Compounds > sb 649868
Page last updated: 2024-11-13

sb 649868

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Description

N-((1-((5-(4-fluorophenyl)-2-methyl-4-thiazolyl)carbonyl)-2-piperidinyl)methyl)-4-benzofurancarboxamide: antagonist of both orexin 1 and orexin 2 receptors; for treating insomnia; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25195495
CHEMBL ID1272307
SCHEMBL ID8045969
MeSH IDM0557222

Synonyms (29)

Synonym
gtpl4461
sb-649,868
sb649868
n-[[(2s)-1-[5-(4-fluorophenyl)-2-methyl-1,3-thiazole-4-carbonyl]piperidin-2-yl]methyl]-1-benzofuran-4-carboxamide
gsk649868
sb-649868 ,
CHEMBL1272307
380899-24-1
unii-1l1v1k2m4v
n-((1-((5-(4-fluorophenyl)-2-methyl-4-thiazolyl)carbonyl)-2-piperidinyl)methyl)-4-benzofurancarboxamide
1l1v1k2m4v ,
sb 649868
4-benzofurancarboxamide, n-(((2s)-1-((5-(4-fluorophenyl)-2-methyl-4-thiazolyl)carbonyl)-2-piperidinyl)methyl)-
bdbm50417257
SCHEMBL8045969
CS-7584
DTXSID90191491
AKOS027323765
HY-10806
c26h24fn3o3s
EX-A2570
sb649868; gsk649868
DB14822
Q7388914
n-[[(2s)-1-[[5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-4-benzofurancarboxamide
D82888
(s)-n-((1-(5-(4-fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide
BS-50120
AC-36150

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" SB-649868 was well tolerated at all doses in this study population, with mechanism-related adverse events (e."( Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist.
Alexander, R; Bettica, P; Gomeni, R; Nucci, G; Pyke, C; Ratti, E; Squassante, L; Zamuner, S, 2012)		0.38

Dosage Studied

ExcerptRelevanceReference
" Evening dosing resulted in significant dose-dependent improvement in latency to persistent sleep, total sleep time and wake after sleep onset as measured by polysomnography."( Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist.
Alexander, R; Bettica, P; Gomeni, R; Nucci, G; Pyke, C; Ratti, E; Squassante, L; Zamuner, S, 2012)		0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Orexin receptor type 1Homo sapiens (human)Ki0.00040.00030.28763.1623AID528164; AID618062; AID618068; AID765089
Orexin receptor type 2Homo sapiens (human)Ki0.00220.00020.37713.7810AID1166953; AID528165; AID618063; AID618069; AID765090
Orexin receptor type 1Rattus norvegicus (Norway rat)Ki0.00010.00010.00010.0001AID618066
Orexin receptor type 2Rattus norvegicus (Norway rat)Ki0.00010.00010.00550.0110AID618067
Sigma non-opioid intracellular receptor 1Rattus norvegicus (Norway rat)Ki0.00040.00030.26715.0700AID765090
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (10)

Processvia Protein(s)Taxonomy
neuropeptide signaling pathwayOrexin receptor type 1Homo sapiens (human)
chemical synaptic transmissionOrexin receptor type 1Homo sapiens (human)
feeding behaviorOrexin receptor type 1Homo sapiens (human)
regulation of cytosolic calcium ion concentrationOrexin receptor type 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeOrexin receptor type 1Homo sapiens (human)
cellular response to hormone stimulusOrexin receptor type 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayOrexin receptor type 2Homo sapiens (human)
neuropeptide signaling pathwayOrexin receptor type 2Homo sapiens (human)
chemical synaptic transmissionOrexin receptor type 2Homo sapiens (human)
feeding behaviorOrexin receptor type 2Homo sapiens (human)
regulation of circadian sleep/wake cycle, wakefulnessOrexin receptor type 2Homo sapiens (human)
circadian sleep/wake cycle processOrexin receptor type 2Homo sapiens (human)
locomotionOrexin receptor type 2Homo sapiens (human)
regulation of cytosolic calcium ion concentrationOrexin receptor type 2Homo sapiens (human)
cellular response to hormone stimulusOrexin receptor type 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityOrexin receptor type 1Homo sapiens (human)
protein bindingOrexin receptor type 1Homo sapiens (human)
orexin receptor activityOrexin receptor type 1Homo sapiens (human)
peptide hormone bindingOrexin receptor type 1Homo sapiens (human)
peptide bindingOrexin receptor type 1Homo sapiens (human)
protein bindingOrexin receptor type 2Homo sapiens (human)
neuropeptide receptor activityOrexin receptor type 2Homo sapiens (human)
orexin receptor activityOrexin receptor type 2Homo sapiens (human)
peptide hormone bindingOrexin receptor type 2Homo sapiens (human)
peptide bindingOrexin receptor type 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneOrexin receptor type 1Homo sapiens (human)
synapseOrexin receptor type 1Homo sapiens (human)
plasma membraneOrexin receptor type 1Homo sapiens (human)
plasma membraneOrexin receptor type 2Homo sapiens (human)
synapseOrexin receptor type 2Homo sapiens (human)
plasma membraneOrexin receptor type 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (84)

Assay IDTitleYearJournalArticle
AID618080Fraction unbound in CD rat plasma at 1 mg/kg, iv after 1 hrs2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1279996Drug metabolism in human plasma assessed as (S)-2-(2-((1-(5-(4-fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methylcarbamoyl)-6-hydroxyphenyl)acetic acid formation at 30 mg, po by LSC analysis2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID1280048Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 30 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID618064Intrinsic clearance in human liver microsomes2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618177Hypnotic activity in CD rat Circadian time model assessed as rapid eye movement sleep at 30 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 3.22 +/- 0.73 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID619505Hypnotic activity in CD rat Circadian time model assessed as total sleep time at 10 mg/kg, po administered during active phase (Rvb = 81 +/- 11 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID765089Binding affinity to orexin receptor 1 (unknown origin)2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective orexin receptor antagonists.
AID618175Hypnotic activity in CD rat Circadian time model assessed as rapid eye movement sleep at 3 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 3.22 +/- 0.73 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1280045Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 10 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID1280052Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 60 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID618170Hypnotic activity in CD rat Circadian time model assessed as non-rapid eye movement sleep at 10 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 78.1 +/- 11.3 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618069Displacement of [3H]almorexant from recombinant human OX2R expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618072Agonist activity at recombinant rat OX1R expressed in CHO cells at 1 uM2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618079Ratio of drug level in brain to blood in CD rat at 1 mg/kg, iv after 1 hrs2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1216100Tmax in human plasma treated with [14C]SB-649868 at 30 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID1216102Apparent oral clearance in human plasma treated with [14C]SB-649868 at 30 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID618172Hypnotic activity in CD rat Circadian time model assessed as rapid eye movement latency period at 3 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 146.3 +/- 54.2 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618071Agonist activity at recombinant human OX2R expressed in CHO cells at 1 uM2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1280056Half life in human plasma2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID618173Hypnotic activity in CD rat Circadian time model assessed as rapid eye movement latency period at 10 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 146.3 +/- 54.2 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1279958Drug metabolism in human plasma assessed as 2-(((S)-1-(5-(4-fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)-3,5-dihydroxy-3,4-dihydroisoquinolin-1(2H)-one formation at 30 mg, po by LSC analysis2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID1280044Effect on sleep parameter in insomnia patient assessed as sleep efficiency at 10 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID618176Hypnotic activity in CD rat Circadian time model assessed as rapid eye movement sleep at 10 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 3.22 +/- 0.73 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1279995Apparent half life of the compound in human2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID618171Hypnotic activity in CD rat Circadian time model assessed as non-rapid eye movement sleep at 30 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 78.1 +/- 11.3 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1216088Drug level in human plasma assessed as radioactivity treated with [14C]SB-649868 at 30 mg, po single dose after 24 hrs by HPLC-MSn analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID1280049Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 30 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID618062Antagonist activity at recombinant human OX1R expressed in CHO cells by FLIPR calcium based functional assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID619507Hypnotic activity in po dosed CD rat Circadian time model assessed as rapid eye movement sleep administered during active phase measured from starting time CT182011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618174Hypnotic activity in CD rat Circadian time model assessed as rapid eye movement latency period at 30 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 146.3 +/- 54.2 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1216097AUC (0 to infinity) in human plasma treated with [14C]SB-649868 at 30 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID1216140Drug level in human plasma assessed as radioactivity treated with [14C]SB-649868 at 30 mg, po single dose after 3 hrs by HPLC-MSn analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID618063Antagonist activity at recombinant human OX2R expressed in CHO cells by FLIPR calcium based functional assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618167Hypnotic activity in CD rat Circadian time model assessed as non-rapid eye movement latency period at 10 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 46.1 +/- 10.0 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1216089Drug level in human plasma assessed as radioactivity treated with [14C]SB-649868 at 30 mg, po single dose after 48 hrs by HPLC-MSn analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID1216092Terminal phase half life in human at 10 to 60 mg2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID618066Antagonist activity at recombinant rat OX1R expressed in CHO cells by FLIPR calcium based functional assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618076Volume of distribution at steady state in CD rat at 1 mg/kg, iv and 3 mg/kg, po2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618068Displacement of [3H]almorexant from recombinant human OX1R expressed in CHO cells2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1216094Elimination half life in dog2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID1216091Drug level in human feces treated with [14C]SB-649868 at 30 mg, po single dose after 3 hrs by HPLC-MSn analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID1216087Drug level in human plasma assessed as radioactivity treated with [14C]SB-649868 at 30 mg, po single dose after 12 hrs by HPLC-MSn analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID618070Agonist activity at recombinant human OX1R expressed in CHO cells at 1 uM2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618078Cmax in CD rat at 1 mg/kg, iv and 3 mg/kg, po2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1280047Effect on sleep parameter in insomnia patient assessed as total sleep time at 10 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID1216101Apparent half life in human plasma treated with [14C]SB-649868 at 30 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID528165Antagonist activity against human orexin 2 receptor expressed in CHO cells assessed as effect in calcium mobilization by FLIPR assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.
AID1216095Drug recovery in human plasma at 30, po single dose after 48 hrs by HPLC-MSn analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID618164Hypnotic activity in CD rat Circadian time model assessed as awake period at 10 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 218 +/- 11.32 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1280054Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 60 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID1280051Effect on sleep parameter in insomnia patient assessed as total sleep time at 30 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID1216093Elimination half life in rat2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID1280050Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 30 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID618163Hypnotic activity in CD rat Circadian time model assessed as awake period at 3 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 218 +/- 11.32 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618073Agonist activity at recombinant rat OX2R expressed in CHO cells at 1 uM2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID619508Hypnotic activity in po dosed CD rat Circadian time model assessed as non-rapid eye movement sleep administered during active phase measured from starting time CT182011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618166Hypnotic activity in CD rat Circadian time model assessed as non-rapid eye movement latency period at 3 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 46.1 +/- 10.0 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1166953Displacement of [125I]-Orexin A from human OX2R expressed in CHO cells after 30 mins by topcount analysis2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists.
AID1216098AUC (0 to t) in human plasma treated with [14C]SB-649868 at 30 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID1192081Half life in human2015Bioorganic & medicinal chemistry, Mar-15, Volume: 23, Issue:6
Discovery and in vitro and in vivo profiles of N-ethyl-N-[2-[3-(5-fluoro-2-pyridinyl)-1H-pyrazol-1-yl]ethyl]-2-(2H-1,2,3-triazol-2-yl)-benzamide as a novel class of dual orexin receptor antagonist.
AID618077Oral bioavailability in CD rat at 3 mg/kg2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618169Hypnotic activity in CD rat Circadian time model assessed as non-rapid eye movement sleep at 3 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 78.1 +/- 11.3 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618165Hypnotic activity in CD rat Circadian time model assessed as awake period at 30 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 218 +/- 11.32 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618180Neurotoxicity in CD rat assessed as impairment of motor coordination at 1 to 10 mg/kg, po by rotarod test in presence of 1 g/kg, ip ethanol2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1280053Effect on sleep parameter in insomnia patient assessed as latency to persistent sleep time at 60 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID618081Fraction unbound in CD rat brain at 1 mg/kg, iv after 1 hrs2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618067Antagonist activity at recombinant rat OX2R expressed in CHO cells by FLIPR calcium based functional assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618168Hypnotic activity in CD rat Circadian time model assessed as non-rapid eye movement latency period at 30 mg/kg, po administered during active phase measured from starting time CT18 (Rvb = 46.1 +/- 10.0 mins)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1216090Drug level in human urine treated with [14C]SB-649868 at 30 mg, po single dose after 3 hrs by HPLC-MSn analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID618082In vivo antagonist activity at OX1R in CD rat assessed as reduction of OX-A induced grooming dosed orally 3 hrs before OX-A injection measured after 1 hrs2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1280046Effect on sleep parameter in insomnia patient assessed as wake after sleep onset time at 10 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID765090Binding affinity to orexin receptor 2 (unknown origin)2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective orexin receptor antagonists.
AID618178Hypnotic activity in po dosed CD rat Circadian time model assessed as non-rapid eye movement latency period during active phase measured from starting time CT182011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID528164Antagonist activity against human orexin 1 receptor expressed in CHO cells assessed as effect in calcium mobilization by FLIPR assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.
AID619506Hypnotic activity in po dosed CD rat Circadian time model assessed as total sleep time measured during active phase after 5 hrs2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1280055Effect on sleep parameter in insomnia patient assessed as total sleep time at 60 mg, po administered two consecutive nights 90 mins prior to sleep by polysomnography2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
AID618075Half life in CD rat at 1 mg/kg, iv and 3 mg/kg, po2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618074Plasma clearance in CD rat at 1 mg/kg, iv and 3 mg/kg, po2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1216096Drug recovery in human plasma at 30, po single dose after 3 hrs by HPLC-MSn analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID618179Neurotoxicity in CD rat assessed as impairment of motor coordination at 1 to 10 mg/kg, po by rotarod test2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID618065Intrinsic clearance in rat liver microsomes2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1216099Cmax in human plasma treated with [14C]SB-649868 at 30 mg, po single dose2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
AID1346381Human OX1 receptor (Orexin receptors)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
AID1346418Human OX2 receptor (Orexin receptors)2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's14 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.54

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index20.54 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index5.91 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.54)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (35.71%)5.53%
Reviews4 (28.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (35.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		3.4811organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
zolpidem
Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.		5.341imidazopyridinecentral nervous system depressant;
GABA agonist;
sedative
thiazoles
[no description available]		9.35851,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		3.4611delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		4.1201,2,3-triazole
benzofurans
Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.		9.3585
sb 408124
SB 408124: a hypocretin receptor type 1 (HcrtR1) antagonist		3.1810organohalogen compound;
quinolines
jnj 10397049
JNJ 10397049: a selective orexin receptor-2 antagonist		4.3930
sb674042
SB674042: nonpeptide antagonist to the human orexin-1 receptor; structure in first source		3.1810
tcs ox2 29
[no description available]		3.1810
almorexant
almorexant: a dual orexin receptor antagonist for treatment of insomnia		5.5460isoquinolines
suvorexant
suvorexant: an orexin receptor antagonist; structure in first source. suvorexant : An aromatic amide obtained by formal condensation of the carboxy group of 5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid with the secondary amino group of 5-chloro-2-[(5R)-5-methyl-1,4-diazepan-1-yl]-1,3-benzoxazole. An orexin receptor antagonist used for the management of insomnia.		5.55601,3-benzoxazoles;
aromatic amide;
diazepine;
organochlorine compound;
triazoles		central nervous system depressant;
orexin receptor antagonist
mk-6096
MK-6096: antagonist of orexin receptors 1 and 2; structure in first source		5.3950
act-462206
ACT-462206: an antagonist of both orexin 1 and oxexin 2 receptors; structure in first source		3.2310
piperidines
Piperidines: A family of hexahydropyridines.		4.3930
gsk 1059865
[no description available]		3.1810
act-335827
[no description available]		3.1810
ConditionIndicatedRelationship StrengthStudiesTrials
Long Sleeper Syndrome
[description not available]		02.0610
Sleep Wake Disorders
Abnormal sleep-wake schedule or pattern associated with the CIRCADIAN RHYTHM which affect the length, timing, and/or rigidity of the sleep-wake cycle relative to the day-night cycle.		14.0610
Chronic Insomnia
[description not available]		08.3862
Sleep Initiation and Maintenance Disorders
Disorders characterized by impairment of the ability to initiate or maintain sleep. This may occur as a primary disorder or in association with another medical or psychiatric condition.		110.3862
Gelineau Syndrome
[description not available]		03.0410
Narcolepsy
A condition characterized by recurrent episodes of daytime somnolence and lapses in consciousness (microsomnias) that may be associated with automatic behaviors and AMNESIA. CATAPLEXY; SLEEP PARALYSIS, and hypnagogic HALLUCINATIONS frequently accompany narcolepsy. The pathophysiology of this disorder includes sleep-onset rapid eye movement (REM) sleep, which normally follows stage III or IV sleep. (From Neurology 1998 Feb;50(2 Suppl 1):S2-S7)		03.0410
Fasting Hypoglycemia
HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.		03.4811
Hypoglycemia
A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.		03.4811