GR 203040
GR 203040 structure
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Common Name | GR 203040 | ||
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| 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 | |
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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 several visceral pain models. As the gerbil NK-1 receptor i... |
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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 evaluate the brain uptake pattern and to explore the potential u... |
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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 NK1 receptor antagonist, GR203040, against various emetic s... |
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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. 38(26) , 4985-92, (1995) 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 antiemeti... |
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The NK1 antagonist GR203040 inhibits cyclophosphamide-induced damage in the rat and ferret bladder.
Gen. Pharmacol. 29(2) , 245-50, (1997) 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 exam... |
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GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity.
Regul. Pept. 65(1) , 45-53, (1996) 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... |