5-Iodo-A-85380 dihydrochloride (3-[(2S)-2-Azetidinylmethoxy]-5-iodopyridine dihydrochloride) | 1217837-17-6

name

5-iodo-a-85380 dihydrochloride

chemical name

3-[(2s)-2-azetidinylmethoxy]-5-iodopyridine dihydrochloride

activity

a 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.

MW

363.03

Formula:

c9h11in2o.2hcl

Solubility:

soluble to 100 mm in water and to 100 mm in dmso

Purity:

>99 %

Storage:

desiccate at +4°c

CAS No:

1217837-17-6

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.

Mukhin et al (2000) 5-Iodo-A-85380, an α4β2 subtype-selective ligand for nicotinic acetylcholine receptors. Mol.Pharmacol. 57 642. PMID: 10692507.

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.