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
Technical Data
Solubility
Calculators
Datasheets
References
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
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
Safety Datasheet
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References
References are publications that support the products' biological activity.
Berget 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
Erikssonet 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
Stenforset 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
Dinget al (2013) Presynaptic serotonergic gating of the subthalamonigral glutamatergic projection. J.Neurosci. 33 4875 PMID: 23486958