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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)
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 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for NAS-181
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
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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
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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.
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