NAS-181

Cat. No. 1413

NAS-181 C19H26N2O4.2CH3SO3H [1217474-40-2]

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Chemical Name: (2R)-2-[[[3-(4-Morpholinylmethyl)-2H-1-benzopyran-8-yl]oxy]methyl]morpholine dimethanesulfonate

Biological Activity

Potent, selective antagonist at the rat 5-HT1B receptor (Ki = 47 nM). Increases synthesis and metabolism of 5-HT in the brain following systemic administration and improves passive avoidance retention performance in vivo. Increases subthalamic nucleus-triggered complex EPSCs and burst firing in SNr GABA neurons

Technical Data

M.Wt:
538.63
Formula:
C19H26N2O4.2CH3SO3H
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>97 %
Storage:
Desiccate at -20°C
CAS No:
1217474-40-2

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Ding et al (2013) Presynaptic serotonergic gating of the subthalamonigral glutamatergic projection. J.Neurosci. 33 4875. PMID: 23486958.

Eriksson et al (2008) Blockade of 5-HT1B receptors facilitates contextual aversive learning in mice by disinhibition of cholinergic and glutamatergic neurotransmission. Neuropharmacology 54 1041. PMID: 18394658.

Stenfors et al (2000) Enhanced 5-HT metabolism and synthesis rate by the new selective r5-HT1B receptor antagonist, NAS-181 in the rat brain. Neuropharmacology 39 553. PMID: 10728876.

Berg et al (1998) (R)-(+)-2-[[[3-Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl]morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist. J.Med.Chem. 41 1934. PMID: 9599242.

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Citations are publications that use Tocris products. Selected citations for NAS-181 include:

Xiao et al (2008) Release of glutamate and CGRP from trigeminal ganglion neurons: Role of calcium channels and 5-HT1 receptor signaling. Neuron 4 12. PMID: 18416824.

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Keywords: NAS-181, supplier, Selective, r5-HT1B, antagonist, Active, vivo, Serotonin, Receptors, Tocris Bioscience, 5-HT1B Receptor Antagonist products

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