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