Page last updated: 2024-12-11

s 21007

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Cross-References

ID SourceID
PubMed CID9863146
CHEMBL ID54720
SCHEMBL ID7298411
MeSH IDM0276435

Synonyms (5)

Synonym
CHEMBL54720 ,
bdbm50407786
SCHEMBL7298411
s-21007
8-(4-benzylpiperazin-1-yl)-3-thia-1,7-diazatricyclo[7.3.0.02,6]dodeca-2(6),4,7,9,11-pentaene
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 3EHomo sapiens (human)IC50 (µMol)0.00140.00042.08059.0000AID6317; AID6355
5-hydroxytryptamine receptor 3EHomo sapiens (human)Ki0.00100.00100.88359.9000AID1855131
5-hydroxytryptamine receptor 3BHomo sapiens (human)IC50 (µMol)0.00140.00041.95059.0000AID6317; AID6355
5-hydroxytryptamine receptor 3BHomo sapiens (human)Ki0.00100.00100.87119.9000AID1855131
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC50 (µMol)0.39810.00010.666410.0000AID3458; AID3459
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)1.86210.00011.03029.0000AID5683; AID5685
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)1.02330.00051.48357.8000AID4298; AID4299
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC50 (µMol)0.00140.00021.13514.6000AID6357
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC50 (µMol)0.00140.00011.07899.0000AID416527; AID6317; AID6355
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.00100.00000.74119.9000AID1855131
5-hydroxytryptamine receptor 1DSus scrofa (pig)IC50 (µMol)14.12540.00030.64963.7153AID4851; AID4852
Adenylate cyclase type 5Rattus norvegicus (Norway rat)IC50 (µMol)0.39810.04680.88292.3000AID3459
5-hydroxytryptamine receptor 3DHomo sapiens (human)IC50 (µMol)0.00140.00042.08059.0000AID6317; AID6355
5-hydroxytryptamine receptor 3DHomo sapiens (human)Ki0.00100.00100.88359.9000AID1855131
5-hydroxytryptamine receptor 2ABos taurus (cattle)IC50 (µMol)4.36520.00902.71404.3652AID5153; AID5154
5-hydroxytryptamine receptor 3CHomo sapiens (human)IC50 (µMol)0.00140.00042.08059.0000AID6317; AID6355
5-hydroxytryptamine receptor 3CHomo sapiens (human)Ki0.00100.00100.88359.9000AID1855131
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC50 (µMol)0.00140.00041.17424.6000AID6357
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (40)

Processvia Protein(s)Taxonomy
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3EHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3EHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3EHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3BHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3BHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3BHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3DHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3DHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3DHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3DHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2ABos taurus (cattle)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2ABos taurus (cattle)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2ABos taurus (cattle)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2ABos taurus (cattle)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3CHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3CHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3CHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3EHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3EHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3BHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3DHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3DHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2ABos taurus (cattle)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2ABos taurus (cattle)
identical protein binding5-hydroxytryptamine receptor 2ABos taurus (cattle)
serotonin binding5-hydroxytryptamine receptor 2ABos taurus (cattle)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2ABos taurus (cattle)
protein binding5-hydroxytryptamine receptor 3CHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3CHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3CHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3EHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3EHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3EHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3BHomo sapiens (human)
cell surface5-hydroxytryptamine receptor 3BHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3DHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3DHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3DHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2ABos taurus (cattle)
axon5-hydroxytryptamine receptor 2ABos taurus (cattle)
cytoplasmic vesicle5-hydroxytryptamine receptor 2ABos taurus (cattle)
presynapse5-hydroxytryptamine receptor 2ABos taurus (cattle)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2ABos taurus (cattle)
plasma membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3CHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3CHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (64)

Assay IDTitleYearJournalArticle
AID35781Inhibitory activity against Alpha-2 adrenergic receptor using [3H]RX-821002 at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID6050Antagonistic activity of compound towards 5-hydroxytryptamine 3 receptor in Von Bezold-Jarisch reflex in rats at 60 (ug/kg), evaluated as percent inhibition of bradycardia1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID140948Inhibitory activity against Muscarinic acetylcholine receptor M2 using [3H]NMS at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID39487Inhibitory activity against Angiotensin II receptor using [3H]Angiotensin II at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID93083Displacement of [3H]insulin from Insulin receptor at 10e-5 M1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID5683Binding affinity against 5-Hydroxytryptamine 2C Receptor was measured using [3H]N-methyl-mesulergine as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID152092Inhibitory activity against Opioid receptor mu 1 using [3H]DAMGO at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID50528Inhibitory activity against Cholecystokinin type A receptor using [3H]L-364718 at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID4298Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID36320Inhibitory activity against Alpha-1 adrenergic receptor using [3H]-prazosin at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID148738Inhibitory activity against Opioid receptor kappa 1 using [3H]U-69593 at 10e-7 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID71406Inhibitory activity against Gamma-aminobutyric acid type B receptor using [3H]GABA at 10e-5 M1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID64131In vitro displacement from Dopamine receptor D21996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID5153Binding affinity against 5-hydroxytryptamine 2A receptor was measured using [3H]ketanserin as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID6317Binding affinity towards 5-hydroxytryptamine 3 receptor2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
First tricyclic oximino derivatives as 5-HT3 ligands.
AID161278Inhibition of [3H]apamin binding to Potassium channel at 10e-5 M1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID148737Inhibitory activity against Opioid receptor kappa 1 using [3H]U-69593 at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID6046Agonistic activity of compound towards 5-hydroxytryptamine 3 receptor in Von Bezold-Jarisch Reflex in rats at 60 (ug/kg), evaluated as change in heart rate1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID215074Inhibitory activity against TNF using [125]TNF at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID6357Binding affinity towards 5-hydroxytryptamine 3 receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID3459Binding affinity for 5-hydroxytryptamine 1A receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID147814Inhibitory activity against Opioid receptor delta 1 using [3H]Cl-phe-DPDPE at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID141746Inhibitory activity against Muscarinic acetylcholine receptor M3 using [3H]NMS at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID51619Inhibitory activity against Cholecystokinin type B receptor using [3H]CCK-8 at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID42991Inhibitory activity against Bradykinin receptor using [3H]bradykinin at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID64132In vitro displacement from Dopamine receptor D21996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID4852Binding affinity for 5-hydroxytryptamine 1D receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID41498Inhibitory activity against Beta-2 adrenergic receptor using [3H]CGP-12177 at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID4299Binding affinity for 5-hydroxytryptamine 1B receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID102659Inhibitory activity against Leukotriene B4 receptor using [3H]- LTB4 at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID40992Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine receptor at 10e-5 M1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID216931Inhibitory activity against VIP using [125]VIP at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID61836Inhibitory activity against Dopamine receptor D1 using [3H]SCH-23,390 at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID212442Inhibitory activity against Thromboxane A2 using [3H]SG-29548 at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID146598Inhibitory activity against Neuropeptide Y receptor type 1 using [3H]-NPY at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID5154Binding affinity towards 5-hydroxytryptamine 2A receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID3458Binding affinity against 5-hydroxytryptamine 1A receptor was measured using [3H]8-OH-DPAT as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID163313Inhibitory activity against Quisqualate receptor using [3H]AMPA at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID40993Inhibition of [3H]PK11195 binding to peripheral Benzodiazepine receptor at 10e-5 M1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID72450Inhibitory activity against Gamma-aminobutyric acid A (GABA-A) receptor using [3H]-muscimol at 10e-5 M1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID205294Inhibition of [3H]batrachotoxin binding to sodium channel at 10e-7 M1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID416527Displacement of [3H]granisetron form 5HT3 receptor in hybrid NG180-15 cells2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.
AID143461Inhibitory activity against NMDA using [3H]CGS-19,755 at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID143660In vitro effective concentration against [14C]guanidinium uptake into NG 108-15 cells1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID4851Binding affinity against 5-hydroxytryptamine 1D receptor was measured using [3H]5-HT as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID1855131Binding affinity to 5-HT3 receptor (unknown origin) assessed as inhibition constant2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID40547Inhibitory activity against Beta-1 adrenergic receptor using [3H]CGP-12177 at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID143659In Vitro 5-HT3 agonist activity on the [14C]guanidinium accumulation in NG 108-15 cells.1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID55236Inhibitory activity against Cysteinyl leukotriene D4 receptor using [3H]- LTD4 at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID5685Binding affinity towards 5-hydroxytryptamine 2C receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID416526Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum membrane2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.
AID205293Inhibition of [3H]batrachotoxin binding to sodium channel at 10e-5 M1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID183866In Vivo 5-HT3 agonist activity in the Von Bezold-Jarisch reflex decrease in heart rate in rats at 120 (ug/kg) dose.1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID141975Inhibitory activity against Muscarinic acetylcholine receptor M1 using [3H]pirenzepine at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID30477Inhibitory activity against Adenosine A1 receptor using [3H]DPCPX at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID210545Inhibitory activity against TRH using [3H]TRH at 10e-5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID91877Inhibitory activity against Interleukin 1d using [3H]IL-1-alpha at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID157595Inhibitory activity against Phencyclidine receptor using [3H]-TCP at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID183870In Vivo 5-HT3 antagonist activity in the Von Bezold-Jarisch reflex in rats at intravenous dose of 60 (ug/kg)1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID6355Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID91468Inhibitory activity against Ionotropic glutamate receptor kainate using [3H]- Kainate at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID33914Inhibitory activity against Adenosine A2 receptor using [3H]CGS-21680 at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID6045Agonistic activity of compound towards 5-hydroxytryptamine 3 receptor in Von Bezold-Jarisch Reflex in rats at 120 (ug/kg), evaluated as change in heart rate1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID158052Inhibitory activity against Platelet activating factor receptor using [3H]PAF at 10e5 (M)1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
[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's2 (40.00)29.6817
2010's0 (0.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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 Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

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]