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.