gsk239512 profile

GSK239512: an H3 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	9976892
CHEMBL ID	3092650
SCHEMBL ID	167578
MeSH ID	M0588759

Synonym
bdbm50444496
720691-69-0
gsk-239512
SCHEMBL167578
gsk-239512a
gsk239512
CHEMBL3092650 ,
YFRBKEVUUCQYOW-UHFFFAOYSA-N ,
1-{6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1h-3-benzazepin-7-yl)oxy]-3-pyridinyl}-2-pyrrolidinone
AKOS025291102
1-(6-((3-cyclobutyl-2,3,4,5-tetrahydro-1h-benzo[d]azepin-7-yl)oxy)pyridin-3-yl)pyrrolidin-2-one
mfcd27922168
2-pyrrolidinone, 1-(6-((3-cyclobutyl-2,3,4,5-tetrahydro-1h-3-benzazepin-7-yl)oxy)-3-pyridinyl)-
unii-4i7u5c459m
4I7U5C459M ,
DB15120
AS-42474
SB16754
1-[6-[(3-cyclobutyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)oxy]pyridin-3-yl]pyrrolidin-2-one
VDB69169
A866322
2-pyrrolidinone, 1-[6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1h-3-benzazepin-7-yl)oxy]-3-pyridinyl]-

Excerpt	Reference	Relevance
"GSK239512 is a potent and selective H₃ receptor antagonist developed for the treatment of cognitive dysfunction in neurodegenerative disorders."	( The safety, tolerability, pharmacokinetics and cognitive effects of GSK239512, a selective histamine H₃ receptor antagonist in patients with mild to moderate Alzheimer's disease: a preliminary investigation. Berges, A; Boardley, R; Lai, R; Lowy, MT; Maruff, P; Nathan, PJ; Nestor, PJ; Scott, N; Sivananthan, T; Upton, N, 2013)	1.35

Excerpt	Reference	Relevance
"GSK239512 treatment was associated with mild to moderate adverse events with headache, dizziness and events related to sleep disturbances being the most common and more pronounced in the early titration period when subjects were first being exposed to GSK239512 at the lower 10µg and 20µg doses."	( A randomized, double-blind, placebo-controlled, 16-week study of the H3 receptor antagonist, GSK239512 as a monotherapy in subjects with mild-to-moderate Alzheimer's disease. Beresford, I; Berges, AC; Boardley, RL; Grove, RA; Harrington, CM; Horrigan, JP; Lowy, MT; Mahler, A; Maruff, P; Nathan, PJ; Nicholls, AP, 2014)	1.34

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Histamine H2 receptor	Homo sapiens (human)	Ki	3.1623	0.0006	2.1973	10.0000	AID1059539
Histamine H1 receptor	Homo sapiens (human)	Ki	2.5119	0.0000	0.5110	10.0000	AID1059538
Histamine H4 receptor	Homo sapiens (human)	Ki	3.1623	0.0006	0.4787	10.0000	AID1059537
Histamine H3 receptor	Rattus norvegicus (Norway rat)	Ki	0.0003	0.0001	0.2963	8.5110	AID1059540; AID1059552
Histamine H3 receptor	Homo sapiens (human)	Ki	0.0026	0.0001	0.3399	8.5110	AID1059541; AID1059543; AID1059553; AID1272284
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
gastric acid secretion	Histamine H2 receptor	Homo sapiens (human)
immune response	Histamine H2 receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Histamine H2 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H2 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H2 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H2 receptor	Homo sapiens (human)
inflammatory response	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
memory	Histamine H1 receptor	Homo sapiens (human)
visual learning	Histamine H1 receptor	Homo sapiens (human)
regulation of vascular permeability	Histamine H1 receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Histamine H1 receptor	Homo sapiens (human)
regulation of synaptic plasticity	Histamine H1 receptor	Homo sapiens (human)
cellular response to histamine	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H1 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H1 receptor	Homo sapiens (human)
inflammatory response	Histamine H4 receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Histamine H4 receptor	Homo sapiens (human)
biological_process	Histamine H4 receptor	Homo sapiens (human)
regulation of MAPK cascade	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H4 receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H4 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H4 receptor	Homo sapiens (human)
neurotransmitter secretion	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H3 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H3 receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
histamine receptor activity	Histamine H2 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H2 receptor	Homo sapiens (human)
neurotransmitter receptor activity	Histamine H2 receptor	Homo sapiens (human)
histamine receptor activity	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H1 receptor	Homo sapiens (human)
neurotransmitter receptor activity	Histamine H1 receptor	Homo sapiens (human)
histamine receptor activity	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Histamine H4 receptor	Homo sapiens (human)
histamine receptor activity	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Histamine H2 receptor	Homo sapiens (human)
synapse	Histamine H2 receptor	Homo sapiens (human)
plasma membrane	Histamine H2 receptor	Homo sapiens (human)
dendrite	Histamine H2 receptor	Homo sapiens (human)
cytosol	Histamine H1 receptor	Homo sapiens (human)
plasma membrane	Histamine H1 receptor	Homo sapiens (human)
synapse	Histamine H1 receptor	Homo sapiens (human)
dendrite	Histamine H1 receptor	Homo sapiens (human)
plasma membrane	Histamine H1 receptor	Homo sapiens (human)
plasma membrane	Histamine H4 receptor	Homo sapiens (human)
plasma membrane	Histamine H4 receptor	Homo sapiens (human)
dendrite	Histamine H4 receptor	Homo sapiens (human)
synapse	Histamine H4 receptor	Homo sapiens (human)
plasma membrane	Histamine H3 receptor	Homo sapiens (human)
presynapse	Histamine H3 receptor	Homo sapiens (human)
plasma membrane	Histamine H3 receptor	Homo sapiens (human)
synapse	Histamine H3 receptor	Homo sapiens (human)
dendrite	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay ID	Title	Year	Journal	Article
AID1059545	Ratio of drug level in brain to blood in rat at 3 mg/kg, po	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059551	Ex vivo binding affinity to histamine H3 receptor in po dosed rat cerebral cortex using [3H]-R-alpha-ethylhistamine after 2 hrs by HPLC analysis	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059524	Tmax in po dosed Sprague-Dawley rat	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059528	Terminal half life in iv dosed Sprague-Dawley rat	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059504	Cognitive enhancing effect against scopolamine-induced memory deficit in po dosed Wistar rat assessed as passive avoidance response after 24 hrs	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059534	Time dependent inhibition of CYP450 (unknown origin)	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059553	Antagonist activity at human histamine H3 receptor expressed in CHOK1 cells assessed as inhibition of GTPgammaS binding	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059522	Total blood clearance in iv dosed Beagle dog	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059540	Displacement of [3H]-R-alpha-ethylhistamine from rat histamine H3 receptor expressed in HEK293 cells after 45 mins by liquid scintillation spectrometry	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059547	Drug level in rat blood at 3 mg/kg, po	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059552	Displacement of [3H]-R-alpha-ethylhistamine from histamine H3 receptor in rat cerebral cortical tissue membranes after 45 mins by liquid scintillation spectrometry	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059512	Volume of distribution at steady-state in iv dosed cynomolgus monkey	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1272284	Binding affinity to recombinant human H3 receptor	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.
AID1059508	Ex vivo receptor occupancy of histamine H3 receptor in rat brain	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059503	Cognitive enhancing effect against scopolamine-induced memory deficit in Wistar rat assessed as passive avoidance response at 3 mg/kg, po after 24 hrs	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059530	Volume of distribution at steady-state in iv dosed Sprague-Dawley rat	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059550	Ex vivo binding affinity to histamine H3 receptor in rat cerebral cortex using [3H]-R-alpha-ethylhistamine at 3 mg/kg, po after 3 hrs by HPLC analysis	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059532	Intrinsic clearance in human liver microsomes	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059506	Terminal half life in po dosed cynomolgus monkey	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059523	Oral bioavailability in Sprague-Dawley rat	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059529	Cmax in iv dosed Sprague-Dawley rat	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059511	Cmax in iv dosed cynomolgus monkey	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059536	Aqueous solubility of the compound	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059520	Terminal half life in iv dosed Beagle dog	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059537	Binding affinity to human histamine H4 receptor	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059509	Cmax in po dosed cynomolgus monkey	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059525	Terminal half life in po dosed Sprague-Dawley rat	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059526	Cmax in po dosed Sprague-Dawley rat	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059514	Oral bioavailability in Beagle dog	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059517	Ratio of drug level in brain to blood in human	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059531	Total blood clearance in iv dosed Sprague-Dawley rat	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059538	Binding affinity to human histamine H1 receptor	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059516	Tmax in po dosed Beagle dog	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059513	Total blood clearance in iv dosed cynomolgus monkey	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059535	Inhibition of human ERG at 10 uM by patch clamp experiment	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059533	Binding affinity to human serum albumin by HPLC analysis	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059544	Reversal of RAMH-induced dipsogenia in po dosed Lister Hooded rat treated 2 hrs before RAMH challenge measured after 1 hr	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059542	Intrinsic clearance in rat liver microsomes	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059543	Displacement of [3H]-R-alpha-ethylhistamine from histamine H3 receptor in human cerebral cortical tissue membranes after 45 mins by liquid scintillation spectrometry	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059510	Terminal half life in iv dosed cynomolgus monkey	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059507	Tmax in po dosed cynomolgus monkey	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059519	Cmax in iv dosed Beagle dog	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059527	Ratio of drug level in brain to blood in iv dosed Sprague-Dawley rat	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059539	Binding affinity to human histamine H2 receptor	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059541	Displacement of [3H]-R-alpha-ethylhistamine from human histamine H3 receptor expressed in HEK293 cells after 45 mins by liquid scintillation spectrometry	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059518	Cmax in po dosed Beagle dog	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059521	Volume of distribution at steady-state in iv dosed Beagle dog	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059505	Oral bioavailability in cynomolgus monkey	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059515	Terminal half life in po dosed Beagle dog	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
AID1059502	Cognitive enhancing effect in Lister Hooded rat assessed as increase of time spent exploring novel versus familiar objects in T2 at 0.3 to 1 mg/kg, po bid	2013	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24	Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	7 (100.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	5 (71.43%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	2 (28.57%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
niacinamide nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.	2.08	1	0	pyridine alkaloid; pyridinecarboxamide; vitamin B3	anti-inflammatory agent; antioxidant; cofactor; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; Escherichia coli metabolite; geroprotector; human urinary metabolite; metabolite; mouse metabolite; neuroprotective agent; Saccharomyces cerevisiae metabolite; Sir2 inhibitor
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	8.5	1	1	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
dibutyl phthalate 6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-3-pyridinecarboxamide: GSK-189254 is the HCl salt; an H3 receptor antagonist; putative cognitive enhancer; structure in first source	2.08	1	0
mk-0249 MK-0249: a histamine-3 receptor inverse agonist; structure in first source	2.13	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Acute Confusional Senile Dementia [description not available]	0	5.36	2	2
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	1	7.36	2	2
Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.	0	4.41	1	1
Dementia Praecox [description not available]	0	4.41	1	1
Schizophrenia A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.	1	11.41	1	1
Acute Relapsing Multiple Sclerosis [description not available]	0	3.53	1	1
Multiple Sclerosis, Relapsing-Remitting The most common clinical variant of MULTIPLE SCLEROSIS, characterized by recurrent acute exacerbations of neurologic dysfunction followed by partial or complete recovery. Common clinical manifestations include loss of visual (see OPTIC NEURITIS), motor, sensory, or bladder function. Acute episodes of demyelination may occur at any site in the central nervous system, and commonly involve the optic nerves, spinal cord, brain stem, and cerebellum. (Adams et al., Principles of Neurology, 6th ed, pp903-914)	1	5.53	1	1

gsk239512

Description

Cross-References

Synonyms (22)

Research Excerpts

Overview

Treatment

Protein Targets (5)

Inhibition Measurements

Biological Processes (19)

Molecular Functions (4)

Ceullar Components (5)

Bioassays (50)

Research

Studies (7)

Market Indicators

Research Demand Index: 21.24

Study Types

gsk239512

Description

Cross-References

Synonyms (22)

Research Excerpts

Overview

Treatment

Protein Targets (5)

Inhibition Measurements

Biological Processes (19)

Molecular Functions (4)

Ceullar Components (5)

Bioassays (50)

Research

Studies (7)

Market Indicators

Research Demand Index: 21.24

Study Types

Related Drugs (4)

Related Conditions (7)