Compounds > pexacerfont
Page last updated: 2024-11-11

pexacerfont

Cross-References

ID SourceID
PubMed CID9884366
CHEMBL ID482950
CHEBI ID177416
SCHEMBL ID5235999
MeSH IDM0537739

Synonyms (39)

Synonym
n-[(2r)-butan-2-yl]-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
pexacerfont
459856-18-9
CHEBI:177416
pyrazolo[1,5-a]-1,3,5-triazine, 13-15
bdbm29490
crf1 antagonist
bms562086
bms-562086
dpc-a69448
CHEMBL482950
8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-n-((1r)-1-methylpropyl)pyrazolo(1,5-a)-1,3,5-triazin-4-amine
unii-lf1vbg4zuk
pyrazolo(1,5-a)-1,3,5-triazin-4-amine, 8-(6-methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-n-((1r)-1-methylpropyl)-
pexacerfont [usan:inn]
lf1vbg4zuk ,
bms 562086
D10022
pexacerfont (usan/inn)
8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-n-[(1r)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine
pexacerfont [inn]
pexacerfont [usan]
n-((2r)-butan-2-yl)-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo(1,5-a)(1,3,5)triazin-4-amine
SCHEMBL5235999
AC-32621
DTXSID60196675
CS-6630
HY-12127
(r)-n-(sec-butyl)-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl pyrazolo[1,5-a][1,3,5]triazin-4-amine
DB12572
ZB1563
Q7179563
EX-A3079
8-(6-methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-n-[(1r)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine
D70085
n-((r)-sec-butyl)-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
MS-25202
gtpl10379
AKOS040742389

Research Excerpts

Overview

Pexacerfont is a corticotrophin-releasing factor subtype 1 receptor (CRF-1) antagonist. It was developed for potential treatment of anxiety and stress-related disorders.

ExcerptReferenceRelevance
"Pexacerfont is a corticotrophin-releasing factor subtype 1 receptor (CRF-1) antagonist developed for potential treatment of anxiety and stress-related disorders. "( T4-mediated rescue of aortic malformations in hypothyroid rats indicates maternal thyroid status can affect great vessel development.
Augustine-Rauch, K; Graziano, M; Liaw, JJ, 2021)		2.06
"Pexacerfont is a corticotropin-releasing factor subtype 1 receptor antagonist that was developed for the treatment of anxiety- and stress-related disorders. "( Toxicity of Pexacerfont, a Corticotropin-Releasing Factor Type 1 Receptor Antagonist, in Rats and Dogs.
Graziano, MJ; Sanderson, TP; White, MR, )		1.95

Treatment

ExcerptReferenceRelevance
"Pexacerfont treatment had no effect on alcohol craving, emotional responses, or anxiety."( The corticotropin releasing hormone-1 (CRH1) receptor antagonist pexacerfont in alcohol dependence: a randomized controlled experimental medicine study.
Anizan, S; Concheiro, M; George, DT; Heilig, M; Huestis, M; Kwako, LE; Momenan, R; Rio, DE; Schwandt, ML; Sinha, R; Spagnolo, PA; Thorsell, A, 2015)		1.38

Pharmacokinetics

ExcerptReferenceRelevance
"The absorption, distribution, metabolism, and excretion (ADME) and the pharmacokinetic characteristics of BMS-562086 [pexacerfont; 8-(6-methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]pyrazolo(1,5-a)-1,3,5-triazin-4-amine (DPC-A69448)] were investigated in vitro and in animals to support its clinical development."( In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Dockens, RC; Grossman, SJ; Iyer, RA; Liu-Kreyche, P; Zhou, L, 2012)		0.59

Bioavailability

ExcerptReferenceRelevance
" BMS-562086 was orally bioavailable in rats, dogs, and chimpanzees, with an absolute oral bioavailability of 40."( In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Dockens, RC; Grossman, SJ; Iyer, RA; Liu-Kreyche, P; Zhou, L, 2012)		0.38

Dosage Studied

Pexacerfont was used in a group of 10 patients who received open-label pexacerfont following the same dosing regimen. The cerebrospinal fluid was sampled to estimate central nervous system exposure.

ExcerptRelevanceReference
" A separate group of 10 patients received open-label pexacerfont following the same dosing regimen and had cerebrospinal fluid sampled to estimate central nervous system exposure."( The corticotropin releasing hormone-1 (CRH1) receptor antagonist pexacerfont in alcohol dependence: a randomized controlled experimental medicine study.
Anizan, S; Concheiro, M; George, DT; Heilig, M; Huestis, M; Kwako, LE; Momenan, R; Rio, DE; Schwandt, ML; Sinha, R; Spagnolo, PA; Thorsell, A, 2015)		0.9
" To better understand this relationship, pregnant rats were implanted with a subcutaneous L-thyroxine pellet designed to provide a sustained release of T4 throughout organogenesis in rat embryos (GD 6 to 15; the dosing period of pexacerfont)."( T4-mediated rescue of aortic malformations in hypothyroid rats indicates maternal thyroid status can affect great vessel development.
Augustine-Rauch, K; Graziano, M; Liaw, JJ, 2021)		0.81
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
pyrazolopyridine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Substance-K receptorHomo sapiens (human)IC50 (µMol)4.90000.00013.12109.5530AID353816
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki2.66000.00011.20929.9700AID353815
Corticotropin-releasing factor receptor 1Homo sapiens (human)IC50 (µMol)2.58770.00070.06490.3400AID1218590; AID1435127; AID1435128; AID353813
Corticotropin-releasing factor receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)0.03680.00420.03030.1290AID1799009; AID353808; AID353812; AID609183
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (49)

Processvia Protein(s)Taxonomy
muscle contractionSubstance-K receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-K receptorHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionSubstance-K receptorHomo sapiens (human)
intestine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionSubstance-K receptorHomo sapiens (human)
operant conditioningSubstance-K receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-K receptorHomo sapiens (human)
positive regulation of monoatomic ion transportSubstance-K receptorHomo sapiens (human)
positive regulation of smooth muscle contractionSubstance-K receptorHomo sapiens (human)
response to electrical stimulusSubstance-K receptorHomo sapiens (human)
prolactin secretionSubstance-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-K receptorHomo sapiens (human)
synaptic transmission, dopaminergicCorticotropin-releasing factor-binding proteinHomo sapiens (human)
inflammatory responseCorticotropin-releasing factor-binding proteinHomo sapiens (human)
signal transductionCorticotropin-releasing factor-binding proteinHomo sapiens (human)
female pregnancyCorticotropin-releasing factor-binding proteinHomo sapiens (human)
learning or memoryCorticotropin-releasing factor-binding proteinHomo sapiens (human)
hormone-mediated signaling pathwayCorticotropin-releasing factor-binding proteinHomo sapiens (human)
cellular response to potassium ionCorticotropin-releasing factor-binding proteinHomo sapiens (human)
regulated exocytosisCorticotropin-releasing factor-binding proteinHomo sapiens (human)
behavioral response to ethanolCorticotropin-releasing factor-binding proteinHomo sapiens (human)
regulation of corticotropin secretionCorticotropin-releasing factor-binding proteinHomo sapiens (human)
negative regulation of corticotropin secretionCorticotropin-releasing factor-binding proteinHomo sapiens (human)
cellular response to calcium ionCorticotropin-releasing factor-binding proteinHomo sapiens (human)
cellular response to cocaineCorticotropin-releasing factor-binding proteinHomo sapiens (human)
cellular response to cAMPCorticotropin-releasing factor-binding proteinHomo sapiens (human)
cellular response to tumor necrosis factorCorticotropin-releasing factor-binding proteinHomo sapiens (human)
cellular response to estrogen stimulusCorticotropin-releasing factor-binding proteinHomo sapiens (human)
cellular response to estradiol stimulusCorticotropin-releasing factor-binding proteinHomo sapiens (human)
cellular response to xenobiotic stimulusCorticotropin-releasing factor-binding proteinHomo sapiens (human)
regulation of cellular response to stressCorticotropin-releasing factor-binding proteinHomo sapiens (human)
cellular response to gonadotropin-releasing hormoneCorticotropin-releasing factor-binding proteinHomo sapiens (human)
negative regulation of corticotropin-releasing hormone receptor activityCorticotropin-releasing factor-binding proteinHomo sapiens (human)
regulation of NMDA receptor activityCorticotropin-releasing factor-binding proteinHomo sapiens (human)
immune responseCorticotropin-releasing factor receptor 1Homo sapiens (human)
cell surface receptor signaling pathwayCorticotropin-releasing factor receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCorticotropin-releasing factor receptor 1Homo sapiens (human)
activation of adenylate cyclase activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
female pregnancyCorticotropin-releasing factor receptor 1Homo sapiens (human)
parturitionCorticotropin-releasing factor receptor 1Homo sapiens (human)
regulation of adenylate cyclase activity involved in G protein-coupled receptor signaling pathwayCorticotropin-releasing factor receptor 1Homo sapiens (human)
adrenal gland developmentCorticotropin-releasing factor receptor 1Homo sapiens (human)
exploration behaviorCorticotropin-releasing factor receptor 1Homo sapiens (human)
fear responseCorticotropin-releasing factor receptor 1Homo sapiens (human)
behavioral response to ethanolCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotropin secretionCorticotropin-releasing factor receptor 1Homo sapiens (human)
general adaptation syndrome, behavioral processCorticotropin-releasing factor receptor 1Homo sapiens (human)
cellular response to corticotropin-releasing hormone stimulusCorticotropin-releasing factor receptor 1Homo sapiens (human)
negative regulation of voltage-gated calcium channel activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
regulation of corticosterone secretionCorticotropin-releasing factor receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
tachykinin receptor activitySubstance-K receptorHomo sapiens (human)
protein bindingSubstance-K receptorHomo sapiens (human)
substance K receptor activitySubstance-K receptorHomo sapiens (human)
protein bindingCorticotropin-releasing factor-binding proteinHomo sapiens (human)
peptide bindingCorticotropin-releasing factor-binding proteinHomo sapiens (human)
corticotropin-releasing hormone bindingCorticotropin-releasing factor-binding proteinHomo sapiens (human)
protein bindingCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotrophin-releasing factor receptor activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
G protein-coupled peptide receptor activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotropin-releasing hormone bindingCorticotropin-releasing factor receptor 1Homo sapiens (human)
corticotropin-releasing hormone receptor activityCorticotropin-releasing factor receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
plasma membraneSubstance-K receptorHomo sapiens (human)
sperm flagellumSubstance-K receptorHomo sapiens (human)
sperm headSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
plasma membraneSubstance-K receptorHomo sapiens (human)
endoplasmic reticulumCorticotropin-releasing factor-binding proteinHomo sapiens (human)
Golgi apparatusCorticotropin-releasing factor-binding proteinHomo sapiens (human)
extracellular regionCorticotropin-releasing factor-binding proteinHomo sapiens (human)
extracellular spaceCorticotropin-releasing factor-binding proteinHomo sapiens (human)
nucleusCorticotropin-releasing factor-binding proteinHomo sapiens (human)
secondary lysosomeCorticotropin-releasing factor-binding proteinHomo sapiens (human)
multivesicular bodyCorticotropin-releasing factor-binding proteinHomo sapiens (human)
microtubuleCorticotropin-releasing factor-binding proteinHomo sapiens (human)
secretory granuleCorticotropin-releasing factor-binding proteinHomo sapiens (human)
dendriteCorticotropin-releasing factor-binding proteinHomo sapiens (human)
dense core granuleCorticotropin-releasing factor-binding proteinHomo sapiens (human)
varicosityCorticotropin-releasing factor-binding proteinHomo sapiens (human)
perikaryonCorticotropin-releasing factor-binding proteinHomo sapiens (human)
axon terminusCorticotropin-releasing factor-binding proteinHomo sapiens (human)
extracellular spaceCorticotropin-releasing factor-binding proteinHomo sapiens (human)
endosomeCorticotropin-releasing factor receptor 1Homo sapiens (human)
plasma membraneCorticotropin-releasing factor receptor 1Homo sapiens (human)
membraneCorticotropin-releasing factor receptor 1Homo sapiens (human)
plasma membraneCorticotropin-releasing factor receptor 1Homo sapiens (human)
neuron projectionCorticotropin-releasing factor receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (228)

Assay IDTitleYearJournalArticle
AID354074Inhibition of ligand binding in neurokinin 2 receptor2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353851Clearance in chimpanzee at 0.5 mg/kg, iv2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218681AUC (infinity) in Sprague-Dawley rat at 5 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353829Ex vivo receptor occupancy of CRF receptor in rat brain at 10 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354084Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in intrapleural pressure at 5 mg/kg after intravenous infusion for 30 mins (RVb= -90.8+/-103 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218679Cmax in Sprague-Dawley rat at 5 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354104Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in airway resistance at 5 mg/kg after intravenous infusion for 30 mins (RVb= 20.2+/-12.3 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353832Toxicity in rat assessed as total distance traveled at 3 mg/kg, po after 1 hr by spontaneous locomotor test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353810Cmax in Beagle dog at 1 mg/kg, po by cassette dosing2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353828Ex vivo receptor occupancy of CRF receptor in rat brain at 3 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354329Effect on acute renal function in rat assessed as change in urine potassium level per 100 gm body weight at 30 mg/kg, po (RVb= 60.3+/-11.1 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353854Elimination half life in chimpanzee at 1 mg/kg, po2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354080Plasma concentration in dog at 5 mg/kg after intravenous infusion for 30 mins2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218706Drug metabolism in dog liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353844Cmax in rat at 5 mg/kg, po2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1435128Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method
AID354334Effect on acute renal function in rat assessed as change in urine urea level per 100 gm body weight at 30 mg/kg, po (RVb= 321+/-62 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353838Toxicity in rat assessed as time spent on rotarod at 10 mg/kg, po after 1 hr by rotarod test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354094Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in tidal volume at 5 mg/kg after intravenous infusion for 6 mins (RVb= 5.8+/-3.8 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353817Aqueous solubility at pH 7.42009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218701Drug metabolism in dog liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218695Drug metabolism in rat liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353822Anxiolytic activity in rat assessed as increase in time spent on open arm at 18 mg/kg, po by elevated plus-maze test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218618Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354090Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in respiration rate at 5 mg/kg after intravenous infusion for 6 mins (RVb= -8.3+/-8.3 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218694Drug metabolism in mouse liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218620Drug metabolism in mouse hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353853Elimination half life in chimpanzee at 0.5 mg/kg, iv2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353858Cardiovascular activity in mongrel dog assessed as change in QRS intervals2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354335Effect on acute renal function in rat assessed as change in glucose level in urine per 100 gm body weight at 30 mg/kg, po (RVb= 9.9+/-1.9 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218700Drug metabolism in rat liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354333Effect on acute renal function in rat assessed as change in urine creatinine level per 100 gm body weight at 30 mg/kg, po (RVb= 16.2+/-3.3 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218626Drug metabolism in rat hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354088Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in peak expiratory flow at 5 mg/kg after intravenous infusion for 30 mins (RVb= -3.3+/-6.4 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218715Detection of compound level in rat hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218705Drug metabolism in rat liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218606Drug metabolism in rat hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218684AUC (infinity) in beagle dog at 1 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218707Drug metabolism in cynomolgus monkey liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354102Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in airway resistance at 5 mg/kg after intravenous infusion for 6 mins (RVb= 3.9+/-4.7 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218673Drug metabolism in rat hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353818Solubility in 0.01 N HCl at pH 2.52009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354113Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in mean arterial pressure at 5 mg/kg after intravenous infusion for 60 mins (RVb= 5.1+/-3.5 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354331Effect on acute renal function in rat assessed as change in urine protein level per 100 gm body weight at 30 mg/kg, po (RVb= 12.0+/-2.4 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353848AUC (0 to infinity) in chimpanzee at 0.5 mg/kg, iv2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218688Drug metabolism in human cryopreserved hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218639Terminal half life in chimpanzee at 0.5 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218696Drug metabolism in beagle dog liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218668Drug metabolism in rat hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218664Detection of compound level in cynomolgus monkey liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353834Toxicity in rat assessed as total distance traveled at 30 mg/kg, po after 1 hr by spontaneous locomotor test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353846AUC in rat at 1 mg/kg, iv and 5 mg/kg, po2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354097Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in tidal volume at 5 mg/kg after intravenous infusion for 60 mins (RVb= 13.0+/-10.3 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354121Plasma concentration in spontaneously breathing dog at 5 mg/kg, iv after 60 mins2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353850Cmax in chimpanzee at 1 mg/kg, po2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218717Detection of compound level in cynomolgus monkey cryopreserved hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218704Drug metabolism in mouse liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354089Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in peak expiratory flow at 5 mg/kg after intravenous infusion for 60 mins (RVb= 0.4+/-6.7 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353820Solubility in acetone2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218634Tmax in beagle dog at 5 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218602Drug metabolism in beagle dog hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218644AUC (infinity) in chimpanzee at 1 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218685Terminal half life in beagle dog at 1 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218609Drug metabolism in human cryopreserved hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353827Ex vivo receptor occupancy of CRF receptor in rat brain at 1 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353806Lipophilicity log P of the compound2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218646Oral bioavailability in chimpanzee at 5 mg/kg2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354118Plasma concentration in spontaneously breathing dog at 5 mg/kg, iv after 6 mins2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218636Terminal half life in beagle dog at 5 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218674Drug metabolism in human liver microsomes assessed as BMS-572273 metabolite formation at 100 uM after 1 hr in presence of NADPH and ketoconazole2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218689Drug metabolism in mouse liver microsomes at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218680Tmax in Sprague-Dawley rat at 5 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218594Protein binding in rat serum after 3 hrs by equilibrium dialysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218699Drug metabolism in mouse liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218633Cmax in beagle dog at 5 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218692Drug metabolism in cynomolgus monkey liver microsomes at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218598Metabolic stability in dog serum after 3 hrs by equilibrium dialysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218714Detection of compound level in mouse hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353830Ex vivo receptor occupancy of CRF receptor in rat brain at 30 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218690Drug metabolism in rat liver microsomes at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218686Drug metabolism in beagle dog hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354105Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in airway resistance at 5 mg/kg after intravenous infusion for 60 mins (RVb= 17.3+/-15.1 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354338Plasma concentration in rat at 30 mg/kg, po after 1 hr2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218617Drug metabolism in beagle dog hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218625Drug metabolism in mouse hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353811Half life in Beagle dog at 1 mg/kg, po by cassette dosing2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218678Terminal volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354101Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in minute volume at 5 mg/kg after intravenous infusion for 60 mins (RVb= -13.4+/-10.7 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218631Plasma clearance in beagle dog at 1 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218628Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1435127Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
AID1218622Drug metabolism in beagle dog hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218691Drug metabolism in dog liver microsomes at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353809AUC in Beagle dog at 1 mg/kg, po by cassette dosing2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353845Tmax in rat at 5 mg/kg, po2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354107Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in pulmonary compliance at 5 mg/kg after intravenous infusion for 15 mins (RVb= 0.8+/-2.0 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218675AUC (infinity) in Sprague-Dawley rat at 1 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354079Plasma concentration in dog at 3 mg/kg after intravenous infusion for 30 mins2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353826Ex vivo receptor occupancy of CRF receptor in rat brain at 0.3 mg/kg, po by [125I]sauvagine binding and autoradiography relative to control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354108Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in pulmonary compliance at 5 mg/kg after intravenous infusion for 30 mins (RVb= -2.8+/-4.0 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218599Metabolic stability in human serum after 3 hrs by equilibrium dialysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218716Detection of compound level in beagle dog hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354116Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in heart rate at 5 mg/kg after intravenous infusion for 30 mins (RVb= -0.9+/-3.8 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218682Terminal half life in Sprague-Dawley rat at 5 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354075Cardiovascular activity in spontaneously breathing mongrel dog at assessed as increase in contractility at 3 mg/kg to 5 mg/kg, iv by dose escalation study2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353833Toxicity in rat assessed as total distance traveled at 10 mg/kg, po after 1 hr by spontaneous locomotor test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354078Plasma concentration in dog at 1 mg/kg after intravenous infusion for 30 mins2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354081Cardiovascular activity in mongrel dog assessed as change in heart rate2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218697Drug metabolism in cynomolgus monkey liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354109Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in pulmonary compliance at 5 mg/kg after intravenous infusion for 60 mins (RVb= -4.8+/-4.5 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218615Drug metabolism in mouse hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353814Displacement of [125I]Tyr0-sauvagine from CRF2beta receptor expressed in pig choroid plexus membrane2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218595Protein binding in dog serum after 3 hrs by equilibrium dialysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218623Drug metabolism in cynomolgus monkey cryopreserved hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218593Apparent permeability from apical to basolateral side in human Caco2 cells2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354339Plasma concentration in rat at 30 mg/kg, po after 5 hrs2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353843Elimination half life in rat at 1 mg/kg, iv and 5 mg/kg, po2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353808Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354087Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in peak expiratory flow at 5 mg/kg after intravenous infusion for 15 mins (RVb= -8.4+/-6.6 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354092Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in respiration rate at 5 mg/kg after intravenous infusion for 30 mins (RVb= -4.5+/-8.2 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354131Effect on acute renal function in rat assessed as change in urine chloride level per 100 gm body weight at 30 mg/kg, po (RVb= 95.3+/-11.6 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353859Cardiovascular activity in mongrel dog assessed as change in PR intervals2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218676Terminal half life in Sprague-Dawley rat at 1 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353841Clearance in rat at 1 mg/kg, iv and 5 mg/kg, po2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353839Toxicity in rat assessed as time spent on rotarod at 30 mg/kg, po after 1 hr by rotarod test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353812Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354120Plasma concentration in spontaneously breathing dog at 5 mg/kg, iv after 30 mins2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354093Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in respiration rate at 5 mg/kg after intravenous infusion for 60 mins (RVb= -19.5+/-16.3 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353816Binding affinity to human neurokinin 2 receptor2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218601Drug metabolism in rat hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218672Drug metabolism in mouse hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354115Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in heart rate at 5 mg/kg after intravenous infusion for 15 mins (RVb= -2.3+/-1.7 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354112Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in mean arterial pressure at 5 mg/kg after intravenous infusion for 30 mins (RVb= 4.0+/-3.0 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218698Drug metabolism in human liver microsomes assessed as DPH-123554 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354091Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in respiration rate at 5 mg/kg after intravenous infusion for 15 mins (RVb= -6.4+/-4.0 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218632Terminal volume of distribution in beagle dog at 1 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218667Drug metabolism in human liver microsomes assessed as DPH-124921 metabolite formation at 100 uM after 1 hr in presence of NADPH and ketoconazole2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218643Tmax in chimpanzee at 1 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218640Plasma clearance in chimpanzee at 0.5 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353823Anxiolytic activity in rat assessed as increase in time spent on open arm at 30 mg/kg, po by elevated plus-maze test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354085Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in intrapleural pressure at 5 mg/kg after intravenous infusion for 60 mins (RVb= 18.5+/-19.9 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218619Drug metabolism in human cryopreserved hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218708Drug metabolism in human liver microsomes assessed as BMS-572273 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354077Plasma concentration in dog at 0.3 mg/kg after intravenous infusion for 30 mins2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1435129Ratio of IC50 for displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes with compound washout to IC50 for displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes without compound wash
AID354119Plasma concentration in spontaneously breathing dog at 5 mg/kg, iv after 15 mins2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354336Effect on acute renal function in rat assessed as change in osmolality in urine per 100 gm body weight at 30 mg/kg, po (RVb= 325+/-1.9 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353847Oral bioavailability in rat at 5 mg/kg2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354083Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in intrapleural pressure at 5 mg/kg after intravenous infusion for 15 mins (RVb= 12.6+/-17.1 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354114Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in heart rate at 5 mg/kg after intravenous infusion for 6 mins (RVb= -0.4+/-0.7 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353824Anxiolytic activity in rat assessed as decrease in latency to exit dark chamber at 10 mg/kg, po by defensive withdrawal test relative to untreated control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354332Effect on acute renal function in rat assessed as change in urine phosphate level per 100 gm body weight at 30 mg/kg, po (RVb= 8.7+/-2.3 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218660Detection of compound level in human cryopreserved hepatocytes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353835Toxicity in rat assessed as total distance traveled at 100 mg/kg, po after 1 hr by spontaneous locomotor test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218663Detection of compound level in beagle dog liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353855Oral bioavailability in chimpanzee at 1 mg/kg2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218605Drug metabolism in mouse hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218597Metabolic stability in rat serum after 3 hrs by equilibrium dialysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218591Binding affinity to CRF-binding protein (unknown origin)2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354096Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in tidal volume at 5 mg/kg after intravenous infusion for 30 mins (RVb= 6.1+/-5.6 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218647Retention time of the compound by HPLC method2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353861Cardiovascular activity in dog assessed as increase in mean atrial pressure at 3 mg to 5 mg/kg, iv by dose escalation study2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353837Toxicity in rat assessed as time spent on rotarod at 3 mg/kg, po after 1 hr by rotarod test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354086Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in peak expiratory flow at 5 mg/kg after intravenous infusion for 6 mins (RVb= 3.6+/-3.7 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218661Detection of compound level in mouse liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354344Agonist activity at CRF1 receptor in rat pituitary cells2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218608Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218637Oral bioavailability in beagle dog at 5 mg/kg2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354082Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in intrapleural pressure at 5 mg/kg after intravenous infusion for 6 mins (RVb= -21.2+/-26.5 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353849AUC (0 to infinity) in chimpanzee at 1 mg/kg, po2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218702Drug metabolism in cynomolgus monkey liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218693Drug metabolism in human liver microsomes at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354103Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in airway resistance at 5 mg/kg after intravenous infusion for 15 mins (RVb= 27.8+/-17.9 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218592Selectivity ratio of IC50 for CRF-binding protein (unknown origin) to IC50 for human CRF1 receptor2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353825Anxiolytic activity in rat assessed as decrease in latency to exit dark chamber at 3 mg/kg, po by defensive withdrawal test relative to untreated control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354110Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in mean arterial pressure at 5 mg/kg after intravenous infusion for 6 mins (RVb= 1.5+/-0.9 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218645Terminal half life in chimpanzee at 1 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354098Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in minute volume at 5 mg/kg after intravenous infusion for 6 mins (RVb= -3.6+/-7.5 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218642Cmax in chimpanzee at 1 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218666Drug metabolism in human liver microsomes assessed as DPH-123554 metabolite formation at 100 uM after 1 hr in presence of NADPH and ketoconazole2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353836Toxicity in rat assessed as time spent on rotarod at 1 mg/kg, po after 1 hr by rotarod test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218596Protein binding in human serum after 3 hrs by equilibrium dialysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218669Drug metabolism in beagle dog hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218662Detection of compound level in rat liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353840Toxicity in rat assessed as time spent on rotarod at 100 mg/kg, po after 1 hr by rotarod test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218630Drug metabolism in mouse hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353819Solubility in ethanol2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID609183Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting2011Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.
AID1218635AUC (infinity) in beagle dog at 5 mg/kg, po2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354337Effect on acute renal function in rat assessed as change in urine volume per 100 gm body weight at 30 mg/kg, po (RVb= 1.7+/-0.2 ml/100g)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354076Binding affinity to human recombinant CRF binding protein2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218703Drug metabolism in human liver microsomes assessed as DPH-124921 metabolite level at 100 uM after 1 hr in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218600Drug metabolism in mouse hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353842Volume of distribution at steady state in rat at 1 mg/kg, iv and 5 mg/kg, po2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218590Antagonist activity at human CRF1 receptor2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354111Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in mean arterial pressure at 5 mg/kg after intravenous infusion for 15 mins (RVb= 2.1+/-1.5 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354330Effect on acute renal function in rat assessed as change in urine sodium level per 100 gm body weight at 30 mg/kg, po (RVb= 49.9+/-3.1 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354099Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in minute volume at 5 mg/kg after intravenous infusion for 15 mins (RVb= -4.7+/-3.4 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218629Drug metabolism in human cryopreserved hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218616Drug metabolism in rat hepatocytes assessed as decrease of compound level at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218687Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as BMS-572273 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218683Oral bioavailability in Sprague-Dawley rat at 5 mg/kg2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354095Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in tidal volume at 5 mg/kg after intravenous infusion for 15 mins (RVb= 2.2+/-4.3 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354100Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in minute volume at 5 mg/kg after intravenous infusion for 30 mins (RVb= 1.0+/-9.7 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218627Drug metabolism in beagle dog hepatocytes assessed as DPH-123554 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354130Effect on acute renal function in rat assessed as change in urine pH per 100 gm body weight at 30 mg/kg, po (RVb= 7.74+/-0.07 mg/dl)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218677Plasma clearance in Sprague-Dawley rat at 1 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218638AUC (infinity) in chimpanzee at 0.5 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218665Detection of compound level in human liver microsomes treated with 25 uM of BMS-562086 after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218621Drug metabolism in rat hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218604Drug metabolism in human cryopreserved hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353815Binding affinity to rat adenosine A1 receptor expressed in CHO cells2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218641Terminal volume of distribution in chimpanzee at 0.5 mg/kg, iv2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID1218670Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353860Cardiovascular activity in dog assessed as increase in mean atrial pressure at 5 mg/kg, iv2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354343Inhibition of ligand binding in adenosine A1 receptor2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353857Cardiovascular activity in mongrel dog assessed as change in QT intervals2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218603Drug metabolism in cynomolgus monkey cryopreserved hepatocytes assessed as 7-ethoxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353852Volume of distribution at steady state in chimpanzee at 0.5 mg/kg, iv2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218671Drug metabolism in human cryopreserved hepatocytes assessed as DPH-124921 metabolite level at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID354117Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in heart rate at 5 mg/kg after intravenous infusion for 60 mins (RVb= -0.9+/-5.8 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218624Drug metabolism in human cryopreserved hepatocytes at 25 uM after 3 hrs by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353813Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID354106Effect on respiratory function in spontaneously breathing mongrel dog assessed as change in pulmonary compliance at 5 mg/kg after intravenous infusion for 6 mins (RVb= 6.0+/-4.2 %)2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1218607Drug metabolism in beagle dog hepatocytes assessed as 7-hydroxycoumarin formation at 25 uM after 3 hrs by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
AID353831Toxicity in rat assessed as total distance traveled at 1 mg/kg, po after 1 hr by spontaneous locomotor test2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID353856Cardiovascular activity in mongrel dog assessed as change in QTc intervals2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
AID1799009In Vitro Binding Autoradiography from Article 10.1021/jm900025h: \\Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.\\2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (16.67)29.6817
2010's9 (75.00)24.3611
2020's1 (8.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.68

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 Index27.68 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.84 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.68)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (38.46%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (61.54%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chlordiazepoxide
Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2.		2.0510benzodiazepine
citalopram
Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group.		4.36112-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound
furosemide
Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.		2.0510chlorobenzoic acid;
furans;
sulfonamide		environmental contaminant;
loop diuretic;
xenobiotic
thyroxine
Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions.		2.31102-halophenol;
iodophenol;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid;
thyroxine zwitterion;
thyroxine		antithyroid drug;
human metabolite;
mouse metabolite;
thyroid hormone
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		2.0510ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
alanine
Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.		2.0710alanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid		EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
mannitol
[no description available]		2.0710mannitolallergen;
antiglaucoma drug;
compatible osmolytes;
Escherichia coli metabolite;
food anticaking agent;
food bulking agent;
food humectant;
food stabiliser;
food thickening agent;
hapten;
metabolite;
osmotic diuretic;
sweetening agent
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		2.0810indazole
isoxazoles
Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.		2.0710isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
methamphetamine
Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.		8.5611amphetamines;
secondary amine		central nervous system stimulant;
environmental contaminant;
neurotoxin;
psychotropic drug;
xenobiotic
7-ethoxycoumarin
7-ethoxycoumarin : A member of the class of coumarins that is umbelliferone in which the hydroxy group at position 7 is replaced by an ethoxy group.		2.0710aromatic ether;
coumarins
atropine
tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.		2.0510
nbi 27914
[no description available]		2.0610dialkylarylamine;
tertiary amino compound
razaxaban
razaxaban: structure in first source		2.0710
7-hydroxycoumarin
7-oxycoumarin: derivatives have anti-oxidant properties. umbelliferone : A hydroxycoumarin that is coumarin substituted by a hydroxy group ay position 7.		2.0710hydroxycoumarinfluorescent probe;
food component;
plant metabolite
cp 154526
[no description available]		2.0610
heroin
Heroin: A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed). heroin : A morphinane alkaloid that is morphine bearing two acetyl substituents on the O-3 and O-6 positions. As with other opioids, heroin is used as both an analgesic and a recreational drug. Frequent and regular administration is associated with tolerance and physical dependence, which may develop into addiction. Its use includes treatment for acute pain, such as in severe physical trauma, myocardial infarction, post-surgical pain, and chronic pain, including end-stage cancer and other terminal illnesses.		8.5611morphinane alkaloidmu-opioid receptor agonist;
opioid analgesic;
prodrug
r 121919
[no description available]		2.0610
nbi-34041
NBI-34041: high-affinity CRF1 (corticotropin-releasing factor receptor 1) receptor antagonist for attenuating elevated stress response		2.0610
dmp 696
DMP 696: a CRF(1) receptor antagonist; structure in first source		2.4620
brivanib
[no description available]		2.0710aromatic ether;
diether;
fluoroindole;
pyrrolotriazine;
secondary alcohol		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist
cp 154526
CP 154526: structure in first source		2.0510
ConditionIndicatedRelationship StrengthStudiesTrials
Central Hypothyroidism
[description not available]		02.3110
Complications, Pregnancy
[description not available]		02.3110
Hypothyroidism
A syndrome that results from abnormally low secretion of THYROID HORMONES from the THYROID GLAND, leading to a decrease in BASAL METABOLIC RATE. In its most severe form, there is accumulation of MUCOPOLYSACCHARIDES in the SKIN and EDEMA, known as MYXEDEMA. It may be primary or secondary due to other pituitary disease, or hypothalamic dysfunction.		02.3110
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.3110
Vascular Malformations
A spectrum of congenital, inherited, or acquired abnormalities in BLOOD VESSELS that can adversely affect the normal blood flow in ARTERIES or VEINS. Most are congenital defects such as abnormal communications between blood vessels (fistula), shunting of arterial blood directly into veins bypassing the CAPILLARIES (arteriovenous malformations), formation of large dilated blood blood-filled vessels (cavernous angioma), and swollen capillaries (capillary telangiectases). In rare cases, vascular malformations can result from trauma or diseases.		02.3110
Chemical Dependence
[description not available]		03.5611
Drug Withdrawal Symptoms
[description not available]		03.5611
Substance Withdrawal Syndrome
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.		03.5611
Substance-Related Disorders
Disorders related to substance use or abuse.		03.5611
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0810
Alcohol Abuse
[description not available]		04.4111
Alcoholism
A primary, chronic disease with genetic, psychosocial, and environmental factors influencing its development and manifestations. The disease is often progressive and fatal. It is characterized by impaired control over drinking, preoccupation with the drug alcohol, use of alcohol despite adverse consequences, and distortions in thinking, most notably denial. Each of these symptoms may be continuous or periodic. (Morse & Flavin for the Joint Commission of the National Council on Alcoholism and Drug Dependence and the American Society of Addiction Medicine to Study the Definition and Criteria for the Diagnosis of Alcoholism: in JAMA 1992;268:1012-4)		04.4111
Colitis, Mucous
[description not available]		03.4311
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		03.4311
Depression
Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.		03.4311
Irritable Bowel Syndrome
A disorder with chronic or recurrent colonic symptoms without a clearcut etiology. This condition is characterized by chronic or recurrent ABDOMINAL PAIN, bloating, MUCUS in FECES, and an erratic disturbance of DEFECATION.		15.4311
Anxiety Neuroses
[description not available]		04.3611
Anxiety Disorders
Persistent and disabling ANXIETY.		16.3611
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