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DRD4
DRD4 Full Name
dopamine receptor D4
DRD4 Introduction
Dopamine receptor D4 is the target of drugs for treating schizophrenia and Parkinson's disease. The D4 receptor is considered D2 like, where activated receptors inhibit adenylate cyclase, thereby reducing the intracellular concentration of the second messenger cyclic AMP. Dopamine receptor D4 is a dopamine D2 like G protein coupled receptor encoded by the DRD4 gene on chromosome 11p15.5. The structure of DRD4 has been reported to be combined with the antipsychotic drug nifedipine. Like other subtypes of dopamine receptors, the D4 receptor is activated by the neurotransmitter dopamine. It is associated with many neurological and psychiatric disorders, including schizophrenia and bipolar disorder, ADHD, addictive behavior, Parkinson's disease, and eating disorders such as anorexia nervosa. The association between DRD4 and borderline personality disorder is weak.
Figure. Dopamine receptor mediated effects on sodium transporters within the kidney. (Source: Ramkumar N, et al, 2024)
Molecular Structure, Pharmacology, and Signaling of DRD4
The DRD4 receptor consists of a single polypeptide chain that spans the membrane seven times, with the amino terminus extracellular and the carboxyl terminus intracellular. Like other G_i/o-linked GPCRs, DRD4 features a large third intracellular loop and a short carboxyl terminal tail. A consensus site for N-linked glycosylation is present in the amino terminus, and the carboxyl terminal amino acid is a cysteine residue believed to be palmitoylated. The third intracellular loop contains multiple potential sites for phosphorylation by protein kinase A and C, as well as GPCR-selective protein kinases (GRKs). 1 Palmitoylation involves covalent attachment of a 16-carbon fatty acid, palmitate, to cysteine residues in the membrane-proximal intracellular region.
Expression Patterns and Neuroanatomical Distribution
DRD4 is expressed at particularly high levels in the prefrontal cortex and nucleus accumbens, regions central to emotional processing and depression. 2 It shows its highest levels of expression in the frontal and cingulate areas, including the anterior cingulate cortex, where it is present in layers II–VI. 14 In the human brain, the highest levels of DRD4 are seen in the lateral septal nucleus, with about 30% lower levels in the entorhinal cortex and dorsomedial thalamus; DRD4 is also present in the hippocampus, hypothalamus, and prefrontal cortex. 15 DRD4 is mainly distributed in the prefrontal cortex, entorhinal cortex, and hippocampus, with less significant distribution in the striatum and thalamus in both rodents and humans.
Alternate Names for DRD4
DRD4; dopamine receptor D4; D(4) dopamine receptor; dopamine D4 receptor; D(2C) dopamine receptor; seven transmembrane helix receptor; D4DR;
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