Human 5-HT3A -- Phe 102

Species Original Mutated to Mutation
Human Phe 102  

 

Rat Equivalent Phe 101    
Mouse Equivalent Phe 107

Tyr

Asn

F107Y

F107N

 

mPhe107Tyr:


5-HT3 F107Y has a lower affinity for 5-HT (Ki = 203 vs 16 nM) and a higher EC(50) value (11 vs 1.2 uM) compared to wild-type receptors.

Activation of maximal 5-HT-activated currents mediated by the mutant receptor was slower than those of the wild-type receptor.

Steward LJ, Boess FG, Steele JA, Liu D, Wong N and Martin IL (2000) Importance of Phenylalanine 107 in Agonist Recognition by the 5-Hydroxytryptamine3A Receptor. Molecular Pharmacology 57:1249-1255

 

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mPhe107Asn

The 5-HT3 F107N mutant has a higher affinity for 5-HT (1.6 vs 16 nM), a reduced EC50 for the agonist (0.2 vs 1.2 uM) compared to wid-type receptors.

The mutant F107N was activated by acetylcholine (EC50 = 260 uM). The response to acetylcholine was blocked by the 5-HT3 antagonist renzapride.

Steward LJ, Boess FG, Steele JA, Liu D, Wong N and Martin IL (2000) Importance of Phenylalanine 107 in Agonist Recognition by the 5-Hydroxytryptamine3A Receptor. Molecular Pharmacology 57:1249-1255

 

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