Human 5-HT3A -- Tyr 284

Species Original Mutated to Mutation
Human Tyr 284  

 

Rat Equivalent Tyr 283    
Mouse Equivalent Tyr 289 Cys Y289C

 

mTyr289Cys

No current was detected after the application of 5-HT up to 1mM or when it was perfused with 10mM dithiothreitol for 3 minutes. After the application of 1mM MTSET with 10uM 5-HT, no current was detected. After the application of 1mM MTSES with 10uM 5-HT, no current was detected.

 

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 Y289C
EC50 1.67 +/- 0.09 not tested
Hill Coefficient 2.0 +/- 0.1 not tested
Mg Inhibition (before MTSET) -41 +/- 3 -14 +/- 3
Mg Inhibition (after MTSET) -39 +/- 3

-14 +/- 3

Deactivation T50 ratio 0.95 +/- 0.03 1.07 +/- 0.04

 

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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