NAS-181

Pricing Availability Delivery Time Qty
Cat.No. 1413 - NAS-181 | C19H26N2O4.2CH3SO3H | CAS No. 1217474-40-2
Description: Selective r5-HT1B antagonist. Active in vivo
Chemical Name: (2R)-2-[[[3-(4-Morpholinylmethyl)-2H-1-benzopyran-8-yl]oxy]methyl]morpholine dimethanesulfonate
Purity: ≥97% (HPLC)
Datasheet
Citations (1)
Literature

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
Storage Desiccate at -20°C
Purity ≥97% (HPLC)
CAS Number 1217474-40-2
PubChem ID 90479790
InChI Key VCIPBXUEKWCJAU-DZYJZKBLSA-N
Smiles CS(=O)(O)=O.CS(=O)(O)=O.N1(CC2=CC3=C(C(OC[C@H]4CNCCO4)=CC=C3)OC2)CCOCC1

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
phosphate buffered saline 53.86 100
DMSO 53.86 100
water 53.86 100

Preparing Stock Solutions

The following data is based on the product molecular weight 538.63. 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 1.86 mL 9.28 mL 18.57 mL
5 mM 0.37 mL 1.86 mL 3.71 mL
10 mM 0.19 mL 0.93 mL 1.86 mL
50 mM 0.04 mL 0.19 mL 0.37 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.

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

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

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


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

1 Citation for NAS-181

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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