Human 5-HT3A -- Phe 276

Species Original Mutated to Mutation
Human Phe 276 (3')

Glu

Lys

F276E

F276K

Rat Equivalent Phe 275    
Mouse Equivalent Phe 281 Cys F281C

 

hPhe276Glu

Specific binding of [3H]granisetron was not significantly different from zero. (8 +/- 6 fmol (mg protein)-1)

Gunthorpe MJ, Peters JA, Gill CH, Lambert JJ, Lummis SCR (2000) The 4'Lysine in the Putative Channel Lining Domain Affects Desensitization but not the Single-Channel Conductance of Recombinant Homomeric 5-HT3A Receptors. Journal of Physiology 522(2):187-198

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hPhe276Lys

Specific binding of [3H]granisetron was not significantly different from zero. (15 +/- 12 fmol (mg protein)-1)

 

Gunthorpe MJ, Peters JA, Gill CH, Lambert JJ, Lummis SCR (2000) The 4'Lysine in the Putative Channel Lining Domain Affects Desensitization but not the Single-Channel Conductance of Recombinant Homomeric 5-HT3A Receptors. Journal of Physiology 522(2):187-198

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mPhe281Cys

After the application of 1mM MTSET with 10uM 5-HT, there was no significant change. 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 F281C
EC50 1.67 +/- 0.09 0.83 +/- 0.02
Hill Coefficient 2.0 +/- 0.1 2.0 +/- 0.1
Mg Inhibition (before MTSET) -41 +/- 3 -14 +/- 2
Mg Inhibition (after MTSET) -39 +/- 3 -14 +/- 1
Deactivation T50 ratio 0.95 +/- 0.03 1.40 +/- 0.07

 

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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