The recombinant 5-HT1A receptor: G protein coupling and signalling pathways

The 5-hydroxytryptamine 5-HT1A receptor was one of the first G protein coup led receptors whose cDNA and gene were isolated by molecular cloning method s. Transfection of the cDNA of this receptor into cells previously bearing no 5-HT receptors has resulted in the acquisition of large amounts of infor mation regarding potential signal transduction pathways linked to the recep tor, correlations of receptor structure to its various functions, and pharm acological properties of the receptor. Transfection studies with the 5-HT1A receptor have generated critical new information that might otherwise have been elusive. This information notably includes the discovery of unsuspect ed novel signalling linkages, the elucidation of the mechanisms of receptor desensitization, the refinement of models of the receptor pharmacophore, a nd the development of silent receptor antagonists, among others. The curren t review summarizes the most important studies of the recombinant 5-HT1A re ceptor in the decade since the identificiation of its cDNA.