Cat. No. 1518
Chemical Name: 3-[(2S)-2-Azetidinylmethoxy]-5-iodo
Biological ActivityA highly potent and subtype-selective agonist for the α4β2 and α6β2 nicotinic acetylcholine receptors. Activates α-CTx-MII-sensitive and -insensitive components of [3H]dopamine release from rat striatal synaptosomes, corresponding to α6β2 and α4β2 (EC50 values are 12.7 and ~35 nM respectively). ~5000- , 25000- and 140000-fold selective over α3β4, α7 and muscle nAChR receptors respectively. Precursor (Cat. No. 1527) also available.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Mogg et al (2004) Functional responses and subunit composition of presynaptic nicotinic receptor subtypes explored using the novel agonist 5-iodo-A-85380. Neuropharmacology 47 848. PMID: 15527819.
Mukhin et al (2000) 5-Iodo-A-85380, an α4β2 subtype-selective ligand for nicotinic acetylcholine receptors. Mol.Pharmacol. 57 642. PMID: 10692507.
Koren et al (1998) 2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling. J.Med.Chem. 41 3690. PMID: 9733494.
If you know of a relevant reference for 5-Iodo-A-85380 dihydrochloride please let us know.
Citations are publications that use Tocris products. Selected citations for 5-Iodo-A-85380 dihydrochloride include:
Brown and Wonnacott (2015) Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors. Pharmacol Res Perspect 40 2047. PMID: 24728867.
Chatzidaki et al (2015) Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons. Neurochem Res 10 e0125116. PMID: 25906356.
Hamouda et al (2009) Photoaffinity labeling the agonist binding domain of alpha4beta4 and alpha4beta2 neuronal nicotinic acetylcholine receptors with [(125)I]epibatidine and 5[(125)I]A-85380. Biochim Biophys Acta 1788 1987. PMID: 19545536.
Do you know of a great paper that uses 5-Iodo-A-85380 dihydrochloride from Tocris? If so please let us know.
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Keywords: 5-Iodo-A-85380 dihydrochloride, supplier, High, affinity, α4β2, a4b2, α6β2, alpha6beta2, a6b2, subtype-selective, agonists, nicotinic, Receptors, Acetylcholine, nAChR, Non-Selective, Subtypes, Other, 5IA85380, Tocris Bioscience, Nicotinic (α4β2) Receptor Agonist products
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Potent positive allosteric modulator of α4β2 nAChRs; also inhibitor of (α4)2(β2)3, muscle-type and Torpedo nAChRs
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