This chapter focuses on the bioenergetics, mechanism, and molecular basis of biogenic amine transport. It discusses some kinetic, biochemical, and pharmacological studies. The neurotransmitter transport systems seem to be equipped very well to achieve high concentration gradients by utilization of pre-existing ion gradients, created and maintained by ion pumps. The putative amine transporter from bovine adrenal chromaffin granules has been partially purified in a single step utilizing affinity chromatography. In addition to the catecholamine-rich chromaffin granules of adrenal medulla, other intracellular organelles from a wide variety of secretory cells accumulate biogenic amines. The amine transporter from bovine chromaffin granules has been solubilized with sodium cholate in the presence of soybean phospholipids. Despite the profusion of noncovalent inhibitors and ligands of the catecholamine transporter, very little information has been gathered about covalent modifiers of the protein. Extraction of chromaffin granule membranes with 1% cholate renders a soluble fraction that can be reconstituted into liposomes.