DRD2 Antibodies

Background

The DRD2 gene encodes dopamine receptor D2, a G protein-coupled receptor mainly distributed in the dopaminergic pathway of the central nervous system. This receptor regulates the release of neurotransmitters by inhibiting the activity of adenylate cyclase and plays a core role in motor coordination, cognitive regulation and reward mechanisms. Most antipsychotic drugs exert their effects by blocking DRD2 receptors, and their genetic polymorphisms have been confirmed to be associated with schizophrenia, Parkinson's disease and susceptibility to drug addiction. As the first cloned dopamine receptor, it was simultaneously identified by multiple laboratories in 1988. The analysis of its tertiary structure provided a key template for the study of the GPCR family. The research on the association between genetic variations of this gene and individual differences in drug responses remains an important model in the fields of neuropsychopharmacology and precision medicine to this day.

Structure Function Application Advantage Our Products

Structure of DRD2

DRD2 is a G protein-coupled receptor with a molecular weight of approximately 44.1 kDa. There are subtle differences in its molecular weight among different splicing variants, mainly due to the length variation of the receptor's C-terminal domain.

Species	Human	Mouse	Rat	Rhesus monkey	Pig
Molecular Weight (kDa)	44.1	43.8	44.0	44.2	43.9
Primary Structural Differences	There are two splice variants, long/short	The C-terminal domain is relatively short	Very high homology with humans	Highly conserved across the membrane area	The ligand binding domains are similar

DRD2 is composed of 414 amino acids and forms a typical seventh-transmembrane topology. Its tertiary structure contains a ligand-binding pocket composed of transmembrane helices, and this domain is highly conserved among species. The third intracellular loop of the receptor is responsible for coupling with Gi/o proteins and mediating downstream signal transduction. Aspartic acid residues bind to sodium ions to stabilize the inactivated state of receptors, while serine residues are involved in agonist-induced receptor phosphorylation and internalization processes.

Fig. 1 Overall structure of the DRD2/haloperidol complex.¹

Key structural properties of DRD2:

Typical seven-fold transmembrane helix topology
Conserved ligand-binding pockets are located in the transmembrane domain
The third cell inner responsible for G protein coupling and signal transduction

Functions of DRD2

The main function of DRD2 receptors is to regulate the transmission of dopaminergic neural signals. In addition, it is also involved in a variety of neurophysiological processes, including motor control, cognitive regulation and reward mechanisms.

Function	Description
Signal transduction	Inhibit the activity of adenylate cyclase through Gi/o protein to reduce the intracellular cAMP level.
Regulation of neurotransmitter release	Inhibit voltage-gated calcium channels and activate inward-rectifying potassium channels to reduce the release of presynaptic membrane neurotransmitters.
Motor coordination	In the substantia nigra striatum - pathways regulate the movement function, its function disorders associated with motor symptoms of Parkinson's disease.
Reward mechanism	The activation of D2 receptors in the nucleus accumbosus can inhibit the reward effect and is closely related to drug addiction behavior.
Regulation of cognitive function	D2 receptors in the prefrontal cortex are involved in the neural regulation of working memory and executive function.

The signal response of DRD2 exhibits typical G protein-coupled receptor characteristics, with an activation threshold lower than that of D1 family receptors. This feature enables it to precisely regulate the steady-state balance of dopaminergic neural circuits.

Applications of DRD2 and DRD2 Antibody in Literature

1. Tan, Yiqing, et al. "Tumor suppressor DRD2 facilitates M1 macrophages and restricts NF-κB signaling to trigger pyroptosis in breast cancer." Theranostics 11.11 (2021): 5214. https://doi.org/10.7150/thno.58322

This study reveals that DRD2 is downregulated in breast cancer due to promoter methylation, and its high expression predicts a better prognosis. DRD2 inhibits tumor progression and enhances chemotherapy sensitivity by suppressing the NF-κB pathway, inducing apoptosis/necroptosis/pyroptosis, and promoting the polarization of M1-type macrophages.

2. Wang, Yan, et al. "Chronic stress accelerates glioblastoma progression via DRD2/ERK/β-catenin axis and Dopamine/ERK/TH positive feedback loop." Journal of Experimental & Clinical Cancer Research 42.1 (2023): 161. https://doi.org/10.1186/s13046-023-02728-8

Studies have shown that chronic stress drives the deterioration of glioblastoma by upregulating dopamine and its receptor DRD2. DRD2 promotes tumor progression by activating the ERK/β-catenin signaling axis and forming a positive feedback loop of dopamine autocrine. DRD2 and β-catenin can serve as potential biomarkers and therapeutic targets for poor prognosis.

3. Mathis, Thibaud, et al. "DRD2 activation inhibits choroidal neovascularization in patients with Parkinson's disease and age-related macular degeneration." The Journal of clinical investigation 134.17 (2024). https://doi.org/10.1172/JCI174199

This study found that levodopa, a drug for treating Parkinson's disease, and its activated DRD2 signaling pathway can significantly inhibit the formation of choroidal neovascularization in the eyes, delay the onset of nAMD and reduce the need for anti-VEGF treatment, suggesting that DRD2 agonists may serve as a potential adjuvant therapy for nAMD.

4. Mangili, Federica, et al. "DRD2 agonist cabergoline abolished the escape mechanism induced by mTOR inhibitor everolimus in tumoral pituitary cells." Frontiers in Endocrinology 13 (2022): 867822. https://doi.org/10.3389/fendo.2022.867822

This study reveals that in pleomorphic adenomas, the DRD2 agonist camergoline can inhibit the compensatory phosphorylation of AKT induced by the mTOR inhibitor everolimus through a β-arrestin 2-dependent mechanism, thereby synergistically reducing tumor cell proliferation. This combined strategy offers potential therapy for drug-resistant tumors expressing β-arrestin 2.

5. Kim, Esther, et al. "Interaction effects of DRD2 genetic polymorphism and interpersonal stress on problematic gaming in college students." Genes 13.3 (2022): 449. https://doi.org/10.3390/genes13030449

This study shows that individuals carrying the DRD2 C957T allele and the Taq1 A1 allele are more likely to adopt an avoidant coping style when facing interpersonal stress, which leads to an intensification of game addiction behavior, revealing the mechanism by which genes and stress influence addiction through behavioral mediation.

Creative Biolabs: DRD2 Antibodies for Research

Creative Biolabs specializes in the production of high-quality DRD2 antibodies for research and industrial applications. Our portfolio includes monoclonal antibodies tailored for ELISA, Flow Cytometry, Western blot, immunohistochemistry, and other diagnostic methodologies.

Custom DRD2 Antibody Development: Tailor-made solutions to meet specific research requirements.
Bulk Production: Large-scale antibody manufacturing for industry partners.
Technical Support: Expert consultation for protocol optimization and troubleshooting.
Aliquoting Services: Conveniently sized aliquots for long-term storage and consistent experimental outcomes.

For more details on our DRD2 antibodies, custom preparations, or technical support, contact us at email.

Reference

Fan, Luyu, et al. "Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands." Nature communications 11.1 (2020): 1074. https://doi.org/10.1038/s41467-020-14884-y