Target expression details
| Target General Information | |||||
|---|---|---|---|---|---|
| Target ID | T63967 | ||||
| Target Name | Nicotinic ACh receptor alpha-4/beta-2 | ||||
| Synonyms | Nicotinic acetylcholine receptor alpha4/beta2 | ||||
| Target Type | Successful | ||||
| Gene Name | CHRNA4 | ||||
| Biochemical Class | Channels/Pores (TC=1) | ||||
| UniProt ID | ACHA4_HUMAN||ACHB2_HUMAN | ||||
| Target Gene Expression Profiles in the Disease-Relevant Drug Targeted Tissue of the Patients and Healthy Individuals | |||||
| Disease | Alzheimer's disease | ||||
| Example drug | AZD-1446 | Phase 2 | [1], [2] | ||
| 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: -0.15 Z-score: -0.61 P-value: 3.51E-10 |
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Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
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| Disease | Irritable bowel syndrome | ||||
| Example drug | TC-6499-12 | Phase 2 | [3], [2] | ||
| Tissue | Rectal colon tissue | ||||
| Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual | Fold-change: -3.94E-03 Z-score: -0.02 P-value: 1.09E-01 |
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Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
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| Disease | Schizophrenia | ||||
| Example drug | Ispronicline | Discontinued in Phase 2 | [4], [2] | ||
| 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: 0.02 Z-score: 0.15 P-value: 7.65E-01 |
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Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
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| Disease | Schizophrenia | ||||
| Example drug | Ispronicline | Discontinued in Phase 2 | [4], [2] | ||
| 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: -0.01 Z-score: -0.11 P-value: 9.89E-01 |
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Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
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| Disease | Parkinson's disease | ||||
| Example drug | SIB-1508Y | Terminated | [5], [6], [2] | ||
| 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: -0.12 Z-score: -0.71 P-value: 1.04E-01 |
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Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
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| Disease | Eosinophilic gastritis | ||||
| Tissue | Gastric antrum tissue | ||||
| Level of differential expression between the patients in the disease section of the tissue and the patients in the normal section of the tissue adjacent to the disease section | Fold-change: 0.19 Z-score: 1.11 P-value: 3.06E-01 |
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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
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| Target Gene Expression Profiles in Other Tissues of Healthy Individuals | |||||
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| Reference | |||||
| REF 1 | ClinicalTrials.gov (NCT01012375) Study to Investigate the Efficacy and Tolerability of AZD1446 in Adult ADHD Patients.. U.S. National Institutes of Health. | ||||
| REF 2 | NCBI GEO: archive for functional genomics data sets--update. | ||||
| REF 3 | ClinicalTrials.gov (NCT01149200) Proof-of-Principle Study of TC-6499 in the Treatment of Constipation Predominant Irritable Bowel Syndrome (IBS). U.S. National Institutes of Health. | ||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011083) | ||||
| REF 5 | Recombinant human receptors and functional assays in the discovery of altinicline (SIB-1508Y), a novel acetylcholine-gated ion channel (nAChR) agonist. Pharm Acta Helv. 2000 Mar;74(2-3):125-30. | ||||
| REF 6 | Pharmacological characterization of (S)-(2)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine HCl (SIB-1508Y, Altinicline), a novel nicotinic acetylcholine receptor agonist. Brain Res. 2008 Oct 9;1234:16-24. | ||||
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