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Merck
CN

SML0780

GR203040

≥98% (HPLC)

Synonym(s):

(2S,3S)-N-[[2-Methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-3-piperidinamine hydrochloride (1:2)

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About This Item

Empirical Formula (Hill Notation):
C20H24N6O · 2HCl
CAS Number:
168398-02-5
Molecular Weight:
437.37
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder

Key Documents

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InChI key

UYDCUPIPQXAELR-OINVMNEBSA-N

InChI

1S/C20H24N6O.2ClH/c1-27-19-10-9-17(26-14-23-24-25-26)12-16(19)13-22-18-8-5-11-21-20(18)15-6-3-2-4-7-15;;/h2-4,6-7,9-10,12,14,18,20-22H,5,8,11,13H2,1H3;2*1H/t18-,20-;;/m0../s1

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H2O: 10 mg/mL, clear (warmed)

storage temp.

2-8°C

Biochem/physiol Actions

GR203040 is a high affinity, non-peptide tachykinin NK1 receptor antagonist.
GR203040 is a high affinity, non-peptide tachykinin NK1 receptor antagonist. GR203040 inhibits substance P binding to human NK1 receptors in CHO cells with a pKi or 10.3. The compound prevents emisis, and reduces bladder damage induced by radiation, cisplatin and cyclophosphamide. 11C-labeled GR203040 is used as a radioligand to image NK1 receptors in the CNS by PET scanning.

Storage Class

13 - Non Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
073M4621V

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C J Gardner et al.
British journal of pharmacology, 116(8), 3158-3163 (1995-12-01)
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 NK1 receptor antagonist, GR203040, against various emetic stimuli in the
P Ward et al.
Journal of medicinal chemistry, 38(26), 4985-4992 (1995-12-22)
The antiemetic, pharmacokinetic, and metabolic profile of CP-99,994, a potent NK1 receptor antagonist, has been carefully evaluated. As a result we began a medicinal chemistry program which initially identified a 3-furanyl analogue (6) with improved antiemetic potency and a methyl
A Alfieri et al.
General pharmacology, 29(2), 245-250 (1997-08-01)
1. The effect of the tachykinin neurokinin1 (NK1) receptor antagonist GR203040 on cyclophosphamide (CYP)-induced bladder damage was investigated in rats and ferrets. The 5-hydroxytryptamine3 receptor antagonists ondansetron and granisetron were similarly examined in ferrets. 2. In the rat, GR203040 (10
C J Gardner et al.
Regulatory peptides, 65(1), 45-53 (1996-08-27)
It has been demonstrated recently that antagonists of the tachykinin NK1 receptor, specifically CP-99,994 and GR203040, possess anti-emetic activity in a range of species. To optimise this activity, a series of analogues based around the structure of GR203040 have been
M Bergström et al.
Neuropharmacology, 39(4), 664-670 (2000-03-23)
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 evaluate the brain uptake pattern and to explore the
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