Human 5-HT3A -- Asn 269

Species Original Mutated to Mutation
Human Asn 269  

 

Rat Equivalent Asp 268    
Mouse Equivalent Asp 274 Cys D274C

 

mAsp274Cys

After the application of 1mM MTSET with 10uM 5-HT, The EC50 current was irreversibly enhanced. After the application of 1mM MTSES with 10uM 5-HT, the EC50 current decreased.

 

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 D274C
EC50 1.67 +/- 0.09 1.27 +/- 0.12
Hill Coefficient 2.0 +/- 0.1 2.3 +/- 0.2
Mg Inhibition (before MTSET) -41 +/- 3 -18 +/- 2
Mg Inhibition (after MTSET) -39 +/- 3 -20 +/- 2
Deactivation T50 ratio 0.95 +/- 0.03 1.97 +/- .13

 

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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