Target General Information
Target ID T54128
Target Name Glutamate receptor AMPA subtype
Synonyms AMPA receptor; AMPA selective glutamate receptor; GluR; Glutamate receptor; Glutamate receptor ionotropic, AMPA
Target Type Successful
Gene Name GABRA1
Biochemical Class Chloride channel
UniProt ID GBRA1_HUMAN||GBRA2_HUMAN||GBRB2_HUMAN||GBRD_HUMAN||GBRG2_HUMAN
Target Gene Expression Profiles in the Disease-Relevant Drug Targeted Tissue of the Patients and Healthy Individuals
Disease Alzheimer's disease
Example drug Dihydroergotoxine Approved [534844], [1572592]
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: -0.69
Z-score: -0.58
P-value: 1.79E-04
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 CX-516 Phase 2/3 [467505], [536120], [1572592]
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: -0.46
Z-score: -0.15
P-value: 5.94E-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 Schizophrenia
Example drug CX-516 Phase 2/3 [467505], [536120], [1572592]
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: -0.52
Z-score: -0.47
P-value: 8.64E-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 Epilepsy
Example drug Talampanel Phase 2 [536498], [543034], [1572592]
Tissue Peritumoral cortex tissue
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of the persons with other diseases not directly affecting the tissue
Disease Parkinson's disease
Example drug Talampanel Phase 2 [536498], [543034], [1572592]
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: -0.39
Z-score: -0.21
P-value: 9.57E-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 Coronary artery disease
Example drug Fanapanel Phase 1 [527708], [542619], [1572592]
Tissue Peripheral blood
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.32
Z-score: -1.90
P-value: 7.03E-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
Target Gene Expression Profiles in Other Tissues of Healthy Individuals
Reference
Ref 467505(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: 4165).
Ref 542619(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: 7636).
Ref 543034(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: 8279).
Ref 534844Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97.
Ref 536120Autism spectrum disorders: emerging pharmacotherapy. Expert Opin Emerg Drugs. 2005 Aug;10(3):521-36.
Ref 527708The AMPA antagonist ZK 200775 in patients with acute ischaemic stroke: a double-blind, multicentre, placebo-controlled safety and tolerability study. Cerebrovasc Dis. 2005;20(5):304-9. Epub 2005 Aug30.
Ref 536498Emerging drugs for epilepsy. Expert Opin Emerg Drugs. 2007 Sep;12(3):407-22.
Ref 1572592NCBI GEO: archive for functional genomics data sets--update.

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