A neurotransmitter receptor (also known as a neuroreceptor) is a membrane receptor protein that is activated by a neurotransmitter. Chemicals on the outside of the cell, such as a neurotransmitter, can bump into its corresponding receptor in the membrane, bind and trigger other events to occur inside the cell. A neurotransmitter receptor is a class of receptors that specifically binds with neurotransmitters as opposed to other molecules. Neurotransmitter (NT) receptors are located on the surface of neuronal and glial cells.

There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic means that ions can pass through the receptor, whereas metabotropic means that a second messenger inside the cell relays the message (i.e. metabotropic receptors do not have channels). Metabotropic receptors are in fact G protein-coupled receptors. Ionotropic receptors are also called Ligand-gated ion channels and they can be excited by neurotransmitters like glutamate and aspartate. There are several major classes of neurotransmitters: Adrenergic, Dopaminergic, GABAergic, Glutaminergic, Histaminergic, Cholinergic, Opioid, Serotonergic, and Glycinergic.

In the brain, most drug targets consist of signaling proteins that go awry in central nervous system diseases, for example with autism in childhood, schizophrenia in adolescence, or Alzheimer's disease in old age. The aim of drug treatment is to correct the inappropriate behavior of these proteins and restore normal brain function. Understanding the effects of neurotransmitters is extremely important in therapeutics. All psychiatric drugs act by affecting neurotransmitters. Understanding their mechanism of action and adverse effects is key to developing new drugs for neurological diseases.

The TargetMol neurotransmitter receptor compound library contains 1660 CNS receptor ligands, which is ideal for screening or identifying recombinant orphan G protein-coupled receptors, target validation, secondary screening, validating new assays, and for routine pharmacological applications.