Human 5-HT3A -- Ile 278

Species Original Mutated to Mutation
Human Ile 278

Glu

Lys

I278E

I278K

Rat Equivalent Ile 277    
Mouse Equivalent Ile 283 Cys I283C

 

hIle278Glu

 

Specific binding of [3H]granisetron was very low. (40 +/- 7 fmol (mg protein)-1) There was no response to a saturating concentration (30uM) of 5-HT.

 

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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hIle278Lys

Reasonable levels of specific binding of [3H]granisetron was observed. (500 +/- 95 fmol (mg protein)-1) There was no response to a saturating concentration (30uM) of 5-HT.

 

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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mIle283Cys

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 I283C
EC50 1.67 +/- 0.09 1.00 +/- 0.02
Hill Coefficient 2.0 +/- 0.1 3.2 +/- 0.1
Mg Inhibition (before MTSET) -41 +/- 3 -18 +/- 2
Mg Inhibition (after MTSET) -39 +/- 3 -18 +/-2
Deactivation T50 ratio 0.95 +/- 0.03 0.97 +/- 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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