Biological Activity
Potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types. Centrally active following oral administration.
Licensing Information
Sold under license
Technical Data
| M. Wt | 534.06 |
| Formula | C29H31N5O3.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 148642-42-6 |
| PubChem ID | 11497466 |
| InChI Key | SRVVUYIJVBLEJI-UHFFFAOYSA-N |
| Smiles | Cl.COC1=C(C=C(NC(=O)C2=CC=C(C=C2)C2=CC=C(C=C2C)C2=NOC(C)=N2)C=C1)N1CCN(C)CC1 |
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 | |||
| water | 49.76 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 534.06. 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 | 1.87 mL | 9.36 mL | 18.72 mL |
| 5 mM | 0.37 mL | 1.87 mL | 3.74 mL |
| 10 mM | 0.19 mL | 0.94 mL | 1.87 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Clitherow et al (1994) Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists. J.Med.Chem. 37 2253 PMID: 8057272
De Vries et al (1996) Blockade of porcine carotid vascular response to sumatriptan by GR 127935, a selective 5-HT1D receptor antagonist. Br.J.Pharmacol. 118 85 PMID: 8733580
Knobelman et al (2001) Genetic regulation of extracellular serotonin by 5-hydroxytryptamine1A and 5-hydroxytryptamine1B autoreceptors in different brain regions of the mouse. J.Pharmacol.Exp.Ther. 298 1083 PMID: 11504805
Keywords: GR 127935 hydrochloride, supplier, Potent, selective, 5-HT1B/1D, antagonist, Serotonin, Receptors, GR127935, hydrochloride, 5-HT1D, Receptors, 5-HT1B, Receptors, 5-HT1D, Receptors, Tocris Bioscience
