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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)
Citations (1)
Literature (4)

Biological Activity for NAS-181

NAS-181 is a 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 for NAS-181

M. Wt 538.63
Formula C19H26N2O4.2CH3SO3H
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 1217474-40-2
PubChem ID 90479790
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for NAS-181

Solvent Max Conc. mg/mL Max Conc. mM
water 53.86 100
DMSO 53.86 100

Preparing Stock Solutions for NAS-181

The following data is based on the product molecular weight 538.63. 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.

Select a batch to recalculate based on the batch molecular weight:
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 for NAS-181

Certificate of Analysis / Product Datasheet
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References for NAS-181

References are publications that support the biological activity of the product.

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

If you know of a relevant reference for NAS-181, please let us know.

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Keywords: NAS-181, NAS-181 supplier, Selective, r5-HT1B, antagonist, Active, vivo, Serotonin, Receptors, 5-HT1B, 1413, 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

Do you know of a great paper that uses NAS-181 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

GPCR Product Listing

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
5-HT Receptors Scientific Review

5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

Cardiovascular Poster

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Parkinson's Poster

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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.