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Submit ReviewGR 127935 hydrochloride
Description: Potent and selective 5-HT1B and 5-HT1D antagonist
Chemical Name: N-[4-Methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1,1'-biphenyl-4-carboxamide hydrochloride
Purity: ≥99% (HPLC)
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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 the degree 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 |
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References
References are publications that support the biological activity of the product.
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 sumatr. 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
If you know of a relevant reference for GR 127935 hydrochloride, please let us know.
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8 Citations for GR 127935 hydrochloride
Citations are publications that use Tocris products. Selected citations for GR 127935 hydrochloride include:
Wei et al (2010) JNK regulates serotonin-mediated proliferation and migration of pulmonary artery smooth muscle cells. Am J Physiol Lung Cell Mol Physiol 298 L863 PMID: 20228179
Morikawa et al (2006) Antimigraine drug, zolmitriptan, inhibits high-voltage activated calcium currents in a population of acutely dissociated rat trigeminal sensory neurons. Mol Pain 2 10 PMID: 16549032
Masterson and Durham (2010) DHE repression of ATP-mediated sensitization of trigeminal ganglion neurons. Headache 50 1424 PMID: 20561068
Khatri et al (2014) Lasting neurobehavioral abnormalities in rats after neonatal activation of serotonin 1A and 1B receptors: possible mechanisms for serotonin dysfunction in autistic spectrum disorders. Psychopharmacology (Berl) 231 1191 PMID: 23975037
Eriksson et al (2013) Bidirectional regulation of emotional memory by 5-HT1B receptors involves hippocampal p11. J Clin Endocrinol Metab 18 1096 PMID: 23032875
Baillie et al (2012) Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres. Mol Psychiatry 63 362 PMID: 22691374
Li et al (2017) Pericytes impair capillary blood flow and motor function after chronic spinal cord injury. Nat Med 23 733 PMID: 28459438
Akerman et al (2013) Endocannabinoids in the brainstem modulate dural trigeminovascular nociceptive traffic via CB1 and "triptan" receptors: implications in migraine. J Neurosci 33 14869 PMID: 24027286
Do you know of a great paper that uses GR 127935 hydrochloride from Tocris? Please let us know.
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