Target's General Information
Target ID T67162
Target Name Dopamine D2 receptor (D2R)
Synonyms Dopamine receptor 2; D(2) dopamine receptor
Target Type Successful
Gene Name DRD2
Biochemical Class GPCR rhodopsin
UniProt ID DRD2_HUMAN
Target's Expression Profile in Disease Related Tissue between Patients and Normal People
Disease Chronic obstructive pulmonary disease
Example drug Sibenadet Discontinued in Phase 3 [1], [2], [3]
Tissue Lung tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.11
Z-score: 0.57
P-value: 3.65E-02
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Chronic obstructive pulmonary disease
Example drug Sibenadet Discontinued in Phase 3 [1], [2], [3]
Tissue Small airway epithelium
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 6.16E-03
Z-score: 0.03
P-value: 9.83E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Alzheimer's disease
Example drug Dihydroergotoxine Approved [2], [3], [4]
Tissue Entorhinal cortex
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.08
Z-score: -0.49
P-value: 2.50E-02
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Bipolar disorder
Example drug Perphenazine Approved [2], [3], [5], [6]
Tissue Pre-frontal cortex
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.07
Z-score: -0.52
P-value: 9.12E-02
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Parkinson's disease
Example drug Lisuride Approved [2], [3], [7], [8]
Tissue Substantia nigra tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.51
Z-score: -1.35
P-value: 2.20E-03
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Schizophrenia
Example drug Perphenazine Approved [2], [3], [5], [6]
Tissue Pre-frontal cortex
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.01
Z-score: -0.05
P-value: 9.39E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Schizophrenia
Example drug Perphenazine Approved [2], [3], [5], [6]
Tissue Superior temporal cortex
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.02
Z-score: -0.28
P-value: 9.91E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Lung cancer
Example drug RBP-7000 Phase 3 [9], [2], [3]
Tissue Lung tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.05
Z-score: -0.2
P-value: 2.88E-02
Level of differential expression between the patients in the disease section of the tissue section of the tissue adjacent to the disease section Fold-change: -0.13
Z-score: -0.37
P-value: 1.55E-02
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles of the patients in the normal section of the tissue adjacent to the disease section
Target gene expression profiles in the tissue of healthy individual
Disease Depression
Example drug CLR-3001 Phase 2 [10], [2], [3]
Tissue Pre-frontal cortex
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 4.29E-03
Z-score: 0.03
P-value: 8.40E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Breast cancer
Example drug Nomifensine Withdrawn from market [2], [3], [11], [12]
Tissue Breast tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.1
Z-score: -0.47
P-value: 8.65E-08
Level of differential expression between the patients in the disease section of the tissue section of the tissue adjacent to the disease section Fold-change: -0.14
Z-score: -0.6
P-value: 1.44E-03
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles of the patients in the normal section of the tissue adjacent to the disease section
Target gene expression profiles in the tissue of healthy individual
Target's Expression Profile across Various Tissues of Healthy Individual
References
REF 1 Anti-obesity drugs and neural circuits of feeding. Trends Pharmacol Sci. 2008 Apr;29(4):208-17.
REF 2 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 3 NCBI GEO: archive for functional genomics data sets--update. Nucleic Acids Res. 2013 Jan;41(Database issue):D991-5.
REF 4 Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97.
REF 5 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 209).
REF 6 Methamphetamine Addiction and Abuse - Perphenazine.
REF 7 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 43).
REF 8 Lisuride, a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction reports supports the concept of a crucial role for 5-HT2B receptor agonism in cardiac valvular fibrosis. Clin Neuropharmacol. 2006 Mar-Apr;29(2):80-6.
REF 9 ClinicalTrials.gov (NCT02109562) Randomized, Double-blind, Placebo Controlled, Multi-center and Tolerability of RBP-7000 in Schizophrenia Patients. U.S. National Institutes of Health.
REF 10 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032468)
REF 11 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4792).
REF 12 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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