Human 5-HT3A -- Trp 55

Species Original Mutated to Mutation
Human Trp 55  

 

Rat Equivalent Trp 54    
Mouse Equivalent Trp 60 Ser W60S

 

 

mTrp60Ser

The EC50 and Hill values for the 5-HT3AW60S mutant were not significantly different from those of the wild-type receptor. The mutation had no effect of receptor function.

 

Wild Type W60S
[3H] Granisetron (Kd) 0.17 +/- 0.003 0.21 +/- 0.05
[3H] Granisetron (nH) 1.03 +/- 0.11 0.84 +/- 0.15
[3H] mCPBG (Kd)

1.48 +/- 0.09

1.31 +/- 0.13
[3H] mCPBG (nH) 1.07 +/- 0.02 0.90 +/- 0.06
5-HT3 (EC50) 2.10 +/-0.40 2.26 +/- 0.21
5-HT3 (nH) 2.22 +/- 0.20 1.71 +/- 0.14

Spier AD, Lumis SCR (2000) The Role of Tryptophan Residues in the 5-Hydroxytryptamine3 Receptor Ligand Binding Domain. The Journal of Biological Chemistry 275(8): 5620-5625

 

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