Understanding neurotransmitter receptors: molecular biology-based strategies

Neurotransmitter receptor proteins can be divided into GPCRs and ligand-gated ion channels. Members within each family utilize a similar signalling mechanism and are structurally related. Multiple receptor subtypes are expressed for individual neurotransmitters, generating orders of complexity that have been exploited for therapeutic intervention. GPCRs have been cloned and extensively studied by using a range of molecular biological strategies, particularly recombinant expression systems. These have located functional domains for ligand binding and G-protein coupling. A combination of molecular biology and computer modelling has increased our understanding of receptor activation and will aid drug design.