5-Iodo-A-85380 dihydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 1518 - 5-Iodo-A-85380 dihydrochloride | C9H11IN2O.2HCl | CAS No. 1217837-17-6
Description: High affinity α4β2 and α6β2 subtype-selective agonist
Chemical Name: 3-[(2S)-2-Azetidinylmethoxy]-5-iodopyridine dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Literature

Biological 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.

Technical Data

M. Wt 363.03
Formula C9H11IN2O.2HCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 1217837-17-6
PubChem ID 54758463
InChI Key ZJVVFYWEBSHGBV-JZGIKJSDSA-N
Smiles IC1=CN=CC(OC[C@@H]2CCN2)=C1.Cl.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.3 100
water 36.3 100

Preparing Stock Solutions

The following data is based on the product molecular weight 363.03. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.75 mL 13.77 mL 27.55 mL
5 mM 0.55 mL 2.75 mL 5.51 mL
10 mM 0.28 mL 1.38 mL 2.75 mL
50 mM 0.06 mL 0.28 mL 0.55 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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


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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, Nicotinic, (a4b2), Receptors, Tocris Bioscience

3 Citations for 5-Iodo-A-85380 dihydrochloride

Citations are publications that use Tocris products. Selected citations for 5-Iodo-A-85380 dihydrochloride include:

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

Chatzidaki et al (2015) Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons. Neurochem Res 10 e0125116 PMID: 25906356

Brown and Wonnacott (2015) Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors. Pharmacol Res Perspect 40 2047 PMID: 24728867


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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