Human 5-HT3A -- Ile 290

Species Original Mutated to Mutation
Human Ile 290  

 

Rat Equivalent Ile 289    
Mouse Equivalent Ile 295 Cys I295C

 

mIle295Cys

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, 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 I295C
EC50 1.67 +/- 0.09

0.27 +/- 0.02

Hill Coefficient 2.0 +/- 0.1 1.9 +/- 0.2
Mg Inhibition (before MTSET) -41 +/- 3 -37 +/- 3
Mg Inhibition (after MTSET) -39 +/- 3 -29 +/- 2
Deactivation T50 ratio 0.95 +/- 0.03 2.68 +/- 0.27

 

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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