Disparate ligand-mediated Ca(2+) responses by wild-type, mutant Ser(200)Ala and Ser(204)Ala alpha(2A)-adrenoceptor: G(alpha15) fusion proteins: evidence for multiple ligand-activation binding sites.

ABSTRACT: Ligand : receptor interactions were analysed at wt, mutant Ser(200)Ala and Ser(204)Ala alpha(2A) ARs by measuring Ca(2+) responses in CHO-K1 cells either by co-expression with a G(alpha15) protein or at a receptor : G(alpha15) protein stoichiometry of 1.0 using fusion proteins. The magnitude of the UK 14304-mediated Ca(2+) response as elicited by a G(alpha15) protein was largest with both mutant Ser(200)Ala and Ser(204)Ala alpha(2A)ARs compared to the wt alpha(2A) AR in the co-expression and fusion protein experiments. The activation profiles of the wt and both mutant alpha(2A) ARs as analysed by a series of alpha(2) AR agonists differed. d-Medetomidine and clonidine appeared most efficacious at the Ser(204)Ala alpha(2A) AR, whereas oxymetazoline was also partially active at the Ser(200)Al

SUBMITTER: Pauwels PJ 

PROVIDER: S-EPMC1572214 | biostudies-literature | 2000 Aug

REPOSITORIES: biostudies-literature