ChemicalBook > CAS DataBase List > 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

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
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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
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
G5793
Product name
GR 127935 hydrochloride hydrate
Purity
>98% (HPLC), powder
Packaging
10mg
Price
$303
Updated
2024/03/01
Sigma-Aldrich
Product number
5.08014
Product name
GR 127935 Hydrochloride - CAS 148642-42-6 - Calbiochem
Packaging
10mg
Price
$265
Updated
2024/03/01
Sigma-Aldrich
Product number
G5793
Product name
GR 127935 hydrochloride hydrate
Purity
>98% (HPLC), powder
Packaging
50mg
Price
$1140
Updated
2022/05/15
Cayman Chemical
Product number
29651
Product name
GR127935 (hydrochloride)
Packaging
5mg
Price
$108
Updated
2024/03/01
Cayman Chemical
Product number
29651
Product name
GR127935 (hydrochloride)
Packaging
50mg
Price
$747
Updated
2024/03/01
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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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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 Suppliers

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148642-42-6, 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 hydrochlorideRelated Search:

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  • GR 127935 hydrate hydrochloride
  • 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
  • GR-127935 hydrochloride (GR127935)
  • 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
  • GR 127935 hydrochloride, 5-HT1B/1D receptor antagonist
  • 148642-42-6
  • C29H31N5O3HCl