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 [522853], [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: -0.15
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 [523082], [1572592]
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 Schizophrenia
Example drug Ispronicline Discontinued in Phase 2 [546915], [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: 0.02
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 [546915], [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: -0.01
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 Parkinson's disease
Example drug SIB-1508Y Terminated [525768], [529637], [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: -0.12
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 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
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 Other Tissues of Healthy Individuals
Reference
Ref
Ref 546915Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011083)
Ref 525768Recombinant 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 529637Pharmacological 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 522853ClinicalTrials.gov (NCT01012375) Study to Investigate the Efficacy and Tolerability of AZD1446 in Adult ADHD Patients.. U.S. National Institutes of Health.
Ref 523082ClinicalTrials.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 1572592NCBI GEO: archive for functional genomics data sets--update.

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