product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
PNU 120596
catalog :
2498/5
quantity :
5 mg (also 25 mg)
price :
127 USD
more info or order :
citations: 15
Reference
Noviello C, Gharpure A, Mukhtasimova N, Cabuco R, Baxter L, Borek D, et al. Structure and gating mechanism of the α7 nicotinic acetylcholine receptor. Cell. 2021;184:2121-2134.e13 pubmed publisher
Barykin E, Garifulina A, Kruykova E, Spirova E, Anashkina A, Adzhubei A, et al. Isomerization of Asp7 in Beta-Amyloid Enhances Inhibition of the α7 Nicotinic Receptor and Promotes Neurotoxicity. Cells. 2019;8: pubmed publisher
Bali Z, Nagy L, Budai D, Hernadi I. 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. 2019;9:9324 pubmed publisher
Giménez Gómez P, Pérez Hernández M, Gutierrez Lopez M, Vidal R, Abuin Martínez C, O Shea E, et al. Increasing kynurenine brain levels reduces ethanol consumption in mice by inhibiting dopamine release in nucleus accumbens. Neuropharmacology. 2018;135:581-591 pubmed publisher
Zhang Q, Du Y, Zhang J, Xu X, Xue F, Guo C, et al. Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor. PLoS ONE. 2015;10:e0137588 pubmed publisher
daCosta C, Free C, Sine S. Stoichiometry for α-bungarotoxin block of α7 acetylcholine receptors. Nat Commun. 2015;6:8057 pubmed publisher
Thomsen M, Zwart R, Ursu D, Jensen M, Pinborg L, Gilmour G, et al. α7 and β2 Nicotinic Acetylcholine Receptor Subunits Form Heteromeric Receptor Complexes that Are Expressed in the Human Cortex and Display Distinct Pharmacological Properties. PLoS ONE. 2015;10:e0130572 pubmed publisher
Chatzidaki A, Fouillet A, Li J, Dage J, Millar N, Sher E, et al. Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons. PLoS ONE. 2015;10:e0125116 pubmed publisher
Kasheverov I, Shelukhina I, Kudryavtsev D, Makarieva T, Spirova E, Guzii A, et al. 6-bromohypaphorine from marine nudibranch mollusk Hermissenda crassicornis is an agonist of human α7 nicotinic acetylcholine receptor. Mar Drugs. 2015;13:1255-66 pubmed publisher
John D, Shelukhina I, Yanagawa Y, Deuchars J, Henderson Z. Functional alpha7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus. Brain Res. 2015;1601:15-30 pubmed publisher
Maldifassi M, Atienza G, Arnalich F, López Collazo E, Cedillo J, Martín Sánchez C, et al. A new IRAK-M-mediated mechanism implicated in the anti-inflammatory effect of nicotine via α7 nicotinic receptors in human macrophages. PLoS ONE. 2014;9:e108397 pubmed publisher
Pandya A, Yakel J. Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT₁a receptor antagonist. Neuropharmacology. 2013;70:35-42 pubmed publisher
Yamauchi J, Gomez K, Grimster N, Dufouil M, Nemecz A, Fotsing J, et al. Synthesis of selective agonists for the ?7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates. Mol Pharmacol. 2012;82:687-99 pubmed
Pérez Alvarez A, Hernández Vivanco A, Alonso y Gregorio S, Tabernero A, McIntosh J, Albillos A. Pharmacological characterization of native ?7 nicotinic ACh receptors and their contribution to depolarization-elicited exocytosis in human chromaffin cells. Br J Pharmacol. 2012;165:908-21 pubmed publisher
David R, Ciuraszkiewicz A, Simeone X, Orr Urtreger A, Papke R, McIntosh J, et al. Biochemical and functional properties of distinct nicotinic acetylcholine receptors in the superior cervical ganglion of mice with targeted deletions of nAChR subunit genes. Eur J Neurosci. 2010;31:978-93 pubmed publisher
product information
brand :
Tocris, a Bio-Techne Brand
catalog number base :
2498
SKU :
2498/5
product name :
PNU 120596
Description :
Positive allosteric modulator of 7 nAChRs; active in vivo
target :
Nicotinic (a7) Receptor Modulators
category :
Small Molecules
unit size :
5 mg (also 25 mg)
purity :
99%
observed molecular weight :
311.72
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
PNU 120596 is a positive allosteric modulator of 7 neuronal nicotinic acetylcholine receptors (EC50 = 216 nM), with no detectable effect on 4 2, 3 4 and 9 10 receptors. Active in vivo following systemic administration. Neuroprotective in an in vivo model of transient focal cerebral ischemia.
extended description :
Positive allosteric modulator of 7 nAChRs; active in vivo
chemical name text :
N-(5-Chloro-2,4-dimethoxyphenyl)-N -(5-methyl-3-isoxazolyl)-urea
formula :
C 13 H 14 ClN 3 O 4
formula text :
C13H14ClN3O4
cas num :
501925-31-1
USD :
127 USD
product details :
Positive allosteric modulator of 7 nAChRs; active in vivo
storage :
Desiccate at +4°C
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK