Human 5-HT3A -- Pro 216
|Rat Equivalent||Thr 215|
|Mouse Equivalent||Pro 221|
The mutation was made in the human 5-HT3A subunit at Pro216. This residue was numbered Pro193 in the paper in which numbering began at the end of the signal sequence.
In order to identify the potency of meta-chlorophenylbiguanide (mCPBG) in human 5-HT3A receptors, the recombinant human and rat 5-HT3A receptors were expressed in Xenopus Oocytes by cRNA injection and 5-HT-evoked currents were recorded using two-electorde voltage-clamp. The effect of replacing human Leu215, Pro216, Tyr217, Arg219, Met223, Ser225 and Tyr228 (numbering from the beginning of the signal sequence) by the equivalent residues (Phe, Thr, Lys,Gln, Ile, Thr and Ser) in the rat was to increase the potency of mCPBG as an agonist at the mutant human 5-HT3A receptor by 13-fold.
Mochizuki S.,Miyake A.,Furuichi K. (1999) Identification of a domain affecting agonist potency of meta-chlorophenylbiguanide in 5-HT3 receptors. European Journal of Pharmacology 369:125-132
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