GR 203040

Modify Date: 2024-02-05 19:27:28

GR 203040 Structure
GR 203040 structure
Common Name GR 203040
CAS Number 168398-02-5 Molecular Weight 437.37
Density N/A Boiling Point 560.4ºC at 760mmHg
Molecular Formula C20H26Cl2N6O Melting Point N/A
MSDS USA Flash Point 292.7ºC

 Use of GR 203040


GR203040 is an orally active NK1 receptor antagonist with a pKi of 10.3. GR203040 shows potent antiemetic activity[1].

 Names

Name N-[[2-methoxy-5-(tetrazol-1-yl)phenyl]methyl]-2-phenylpiperidin-3-amine
Synonym More Synonyms

 GR 203040 Biological Activity

Description GR203040 is an orally active NK1 receptor antagonist with a pKi of 10.3. GR203040 shows potent antiemetic activity[1].
Related Catalog
Target

pKi: 10.3 (NK1 receptor)[1]

References

[1]. Ward P, et al. Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity. J Med Chem. 1995 Dec 22;38(26):4985-92.  

 Chemical & Physical Properties

Boiling Point 560.4ºC at 760mmHg
Molecular Formula C20H26Cl2N6O
Molecular Weight 437.37
Flash Point 292.7ºC
Exact Mass 364.20100
PSA 76.89000
LogP 2.97350
Vapour Pressure 1.37E-12mmHg at 25°C

 Safety Information

RIDADR NONH for all modes of transport

 Articles6

More Articles
Attenuation of the gerbil writhing response by mu-, kappa- and delta-opioids, and NK-1, -2 and -3 receptor antagonists.

Pharmacol. Biochem. Behav. 79(1) , 125-35, (2004)

Mu-, kappa- and delta-opioid receptor agonists are reported to attenuate the acetic-acid-induced abdominal constriction response in mice. NK-1, -2 and -3 receptor antagonists also display activity in ...

Brain uptake and receptor binding of two [11C]labelled selective high affinity NK1-antagonists, GR203040 and GR205171--PET studies in rhesus monkey.

Neuropharmacology 39(4) , 664-70, (2000)

Two high affinity and selective NK1-receptor antagonists, GR203040 and GR205171, were labelled with 11C and used in a series of experiments in rhesus monkeys. The purpose of these studies was to evalu...

The broad-spectrum anti-emetic activity of the novel non-peptide tachykinin NK1 receptor antagonist GR203040.

Br. J. Pharmacol. 116(8) , 3158-63, (1995)

1. Following our earlier observations that the tachykinin NK1 receptor antagonist CP-99,994 is an effective anti-emetic in ferrets, we have examined the anti-emetic effects of a more potent and novel ...

 Synonyms

3-Piperidinamine,N-[[2-methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-,hydrochloride(1:2),(2S,3S)
3-Piperidinamine,N-[[2-methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-,dihydrochloride,(2S-cis)
3-Piperidinamine,N-[[2-methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-,dihydrochloride,(2S,3S)-(9CI)
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: GR-203040
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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