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Namespace Prefixes

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Statements

Subject Item
n2:DB05708
rdf:type
n3:Drug
n3:description
GTS-21 (also known as DMBX-A), is a novel, small-molecule, orally active and selective alpha-7 nicotinic acetylcholine (nACh) receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials. Athenagen licensed the exclusive rights to the compound and a related library of analogs as part of the acquisition of Osprey Pharmaceutical Company in April 2006. GTS-21 has been studied in multiple Phase I studies in healthy volunteers and one Phase I/II study in schizophrenic patients. In all studies, the compound was well tolerated. In a Phase I multi-dose, double-blind, placebo controlled study in healthy adults, GTS-21 also demonstrated cognitive enhancement across all doses, with a statistically significant improvement in attention related and memory related tasks (Kitagawa, et al. Neuropsychopharmacology (2003), 28, 542-551).
n3:generalReferences
# Martin LF, Kem WR, Freedman R: Alpha-7 nicotinic receptor agonists: potential new candidates for the treatment of schizophrenia. Psychopharmacology (Berl). 2004 Jun;174(1):54-64. Epub 2004 Feb 19. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15205879 # Kitagawa H, Takenouchi T, Azuma R, Wesnes KA, Kramer WG, Clody DE, Burnett AL: Safety, pharmacokinetics, and effects on cognitive function of multiple doses of GTS-21 in healthy, male volunteers. Neuropsychopharmacology. 2003 Mar;28(3):542-51. Epub 2002 Jul 11. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12629535 # Kem WR: The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21). Behav Brain Res. 2000 Aug;113(1-2):169-81. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10942043 # van Haaren F, Anderson KG, Haworth SC, Kem WR: GTS-21, a mixed nicotinic receptor agonist/antagonist, does not affect the nicotine cue. Pharmacol Biochem Behav. 1999 Oct;64(2):439-44. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10515327 # Azuma R, Komuro M, Korsch BH, Andre JC, Onnagawa O, Black SR, Mathews JM: Metabolism and disposition of GTS-21, a novel drug for Alzheimer's disease. Xenobiotica. 1999 Jul;29(7):747-62. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10456692
n3:group
investigational
n3:indication
Investigated for use/treatment in alzheimer's disease and schizophrenia and schizoaffective disorders.
owl:sameAs
n9:DB05708
dcterms:title
GTS-21
adms:identifier
n7:DB05708 n10:6438361 n11:4942844 n12:43031369
n3:mechanismOfAction
Auditory sensory gating, a biological measurement of the ability to suppress the evoked response to the second of two auditory stimuli, is diminished in people with schizophrenia. Deficits in sensory gating are associated with attentional impairment, and may contribute to cognitive symptoms and perceptual disturbances. This inhibitory process, which involves the alpha(7) nicotinic receptor mediated release of gamma-aminobutyric acid (GABA) by hippocampal interneurons, represents a potential new target for therapeutic intervention in schizophrenia. GTS-21 is an orally active alpha-7 nicotinic acetylcholine (nACh) receptor agonist.
n3:synonym
DMXB-Anabaseine DMXB-A
n3:IUPAC-Name
n4:271B4612-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B4618-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B4617-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B4614-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B4615-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B4616-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B4611-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n4:271B461E-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B461F-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B4619-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B461A-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B461C-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B461B-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B461D-363D-11E5-9242-09173F13E4C5
n3:absorption
Rapidly and extensively absorbed after oral administration. In rat, GTS-21 showed linear pharmacokinetics over doses ranging from 1 to 10 mg/kg with an absolute bioavailability of 23%. In dog, the absolute bioavailability was 27% at an oral dose of 3 mg/kg.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
156223-05-1
n3:category
n3:Bioavailability
n4:271B4623-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B4625-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B4626-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B4622-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4621-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B4624-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B4613-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B4620-363D-11E5-9242-09173F13E4C5