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Submit ReviewPHA 543613 hydrochloride
Description: Potent and selective α7 nAChR agonist
Chemical Name: N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-furo[2,3-c]pyridine-5-carboxamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for PHA 543613 hydrochloride
PHA 543613 hydrochloride is a potent α7 nAChR agonist that displays selectivity over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. Positively influences sensory gating and memory in in vivo models of schizophrenia. Orally active and brain penetrant.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for PHA 543613 hydrochloride
PHA 543613 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for PHA 543613 hydrochloride
| M. Wt | 307.78 |
| Formula | C15H17N3O2.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1586767-92-1 |
| PubChem ID | 56972222 |
| InChI Key | YMTPSZUBRSEWNY-ZOWNYOTGSA-N |
| Smiles | O=C(C2=NC=C(OC=C3)C3=C2)N[C@@H]1C4CCN(CC4)C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PHA 543613 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 30.78 | 100 | |
| DMSO | 7.69 | 25 |
Preparing Stock Solutions for PHA 543613 hydrochloride
The following data is based on the product molecular weight 307.78. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 3.25 mL | 16.25 mL | 32.49 mL |
| 5 mM | 0.65 mL | 3.25 mL | 6.5 mL |
| 10 mM | 0.32 mL | 1.62 mL | 3.25 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.65 mL |
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Product Datasheets for PHA 543613 hydrochloride
References for PHA 543613 hydrochloride
References are publications that support the biological activity of the product.
Wishka et al (2006) Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the α7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia; synthesis and st J.Med.Chem. 49 4425 PMID: 16821801
Faghih et al (2008) Allosteric modulators of the α7 nicotinic acetylcholine receptor. J.Med.Chem. 51 701 PMID: 18198823
Acker et al (2008) Discovery of N-[3R,5R)-1-azabicyclo[3.2.1]ocy-3-yl]furo-[2,3-c]pyridine-5-carboxamide as an agonist of the α7 nicotinic acetylcholine receptor: in vitro and in vivo activity. Bioorg.Med.Chem.Letts. 18 3611 PMID: 1849016
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7 Citations for PHA 543613 hydrochloride
Citations are publications that use Tocris products. Selected citations for PHA 543613 hydrochloride include:
Macpherson et al (2014) The α7 nicotinic receptor agonist PHA-543613 hydrochloride inhibits Porphyromonas gingivalis-induced expression of interleukin-8 by oral keratinocytes. Front Med (Lausanne) 63 557 PMID: 24609617
Bali et al (2019) Facilitation and inhibition of firing activity and N-methyl-D-aspartate-evoked responses of CA1 hippocampal pyramidal cells by alpha7 nicotinic acetylcholine receptor selective compounds in vivo. Sci Rep 9 9324 PMID: 31249369
Sérriàre et al (2015) Assessment of the Protection of DArgic Neurons by an α7 Nicotinic Receptor Agonist, PHA 543613 Using [(18)F]LBT-999 in a Parkinson's Disease Rat Model. Cell Death Differ 2 61 PMID: 26389120
Foucault-Fruchard (2017) Neuroprotective effect of the alpha 7 nicotinic receptor agonist PHA 543613 in an in vivo excitotoxic adult rat model. Neuroscience 356 52 PMID: 28527955
Bali et al (2019) Cognitive enhancer effects of low Mem. doses are facilitated by an alpha7 nicotinic acetylcholine receptor agonist in scopolamine-induced amnesia in rats. Front Pharmacol 10 73 PMID: 30804787
Wang et al (2012) Electroacupuncture pretreatment attenuates cerebral ischemic injury through α7 nicotinic acetylcholine receptor-mediated inhibition of high-mobility group box 1 release in rats. J Neuroinflammation 9 24 PMID: 22277256
Bali et al (2015) Differential effects of α7 nicotinic receptor agonist PHA-543613 on spatial memory performance of rats in two distinct pharmacological dementia models. Behav Brain Res 278 404 PMID: 25447295
Do you know of a great paper that uses PHA 543613 hydrochloride from Tocris? Please let us know.
Reviews for PHA 543613 hydrochloride
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Cognitive enhancer effect of PHA 543613 in rat behavioral tests.
By
Zsolt Bali on 02/14/2018
Assay Type: In Vivo
Species: Rat
We used PHA 543613 in behavioral pharmacology experiments and tested its cognitive enhancer effect. PHA 543613 was found effective in different behavioral paradigms, and in different models of cognitive impairment. For instance, PHA 543613 dose-dependently reversed scopolamine induced transient amnesia in the spontaneous alternation (t-maze) task of rats.
Sometimes we experienced poor solubility in physiological saline. Slight warming and ultrasonics might help.
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