Human 5-HT3A -- Glu 93

Species Original Mutated to Mutation
Human

Glu 93

Gln

Asp

E93Q

E93D

Rat Equivalent Glu 92    
Mouse Equivalent Glu 98    

 

hGlu93Gln

EC50 (uM) Granisetron Inhibition (IC50) (nM) [3H]mCPBG (Kd) [3H]MCPBG (Granisetron Inhibition Ki) (nM) [3H] GR65630 (Kd) [3H]GR65630 (Granisetron Inhibition Ki) (nM) [3H]GR65630 (mCPBG Inhibition Ki)
Wild Type 2.1 +/- 0.6 0.14 +/- 0.1 12.7 +/- 1.9 2.0 +/- 0.6 1.4 +/- 0.3 1.4 +/- 0.4 11 +/- 4
E93Q 2.0 +/- 1.4 0.19 +/- 0.1 29 +/- 12 4.3 +/- 2.1 2.3 +/- 0.8 0.8 +/- 0.3 5.3 +/- 1.8

 

Schreiter C, Hovius R, Costioli M, Pick H, Kellenberger S, Schild L, Vogel H (2003) Characterization of the Ligand-Binding Site of the Serotonin 5-HT3 Receptor. The Journal of Biological Chemistry 278(25):22709-22716


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hGlu93Asp

EC50 (uM) Granisetron Inhibition (IC50) (nM) [3H]mCPBG (Kd) [3H]MCPBG (Granisetron Inhibition Ki) (nM) [3H] GR65630 (Kd) [3H]GR65630 (Granisetron Inhibition Ki) (nM) [3H]GR65630 (mCPBG Inhibition Ki)
Wild Type 2.1 +/- 0.6 0.14 +/- 0.1 12.7 +/- 1.9 2.0 +/- 0.6 1.4 +/- 0.3 1.4 +/- 0.4 11 +/- 4
E93D 2.1 +/- 0.9 0.25 +/- 0.1 12.8 +/- 3.5 1.4 +/- 0.4 3.5 +/- 0.3 1.8 +/- 0.4 12 +/- 2

 

Schreiter C, Hovius R, Costioli M, Pick H, Kellenberger S, Schild L, Vogel H (2003) Characterization of the Ligand-Binding Site of the Serotonin 5-HT3 Receptor. The Journal of Biological Chemistry 278(25):22709-22716

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