Page last updated: 2024-12-11

ro 70-0004

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID9872515
CHEMBL ID24777
SCHEMBL ID7822496
MeSH IDM0331766

Synonyms (19)

Synonym
gtpl497
ro-70-0004
3-[3-[4-[4-fluoro-2-(2,2,2-trifluoroethoxy)phenyl]piperazin-1-yl]propyl]-5-methyl-1h-pyrimidine-2,4-dione
CHEMBL24777 ,
rs-100975
ro-700004
L000519
bdbm50160152
3-(3-{4-[4-fluoro-2-(2,2,2-trifluoro-ethoxy)-phenyl]-piperazin-1-yl}-propyl)-5-methyl-1h-pyrimidine-2,4-dione
3-(3-{3-[4-fluoro-2-(2,2,2-trifluoro-ethoxy)-phenyl]-piperazin-1-yl}-propyl)-5-methyl-1h-pyrimidine-2,4-dione
SCHEMBL7822496
unii-3ak2rkg763
ro700004
wezfjpkjuigdps-uhfffaoysa-n
186386-21-0
Q27088602
2,4(1h,3h)-pyrimidinedione, 3-(3-(4-(4-fluoro-2-(2,2,2-trifluoroethoxy)phenyl)-1-piperazinyl)propyl)-5-methyl-
3AK2RKG763 ,
AKOS040749356

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Dog pharmacokinetic parameters of 12 (RO700004) and its metabolite 40 (RO1104253) were established."( Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
Arias, L; Blue, DR; Chan, R; Clarke, DE; Elworthy, TR; Ford, AP; Guzman, A; Jaime-Figueroa, S; Jasper, JR; Lopez, FJ; Morgans, DJ; Padilla, F; Perez-Medrano, A; Quintero, C; Romero, M; Sandoval, L; Smith, SA; Williams, TJ, 2003
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1A adrenergic receptorOryctolagus cuniculus (rabbit)Ki0.00100.00000.02040.2512AID36753
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.06310.00000.929610.0000AID35473
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.06310.00000.970810.0000AID35473
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.06310.00000.937510.0000AID35473
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.08160.00000.360910.0000AID35468; AID35473
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.00110.00000.272610.0000AID36753; AID36758
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.07940.00000.471310.0000AID37478; AID37486
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (37)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID9894Volume of distribution by as 4 fold increase by iv administration in dogs2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID5936350% reduction in agonist induced pressor response in anesthetized dog1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID35616Antagonist inhibition noradrenaline-stimulated contractions of rat aortic strings for Alpha-1D adrenergic receptor2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID5936450% reduction in intraurethral pressure (IUP) in response to hypogastric nerve stimulation or agonist (phenylephrine or norepinephrine) administration in anesthetized dog1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID36765Antagonist inhibition of noradrenaline-stimulated contractions of rabbit bladderneck (RBN) for Alpha-1A adrenergic receptor2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID35473Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1D adrenergic receptor2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID35441Ratio of binding affinities for human cloned alpha1D- adrenoceptor to that of human cloned alpha1A- adrenoceptor (alpha-1D/alpha-1A)2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID8529Plasma clearance by iv administration in dog at a dose of 0.3 mg/kg2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID9706Half life period by iv administration in dog at a dose of 0.3 mg/kg2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID36624Ratio of antagonistic activities against alpha-1A vs alpha-1B determined in rat aorta and rabbit bladder neck respectively2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID36758Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID9325Oral bioavailability in dog2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID239800Binding affinity for alpha 1b adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID239799Binding affinity for alpha 1a adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID9707Half life period by po administration in dog at a dose of 0.3 mg/kg2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID37486Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1B adrenergic receptor2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID36753Binding affinity was tested on human Alpha-1A adrenergic receptor1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID36124pA2 for Alpha-1 adrenergic receptor from human prostate.1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID37478Binding affinity was tested on human Alpha-1B adrenergic receptor1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID9324Oral bioavailability in dog (i.v. dosing)2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID239801Binding affinity for alpha 1d adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID9546In vitro relative rate of metabolism was determined in dog liver microsomes2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID37341Ratio of binding affinities for human cloned alpha1B- adrenoceptor to that of human cloned alpha1A- adrenoceptor (alpha-1B/alpha-1A)2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
AID239249Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists.
AID229372Ratio of intraurethral pressure to that of pressor response in dog.1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID35468Binding affinity was tested on human Alpha-1D adrenergic receptor1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID1345971Human alpha1D-adrenoceptor (Adrenoceptors)1999British journal of pharmacology, May, Volume: 127, Issue:1
In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.
AID1346000Human alpha1B-adrenoceptor (Adrenoceptors)1999British journal of pharmacology, May, Volume: 127, Issue:1
In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)1999British journal of pharmacology, May, Volume: 127, Issue:1
In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (40.00)18.2507
2000's3 (60.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.66

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.66 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.66)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]