Dopaminergic Neurotransmission*
John A. Schetz
University of North Texas Health Science Center, Fort Worth, Texas
Search for more papers by this authorDavid R. Sibley
National Institutes of Health, Bethesda, Maryland
Search for more papers by this authorJohn A. Schetz
University of North Texas Health Science Center, Fort Worth, Texas
Search for more papers by this authorDavid R. Sibley
National Institutes of Health, Bethesda, Maryland
Search for more papers by this authorAbstract
Dopamine is a neurotransmitter in the central and peripheral nervous systems where it regulates numerous physiological processes. Within the CNS, dopamine is known to regulate emotion, reward, cognition, memory, endocrine functions, and motor control. Alterations in dopaminergic transmission are known to be involved in the etiology and/or therapy of a number of neurological and psychiatric disorders including Parkinson's disease, Tourette's syndrome, attention deficit hyperactivity disorder, schizophrenia and substance use. One of the hallmarks of these disorders is that they are all treated with drugs that either enhance or impede dopaminergic transmission. Dopamine exerts its effects by binding to and activating five different receptor proteins that are members of the G protein-coupled receptor (GPCR) family. These five receptors are made up of two subfamilies: D1-like D2-like. The D1 and D5 receptors comprise the D1-like subfamily while the D2, D3 and D4 receptors make up the D2-like subfamily. In general, the D1-like receptors stimulate the production of the ubiquitous second messenger cAMP whereas D2-like receptors suppress cAMP production and also couple to additional signaling pathways. Different therapeutic agents are known to selectively activate or inhibit each of the dopamine receptor subtypes. A current goal of medicinal chemists is to develop drugs with even greater selectivity or specific mixed properties for the treatment of brain disorders that are associated with aberrations in various dopaminergic signaling pathways.
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