Target's General Information
Target ID T63967
Target Name Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2)
Synonyms CHRN; nAChR
Target Type Successful
Gene Name CHRNA4-CHRNB2
Biochemical Class Neurotransmitter receptor
UniProt ID ACHA4_HUMAN||ACHB2_HUMAN
Target's Expression Profile in Disease Related Tissue between Patients and Normal People
Disease Schizophrenia
Example drug Ispronicline Discontinued in Phase 2 [1], [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: 0.02
Z-score: 0.15
P-value: 7.65E-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 Ispronicline Discontinued in Phase 2 [1], [2], [3]
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
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 AZD-1446 Phase 2 [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: -0.15
Z-score: -0.61
P-value: 3.51E-10
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 Irritable bowel syndrome
Example drug TC-6499-12 Phase 2 [2], [3], [5]
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
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 SIB-1508Y Terminated [2], [3], [6], [7]
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
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 Eosinophilic gastritis
Tissue Gastric antrum tissue
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: 0.19
Z-score: 1.11
P-value: 3.06E-01
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 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 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 ClinicalTrials.gov (NCT01012375) Study to Investigate the Efficacy and Tolerability of AZD1446 in Adult ADHD Patients.. U.S. National Institutes of Health.
REF 5 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 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.
REF 7 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.

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