Compounds > snap 6201
Page last updated: 2024-11-12

snap 6201

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 CID10099811
CHEMBL ID356584
MeSH IDM0353076

Synonyms (6)

Synonym
L014930
bdbm50082784
1-(3-{[5-carbamoyl-6-(3,4-difluoro-phenyl)-4-ethyl-2-oxo-3,6-dihydro-2h-pyrimidine-1-carbonyl]-amino}-propyl)-4-phenyl-piperidine-4-carboxylic acid methyl ester
snap-6201
CHEMBL356584 ,
methyl 1-[3-[[5-carbamoyl-4-(3,4-difluorophenyl)-6-ethyl-2-oxo-1,4-dihydropyrimidine-3-carbonyl]amino]propyl]-4-phenylpiperidine-4-carboxylate
[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)
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki4.00000.00000.38458.6000AID152093
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.00020.00000.272610.0000AID36608
Mu-type opioid receptorHomo sapiens (human)Ki4.00000.00000.419710.0000AID152093; AID152203
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Ki4.00000.00000.27869.0000AID152093; AID152203
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kb1.00000.02800.45400.8800AID37162
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kb1.00000.01180.30660.8800AID37162
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kb0.75010.00040.30280.8800AID36889; AID37162
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (46)

Processvia Protein(s)Taxonomy
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 pathway, coupled to cyclic nucleotide second messengerMu-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
sensory perceptionMu-type opioid receptorHomo sapiens (human)
negative regulation of cell population proliferationMu-type opioid receptorHomo sapiens (human)
sensory perception of painMu-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayMu-type opioid receptorHomo sapiens (human)
behavioral response to ethanolMu-type opioid receptorHomo sapiens (human)
positive regulation of neurogenesisMu-type opioid receptorHomo sapiens (human)
negative regulation of Wnt protein secretionMu-type opioid receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMu-type opioid receptorHomo sapiens (human)
calcium ion transmembrane transportMu-type opioid receptorHomo sapiens (human)
cellular response to morphineMu-type opioid receptorHomo sapiens (human)
regulation of cellular response to stressMu-type opioid receptorHomo sapiens (human)
regulation of NMDA receptor activityMu-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayMu-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
G-protein alpha-subunit bindingMu-type opioid receptorHomo sapiens (human)
G protein-coupled receptor activityMu-type opioid receptorHomo sapiens (human)
beta-endorphin receptor activityMu-type opioid receptorHomo sapiens (human)
voltage-gated calcium channel activityMu-type opioid receptorHomo sapiens (human)
protein bindingMu-type opioid receptorHomo sapiens (human)
morphine receptor activityMu-type opioid receptorHomo sapiens (human)
G-protein beta-subunit bindingMu-type opioid receptorHomo sapiens (human)
neuropeptide bindingMu-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
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)
endosomeMu-type opioid receptorHomo sapiens (human)
endoplasmic reticulumMu-type opioid receptorHomo sapiens (human)
Golgi apparatusMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
axonMu-type opioid receptorHomo sapiens (human)
dendriteMu-type opioid receptorHomo sapiens (human)
perikaryonMu-type opioid receptorHomo sapiens (human)
synapseMu-type opioid receptorHomo sapiens (human)
plasma membraneMu-type opioid receptorHomo sapiens (human)
neuron projectionMu-type opioid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (59)

Assay IDTitleYearJournalArticle
AID36129Antagonistic activity against Alpha-1 adrenergic receptor in human prostate tissue using phenylephrine as agonist1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID23622Plasma half life in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID93444Binding affinity in human prostate using A-616031999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID19919Duration of action in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID93442Antagonism against phenylephrine induced contractions in isolated prostate tissue of human1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID58519Potency to inhibit phenylephrine stimulated diastolic blood pressure in dog.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID23618Plasma half life in dog1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID23621Plasma half life in dog.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID22958Duration of action in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID229705Fold selectivity (alpha-1b,1d/ Alpha-1A) in rat (using [3H]-prazosin as a radioligand)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID196113Inhibition of phenylephrine induced contraction of the rat prostate.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID23625Plasma half life in rat.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID186989Antagonism against phenylephrine induced contractions in isolated prostate tissue of rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID23623Plasma half life in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID229687Selectivity ratio( alpha-1b,1d/alpha1a)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID36770In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID23619Plasma half life in dog1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID37161Antagonistic activity against Alpha-1 adrenergic receptor in rat prostate tissue using A61603 as agonist1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID37329In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID36611In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID36467In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of dog1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID152093Binding affinity against opioid receptor using [3H]-DAMGO as radioligand.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID35323In vitro binding affinity against alpha-1D adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID229688Selectivity ratio( alpha-1b,1d/alpha1a)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID18652The oral bioavailability in dog1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID196112Dose required to inhibit 50% of the contractions produced by phenylephrine in rat prostate1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID37162Binding affinity radioligand)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID37328In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID36889Binding affinity radioligand)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID239202Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists.
AID711521Inhibition of alpha 1a adrenoceptor2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Synopsis of some recent tactical application of bioisosteres in drug design.
AID36610In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID195210Antagonism against norepinephrine induced contractions in rat aorta.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID229690Selectivity ratio( alpha-2a,2b,2c/alpha1a)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID229706Fold selectivity (alpha-2a,b,c/ Alpha-1A) in rat (using [3H]rauwolscine as a radioligand)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID196114Antagonism against phenylephrine induced contractions in rat prostate.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID58517Potency to inhibit phenylephrine induced intraurethral pressure in dog1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID35322In vitro binding affinity against Alpha-1D adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID169744Dose required to produce 50% inhibition of phenylephrine induced contractile response in situ rat prostate.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID226253Fold selectivity against alpha 1A adrenergic receptor over alpha 2A, 2B and 2C adrenergic receptors1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID18392Oral bioavailability in dog1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID37327In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID18631Bioavailability in dog1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID197107Antagonistic activity against norepinephrine induced contractions in rat vas deferens.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID58505Antagonism against phenylephrine induced contractions in isolated prostate tissue of dog1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID169745Dose required to produce 50% inhibition of phenylephrine induced diastolic blood pressure in rat.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID36612In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID19920Duration of action in rat.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID35324In vitro binding affinity against Alpha-1D adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID58520Potency to inhibit phenylephrine stimulated intraurethral pressure in dog.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID36609In vitro binding affinity against Alpha-1A adrenergic receptor in isolated prostate tissue of human1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID58515Potency to inhibit phenylephrine induced diastolic blood pressure in dog1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID18633Bioavailability in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID18653Oral bioavailability in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID18395Oral bioavailability in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID36608In vitro binding affinity radioligand1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID152203Binding affinity against Opioid receptor mu 11999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID195211Antagonistic activity against norepinephrine induced contractions in rat aorta.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID229689Selectivity ratio( alpha-2a,2b,2c/alpha1a)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
[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's3 (60.00)18.2507
2000's1 (20.00)29.6817
2010's1 (20.00)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: 12.60

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 Index12.60 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.39 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		2.0610amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
phenol
[no description available]		2.0610phenolsantiseptic drug;
disinfectant;
human xenobiotic metabolite;
mouse metabolite
acetohydroxamic acid
acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group.		2.0610acetohydroxamic acids;
carbohydroximic acid		algal metabolite;
EC 3.5.1.5 (urease) inhibitor
bmy 7378
[no description available]		2.0210piperazines
celecoxib
[no description available]		2.0610organofluorine compound;
pyrazoles;
sulfonamide;
toluenes		cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		2.0610aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		2.0610biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
naftopidil
[no description available]		2.0210piperazines
nan 190
1-(2-methoxyphenyl)-4-(4-(2-phthalimido)butyl)piperazine: RN from Toxlit. NAN 190 : An N-alkylpiperazine that consists of (2-methoxyphenyl)piperazine in which the amine hydrogen is substituted by a 4-(2-phthalimido)butyl group.		2.0210N-alkylpiperazine;
N-arylpiperazine;
phthalimides		serotonergic antagonist
nimesulide
nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups.		2.0610aromatic ether;
C-nitro compound;
sulfonamide		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
pd 153035
4-((3-bromophenyl)amino)-6,7-dimethoxyquinazoline: structure given in first source. PD-153035 : A member of the class of quinazolines carrying a 3-bromophenylamino substituent at position 4 and two methoxy substituents at positions 6 and 7.		2.0610aromatic amine;
aromatic ether;
bromobenzenes;
quinazolines;
secondary amino compound		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist
prazosin
Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.		210aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
risperidone
Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.		2.02101,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist
spiperone
Spiperone: A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.. spiperone : An azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.		2.0210aromatic ketone;
azaspiro compound;
organofluorine compound;
piperidines;
tertiary amino compound		alpha-adrenergic antagonist;
antipsychotic agent;
dopaminergic antagonist;
psychotropic drug;
serotonergic antagonist
terazosin
Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia		2.6930furans;
piperazines;
primary amino compound;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
trifluperidol
Trifluperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in the treatment of PSYCHOSES including MANIA and SCHIZOPHRENIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p621)		2.0610aromatic ketone
venlafaxine
venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.		2.0610cyclohexanols;
monomethoxybenzene;
tertiary alcohol;
tertiary amino compound		adrenergic uptake inhibitor;
analgesic;
antidepressant;
dopamine uptake inhibitor;
environmental contaminant;
serotonin uptake inhibitor;
xenobiotic
estrone
Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.		2.061017-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols		antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
nifenalol
nifenalol: adrenergic beta-blocker with good antiarrhythmic properties; also tends to lower blood pressure & provide protection against angina; minor descriptor (75-86); on-line & INDEX MEDICUS search ETHANOLAMINES (75-86); RN given refers to parent cpd without isomeric designation		2.0610C-nitro compound
2'-deoxyadenosine triphosphate
2'-deoxyadenosine triphosphate: RN given refers to unlabeled parent cpd		2.06102'-deoxyadenosine 5'-phosphate;
purine 2'-deoxyribonucleoside 5'-triphosphate		Escherichia coli metabolite;
mouse metabolite
normeperidine
normeperidine: RN given refers to parent cpd; structure		210
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		2.0610glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
niguldipine
[no description available]		2.0210diarylmethane
thymidine 5'-triphosphate
thymidine 5'-triphosphate: RN given refers to parent cpd. dTTP : A thymidine phosphate having a triphosphate group at the 5'-position.		2.0610pyrimidine 2'-deoxyribonucleoside 5'-triphosphate;
thymidine phosphate		Escherichia coli metabolite;
mouse metabolite
2'-deoxycytidine 5'-triphosphate
2'-deoxycytidine 5'-triphosphate: RN given refers to unlabeled parent cpd		2.06102'-deoxycytidine phosphate;
pyrimidine 2'-deoxyribonucleoside 5'-triphosphate		Escherichia coli metabolite;
human metabolite;
mouse metabolite
5,6,7,8-tetrahydro-1-naphthol
5,6,7,8-tetrahydro-1-naphthol : 1-naphthol hydrogenated at C-5, -6, -7 and -8.		2.0610tetralins
dmp 323
(4R,5S,6S,7R)-4,7-dibenzyl-5,6-dihydroxy-1,3-bis[4-(hydroxymethyl)benzyl]-1,3-diazepan-2-one : A 1,3-diazepanone ring with two 4-(hydroxymethyl)benzyl groups as substituents at positions N-1 and N-4, two benzyl groups at C-4 and C-7, and two hydroxy groups at C-5 and C-6 respectively.		2.0610diazepanone;
ureas		anti-HIV agent;
metabolite
corynanthine
Corynanthine: A stereoisomer of yohimbine.		2.0210yohimban alkaloid
estrone 3-methyl ether
estrone 3-methyl ether: RN given refers to cpd with unspecified isomeric designation; structure		2.0610
sc 58125
1-((4-methylsulfonyl)phenyl)-3-trifluoromethyl-5-(4-fluorophenyl)pyrazole: a COX-2 inhibitor		2.0610organofluorine compound;
pyrazoles;
sulfone		antineoplastic agent;
cyclooxygenase 2 inhibitor
bmy 45778
BMY 45778: structure given in first source; partial prostacyclin agonist		2.0610bisoxazolepartial prostacyclin agonist
tamsulosin
[no description available]		2.02105-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamidealpha-adrenergic antagonist;
antineoplastic agent
exp7711
EXP7711: to search, use E#P7711(nm); angiotensin II receptor antagonist; structure given in first source		2.0610
bmy 42393
BMY 42393: partial prostacyclin agonist		2.0610
mk 996
MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source		2.0610
rec 15-2739
Rec 15-2739: an alpha-1 antagonist selective for the lower urinary tract; structure given in first source		2.0210
ezetimibe
Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).		2.0610azetidines;
beta-lactam;
organofluorine compound		anticholesteremic drug;
antilipemic drug;
antimetabolite
l 158809
L 158809: RN & structure given in first source; angiotensin receptor antagonist		2.0610
nantenine
nantenine: from Nandina domestica Thundberg; RN given refers to (S)-isomer; structure given in first source		2.0210oxoaporphine alkaloidmetabolite
ar-c239
AR-C239: structure given in first source; alpha(2B)-selective adrenoreceptor		2.0210piperazines
telaprevir
[no description available]		2.0610cyclopentapyrrole;
cyclopropanes;
oligopeptide;
pyrazines		antiviral drug;
hepatitis C protease inhibitor;
peptidomimetic
chaetomellic acid a
chaetomellic acid A: structure given in first source; an inhibitor of farnesyl-protein transferase		2.0610
rs 100329
RS 100329: an alpha(1A)-adrenoceptor antagonist; structure in first source		2.0210piperazines
rs 17053
[no description available]		2.0210indoles
ophiocordin
azepinostatin: isolated from Fusarium merismoides; structure in first source; RN assigned by CAS - 63590-19-2 (ophiocordin; azepinostatin is not the same as ophiocordin)		2.0610
upf 596
UPF 596: structure in first source		2.0610
iloprost
Iloprost: An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of EPOPROSTENOL, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation.. iloprost : A carbobicyclic compound that is prostaglandin I2 in which the endocyclic oxygen is replaced by a methylene group and in which the (1E,3S)-3-hydroxyoct-1-en-1-yl side chain is replaced by a (3R)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl group. A synthetic analogue of prostacyclin, it is used as the trometamol salt (generally by intravenous infusion) for the treatment of peripheral vascular disease and pulmonary hypertension.		2.0610carbobicyclic compound;
monocarboxylic acid;
secondary alcohol		platelet aggregation inhibitor;
vasodilator agent
silodosin
silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source		2.0210indolecarboxamide
n-(3-(cyclohexylidene-(1h-imidazol-4-ylmethyl))phenyl)ethanesulfonamide
[no description available]		2.0210
ro 70-0004
[no description available]		2.0210
way 133537
[no description available]		2.0610
dpc 423
[no description available]		2.0610
deoxyguanosine triphosphate
[no description available]		2.0610deoxyguanosine phosphate;
guanyl deoxyribonucleotide;
purine 2'-deoxyribonucleoside 5'-triphosphate		Arabidopsis thaliana metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
guanosine diphosphate
Guanosine Diphosphate: A guanine nucleotide containing two phosphate groups esterified to the sugar moiety.		2.0610guanosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate		Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
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