Determinants involved in subtype-specific functions of rat trace amine-associated receptors 1 and 4.

ABSTRACT:

Aims

The trace amine-associated receptor (Taar) family displays high species- and subtype-specific pharmacology. Several trace amines such as β-phenylethylamine (β-PEA), p-tyramine and tryptamine are agonists at TA(1) but poorly activate rat and mouse Taar4.

Principal results

Using rat TA(1) and Taar4 chimera, we identified determinants in transmembrane helices 3 and 6, which, when replaced by the corresponding portion of rat TA(1) , can rescue cell surface expression of rat Taar4. When expressed at the cell surface, rat Taar4 pharmacology was very similar to that of TA(1) and coupled to the Gα(s) -protein/AC pathway. Our data suggest that binding pockets of Taar for surrogate agonists overlap between paralogs.

Conclusions

This implicates that the repertoire of Taa

SUBMITTER: Staubert C 

PROVIDER: S-EPMC3594682 | biostudies-literature | 2013 Mar

REPOSITORIES: biostudies-literature