Human 5-HT3A -- Leu 282

Species Original Mutated to Mutation
Human Leu 282  

 

Rat Equivalent Leu 281    
Mouse Equivalent Leu 287 Cys L287C

 

mLeu287Cys

After the application of 1mM MTSET with 10uM 5-HT, the EC50 current was irreversibly reduced. The channels were locked in the open state. After the application of 1mM MTSES with 10uM 5-HT, there was no significant change.

 

Reeves DC, Goren EN, Akabas MH, Lummis SCR (2001) Structural and Electrostatic Properties of the 5-HT3 Receptor Pore Revealed by Substituted Cysteine Accessibility Mutagenesis. The Journal of Biological Chemistry 276(45):42035-42042

 

  Wild Type L287C
EC50 1.67 +/- 0.09 0.30 +/- 0.01
Hill Coefficient 2.0 +/- 0.1 3.0 +/- 0.4
Mg Inhibition (before MTSET) -41 +/- 3 -56 +/- 1
Mg Inhibition (after MTSET) -39 +/- 3 -40 +/- 1
Deactivation T50 ratio 0.95 +/- 0.03 1.54 +/- 0.16

 

Panicker S, Cruz H, Arrabit C, Slesinger PA (2002) Evidence for a Centrally Located Gate in the Pore of a Serotonin-Gated Ion Channel. The Journal of Neuroscience 22(5): 1629-1639

 

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