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 hydrate hydrochloride
- Product 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 hydrate hydrochloride
- CAS No.
- 148642-42-6
- 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 hydrate hydrochloride
- Synonyms
- GR 127935 hydrate hydrochloride;GR-127935 hydrochloride (GR127935);GR 127935 hydrochloride, 5-HT1B/1D receptor antagonist;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 hydrate;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 hydrate hydrochloride
- CBNumber
- CB12102772
- Molecular Formula
- C29H31N5O3HCl
- Formula Weight
- 0
- MOL File
- 148642-42-6.mol
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 hydrate hydrochloride Property
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble10mg/mL, clear
- form
- powder
- color
- white to beige
- Water Solubility
- Soluble to 100 mM in water
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- G5793
- Product name
- GR 127935 hydrochloride hydrate
- Purity
- >98% (HPLC), powder
- Packaging
- 10mg
- Price
- $303
- Updated
- 2024/03/01
- Product number
- 5.08014
- Product name
- GR 127935 Hydrochloride - CAS 148642-42-6 - Calbiochem
- Packaging
- 10mg
- Price
- $265
- Updated
- 2024/03/01
- Product number
- G5793
- Product name
- GR 127935 hydrochloride hydrate
- Purity
- >98% (HPLC), powder
- Packaging
- 50mg
- Price
- $1140
- Updated
- 2022/05/15
- Product number
- 29651
- Product name
- GR127935 (hydrochloride)
- Packaging
- 5mg
- Price
- $108
- Updated
- 2024/03/01
- Product number
- 29651
- Product name
- GR127935 (hydrochloride)
- Packaging
- 50mg
- Price
- $747
- Updated
- 2024/03/01
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 hydrate hydrochloride Chemical Properties,Usage,Production
Description
GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively). It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine . It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg. It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.
Uses
GR 127935 Hydrochloride is a selective and potent 5-HT1B/1D serotonin receptor antagonist.
Definition
ChEBI: GR 127935 hydrochloride is a hydrochloride obtained by reaction of GR 127935 with one equivalent of hydrochloric acid. 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. It has a role as a serotonergic antagonist. It contains a GR 127935(1+).
Biochem/physiol Actions
Potent, selective and orally active 5-HT1B/1D serotonin receptor antagonist.
storage
Desiccate at RT
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 hydrate hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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