GR 203040

Names

[ Name ]:
GR 203040

[Synonym ]:
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)

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]:

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

[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

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 ...

Related Compounds

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