Title:A Review of Neuroreceptors for Clinical and Experimental Neuropharmacology
in Central Nervous System Disorders
Volume: 18
Issue: 3
Author(s): Susan C. McKarns*
Affiliation:
- University of Missouri School of Medicine, Columbia, MO, USA
- Laboratory of TGF-β Biology, Epigenetics, and
Cytokine Regulation, Department of Surgery, University of Missouri School of Medicine, Columbia, MO, USA
- Department of Microbiology and Immunology, University of Missouri School of Medicine, Columbia, MO, USA
Keywords:
Neuroreceptor, central nervous system, drug discovery, environmental stimuli, ion channels, G protein-coupled receptors, enzyme-linked receptors, nuclear receptors, endogenous ligands, signaling cascades.
Abstract: The neurobiology drug discovery landscape has transformed over the past decade or so by
the discovery of allosteric modulators of receptor superfamilies. A wide range of physiological reactions
can occur in response to a limited number of neurotransmitters. This review provides an update
on physiological features of the receptors and the signaling pathways that are generated in response to
neuroreceptor activation that allow the explanation of this vast array of neurotransmitter responses.
Primarily based upon structure, receptors in the nervous system can be classified into four groups: Gprotein
coupled receptors, ligand-gated receptors, enzyme-linked receptors, and nuclear receptors.
With a particular emphasis on the central nervous system, i.e., brain, spinal cord, and optic nerves, we
identify the neuroreceptors, their endogenous agonists, antagonists, sites of expression within the
nervous system, current neuropharmacological clinical use, and potential for new drug discovery. New
molecular approaches and advances in our knowledge of neuronal communication in processes involved
in development, functioning and disorders of the nervous system combined with opportunities
to re-purpose existing drugs for new indications continue to highlight the exciting opportunities to improve
human health.