996-06-01)
The in vitro pharmacological properties of a novel cholinergic channel ligand, A-85380 [3-(2(S)-azetidinylmethoxy)pyridine], were examined using tissue preparations that express different putative nAChR subtypes. In radioligand binding studies, A-85380 is shown to be a potent and selective ligand for the
Molecular pharmacology, 57(3), 642-649 (2000-02-29)
In an effort to develop selective radioligands for in vivo imaging of neuronal nicotinic acetylcholine receptors (nAChRs), we synthesized 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine (5-iodo-A-85380) and labeled it with (125)I and (123)I. Here we present the results of experiments characterizing this radioiodinated ligand in
Journal of medicinal chemistry, 39(4), 817-825 (1996-02-16)
Recent evidence indicating the therapeutic potential of cholinergic channel modulators for the treatment of central nervous system (CNS) disorders as well as the diversity of brain neuronal nicotine acetylcholine receptors (nAChRs) have suggested an opportunity to develop subtype-selective nAChR ligands
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