Words similar to granisetron

Example sentences for: granisetron

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Previous studies concluded that R91 was an important interaction for the 5-HT 3 R agonist 5-hydroxytryptamine (5-HT), since the K i for 5-HT inhibition increased over 3000 fold as a result of the R91A mutation [ 24 ] . A change in K d for [ 3H]granisetron binding to R91A was also observed.
The effects of these mutations on the K i for analogs 1 and 2 are shown in figure 4B, 4Cand Table 1. Analog 1 inhibited [ 3H]-granisetron binding to W89F receptors with a K i of 170 ± 54 nM (7 ± 3.2 fold increase, p < 0.001) and W89Y receptors with a K i of 81 ± 14 nM (3.
[ 3H]granisetron does not appear to interact with any of the amino acids tested while d -tc interacts with only Y140, m CPBG and 5-HT with Y142 and lerisetron with both Y142 and Y152.
For K d determinations, 100 μl of homogenate was incubated at 37°C for 1 hour with varying concentrations of [ 3H]granisetron (NEN, MA).
It is apparent, however, that [ 3H]granisetron does occupy the same binding cleft as other 5-HT 3 R ligands as evidenced by the ability of 5-HT, m CPBG, d -tc and lerisetron to displace it from the binding site.