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 also available.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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.
|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|
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for 5-Iodo-A-85380 dihydrochloride, please let us know.
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Keywords: 5-Iodo-A-85380 dihydrochloride, 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, (Other, Subtypes), (a4b2), 1518, 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:
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
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? Please let us know.
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Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.