Human 5-HT3A -- Val 237

Species Original Mutated to Mutation
Human Val 237 Ile

V237I

Rat Equivalent Val 236    
Mouse Equivalent Ile 242 Val I242V

 

hVal237Ile

When the quintuple mutation of hM223I, hE224D, hS225I, hY217Q and hR219K was combined with hY228S and V237I, there was a further decrement of 2-fold of the IC50 value of (+)-Tubocurarine relative to the quintuple mutant.

Hope AG, Belelli D, Mair ID, Lambert JJ, Peters JA (1999) Molecular Determinants of (+)- Tubocurarine Binding at Recombinant 5-Hydroxytryptamine3A Receptor Subunits. Molecular Pharmacology 55:1037-1043

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mIle242Val

In a single point mutation of I242V, the IC50 value for (+)- Tubocurarine was indistinguishable from the wildtype.

When the quintuple mutation of mI228M, mD229E, mI230S, mQ222Y and mK224R was combined with mS233Y and mI242V, there was a further increment of 3-fold of the IC50 value of the (+)-Tubocurarine relative to the quintuple mutant.

Hope AG, Belelli D, Mair ID, Lambert JJ, Peters JA (1999) Molecular Determinants of (+)- Tubocurarine Binding at Recombinant 5-Hydroxytryptamine3A Receptor Subunits. Molecular Pharmacology 55:1037-1043

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