Page last updated: 2024-12-11

1-(3-(5-(1,2,4-triazol-4-yl)-1h-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazine

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

Description

The compound you described, **1-(3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazine**, is a complex organic molecule with a long and descriptive chemical name. Its importance lies in its potential as a **research tool** for understanding and treating certain medical conditions, particularly in the field of **neuroscience**.

Here's a breakdown of the compound's features and why it's interesting to researchers:

* **Structure:** The molecule is composed of several distinct components:
* **Indole ring:** A core structure commonly found in biologically active molecules.
* **Triazole ring:** This heterocyclic ring often contributes to drug-like properties.
* **Piperazine ring:** A common component of many pharmaceutical compounds, often associated with antihistamine or antipsychotic activity.
* **3-Fluorophenyl group:** This aromatic group might influence the molecule's interaction with biological targets.
* **Potential Applications:** The combination of these structural features suggests that the compound could have activity in the central nervous system. Research is ongoing to understand its potential therapeutic effects, which could include:
* **Anti-inflammatory properties:** The molecule might interact with certain receptors or enzymes involved in inflammation processes.
* **Neuroprotective effects:** It could potentially protect neurons from damage caused by various factors.
* **Modulation of neurotransmitter activity:** The compound might influence the activity of neurotransmitters like serotonin or dopamine, which are implicated in various brain functions and disorders.

**Importance for Research:**

The complex structure and potential biological activity of this compound make it a valuable tool for:

* **Drug Discovery:** Scientists can study the compound's interactions with various biological targets and explore its potential for developing new drugs.
* **Understanding Brain Function:** By studying the molecule's effects on the nervous system, researchers can gain insights into the mechanisms underlying brain function and dysfunction.
* **Developing Therapies:** If the compound demonstrates therapeutic potential, it could pave the way for new treatments for conditions like neurodegenerative diseases, inflammatory disorders, or psychiatric illnesses.

**It's important to remember:**

* **This is a research compound:** It hasn't been approved for any medical use yet.
* **Further research is needed:** Extensive studies are required to fully understand the compound's safety, efficacy, and potential therapeutic applications.

While the specific effects and potential benefits of this compound are still being investigated, it represents a promising avenue for exploration in the field of drug discovery and neuroscience research.

1-(3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazine: an h5-HT(1D) receptor agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6426760
CHEMBL ID292779
SCHEMBL ID7477108
MeSH IDM0301913

Synonyms (19)

Synonym
gtpl114
l-775,606
1-(3-(5-(1,2,4-triazol-4-yl)-1h-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazine
L016148
l-775606
CHEMBL292779 ,
3-[3-[4-[2-(3-fluorophenyl)ethyl]piperazin-1-yl]propyl]-5-(1,2,4-triazol-4-yl)-1h-indole
3-[3-[4-[2-(3-fluorophenyl)ethyl]-1-piperazinyl]propyl]-5-(4h-1,2,4-triazol-4-yl)-1h-indole
bdbm50060437
3-(3-{4-[2-(3-fluoro-phenyl)-ethyl]-piperazin-1-yl}-propyl)-5-[1,2,4]triazol-4-yl-1h-indole
SCHEMBL7477108
188400-51-3
l 775606
1h-indole, 3-(3-(4-(2-(3-fluorophenyl)ethyl)-1-piperazinyl)propyl)-5-(4h-1,2,4-triazol-4-yl)-
1-(3-[5-{1,2,4-triazol-4-yl}-1h-indol-3-yl]propyl)-4-(2-{3-fluorophenyl}ethyl)piperazine
ZUTQCPBDRJBADG-UHFFFAOYSA-N ,
1-[3-(5-(1,2,4-triazol-4-yl)-1h-indol-3-yl)propyl]-4-[2-(3-fluorophenyl)ethyl]piperazine
Q27078430
AKOS040748709

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"It has previously been reported that a 3-(3-(piperazin-1-yl)propyl)indole series of 5-HT1D receptor ligands have pharmacokinetic advantages over the corresponding 3-(3-(piperidin-1-yl)propyl)indole series and that the reduced pKa of the piperazines compared to the piperidines may be one possible explanation for these differences."( Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
Beer, MS; Broughton, HB; Castro, JL; Cheng, SK; Collins, I; Goodacre, SC; Heald, A; Locker, KL; MacLeod, AM; Morrison, D; Moyes, CR; O'Connor, D; Pike, A; Rowley, M; Russell, MG; Sohal, B; Stanton, JA; Thomas, S; van Niel, MB; Verrier, H; Watt, AP, 1999
)
0.3

Bioavailability

ExcerptReferenceRelevance
" The optimum compound was 1-(3-[5-(1,2, 4-triazol-4-yl)-1H-indol-3-yl]propyl)-4-(2-(3-fluorophenyl)ethyl)p ipe razine (7f) which has excellent selectivity for h5-HT1D receptors over other 5-HT receptor subtypes and good oral bioavailability in three species."( 3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
Beer, MS; Chambers, MS; Goodacre, S; Hobbs, SC; Hunt, P; Jelley, RA; MacLeod, AM; Matassa, VG; Rathbone, D; Reeve, AJ; Stanton, JA; Sternfeld, F; Street, LJ; Watt, AP, 1999
)
0.3
" The incorporation of fluorine was found to significantly reduce the pKa of the compounds, and this reduction of basicity was shown to have a dramatic, beneficial influence on oral absorption, although the effect on oral bioavailability could not always be accurately predicted."( Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
Beer, MS; Broughton, HB; Castro, JL; Cheng, SK; Collins, I; Goodacre, SC; Heald, A; Locker, KL; MacLeod, AM; Morrison, D; Moyes, CR; O'Connor, D; Pike, A; Rowley, M; Russell, MG; Sohal, B; Stanton, JA; Thomas, S; van Niel, MB; Verrier, H; Watt, AP, 1999
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (17)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 3EHomo sapiens (human)IC50 (µMol)9.00000.00042.08059.0000AID5956
5-hydroxytryptamine receptor 3BHomo sapiens (human)IC50 (µMol)9.00000.00041.95059.0000AID5956
5-hydroxytryptamine receptor 1DHomo sapiens (human)IC50 (µMol)0.00060.00050.28702.4000AID404703; AID4595; AID4597; AID4602; AID4603; AID4604
5-hydroxytryptamine receptor 1BHomo sapiens (human)IC50 (µMol)0.07350.00050.39756.5000AID4510; AID4512; AID4516; AID4517
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.37000.00010.88018.8500AID5366
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)9.00000.00011.03029.0000AID5956
5-hydroxytryptamine receptor 1EHomo sapiens (human)IC50 (µMol)10.00005.50005.50005.5000AID4970
5-hydroxytryptamine receptor 1FHomo sapiens (human)IC50 (µMol)3.80000.08781.94393.8000AID4977
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC50 (µMol)9.25000.00011.07899.0000AID5956; AID6358
5-hydroxytryptamine receptor 1BOryctolagus cuniculus (rabbit)IC50 (µMol)0.00060.00060.09430.1880AID404703
5-hydroxytryptamine receptor 1AMus musculus (house mouse)IC50 (µMol)0.05500.00210.35812.0000AID4460
5-hydroxytryptamine receptor 3DHomo sapiens (human)IC50 (µMol)9.00000.00042.08059.0000AID5956
5-hydroxytryptamine receptor 3CHomo sapiens (human)IC50 (µMol)9.00000.00042.08059.0000AID5956
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Rattus norvegicus (Norway rat)EC50 (µMol)0.00100.00100.00100.0010AID4579
cAMP-specific 3',5'-cyclic phosphodiesterase 4CRattus norvegicus (Norway rat)EC50 (µMol)0.00100.00100.00100.0010AID4579
cAMP-specific 3',5'-cyclic phosphodiesterase 4BRattus norvegicus (Norway rat)EC50 (µMol)0.00100.00100.00100.0010AID4579
5-hydroxytryptamine receptor 1DHomo sapiens (human)EC50 (µMol)0.00110.00080.00600.0160AID45060; AID4574; AID4579; AID4582
5-hydroxytryptamine receptor 1BHomo sapiens (human)EC50 (µMol)0.43000.01160.13880.4300AID4499
cAMP-specific 3',5'-cyclic phosphodiesterase 4ARattus norvegicus (Norway rat)EC50 (µMol)0.00100.00100.00100.0010AID4579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (77)

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)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1DHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of locomotion5-hydroxytryptamine receptor 1DHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1DHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1DHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of serotonin secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, GABAergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to cocaine5-hydroxytryptamine receptor 1BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1BHomo sapiens (human)
drinking behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to ethanol5-hydroxytryptamine receptor 1BHomo sapiens (human)
bone remodeling5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to mineralocorticoid5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to alkaloid5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to xenobiotic stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration5-hydroxytryptamine receptor 1BHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of synaptic vesicle exocytosis5-hydroxytryptamine receptor 1BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1BHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo 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)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1EHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1EHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1EHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1EHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1EHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1FHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1FHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1FHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1FHomo 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)
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 (16)

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 1DHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo 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)
G protein-coupled receptor activity5-hydroxytryptamine receptor 1EHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1EHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1EHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1EHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1EHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1FHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1FHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1FHomo 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)
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 (22)

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 1DHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1DHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1DHomo sapiens (human)
endoplasmic reticulum5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
calyx of Held5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonergic synapse5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 1BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo 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 1EHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1EHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1FHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1FHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1FHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1FHomo 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)
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 (35)

Assay IDTitleYearJournalArticle
AID4574Compound was evaluated for the stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor.1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID404707Selectivity for human 5HT1D receptor over human 5HT1B receptor2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
AID18396Oral bioavailability in rat1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID4597Compound was evaluated for the affinity at 5-hydroxytryptamine 1D receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID234716Relative efficacy in stimulation of [35S]GTP-gamma-S, binding in CHO cells compared to 5-HT1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID4602Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.
AID4582Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID6358Compound was evaluated for the affinity at 5-hydroxytryptamine 3 receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID404703Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1D receptor expressed in CHOK1 cells by liquid scintillation counting2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
AID4590Percent efficacy relative to 5-HT treatment of CHO cells expressing 5-HT 1d receptor1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.
AID4579Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the human 5-hydroxytryptamine 1D receptor.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID4587Efficacy was evaluated relative to human 5-hydroxytryptamine 1D receptor using [35S]GTP-gamma-S, as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID4505Efficacy of compound was evaluated relative to human 5-hydroxytryptamine 1B receptor using [35S]GTP-gamma-S, as radioligand1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID4638Selectivity towards 5-HT1D and to that of 5-HT1B in CHO cells1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID4510Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID5956Compound was evaluated for the affinity at 5-hydroxytryptamine 2C receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID4970Compound was evaluated for the affinity at 5-hydroxytryptamine 1E receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID233219Relative binding to serotonin 5-HT 1B and 5-HT 1D receptors1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID4604Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1D receptor expressed in CHO cells1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID4595Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID45060Agonist induced [35S]GTP-gamma-S, binding in CHO cells expressing 5-HT 1d receptor1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.
AID4603Displacement of [3H]5-HT binding to the cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID4588Maximum stimulation of [35S]GTP-gamma-S, binding expressed relative to the maximal effect produced by 5-hydroxytryptamine 1D receptor.1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID4516Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID4977Compound was evaluated for the affinity at 5-hydroxytryptamine 1F receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID5366Compound was evaluated for the affinity at 5-hydroxytryptamine 2A receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID4512Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID233043Relative binding to serotonin 5-HT1D and 5-HT1B receptors1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.
AID4460Compound was evaluated for the affinity at 5-hydroxytryptamine 1A receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID26361pKa value was determined1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID234526Selectivity of compound towards human 5-HT1D receptor over human 5-HT1B receptor1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID4517Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID4499Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID16487Rate of clearance in rat was determined1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)2000Molecular pharmacology, Nov, Volume: 58, Issue:5
Inverse agonism and constitutive activity as functional correlates of serotonin h5-HT(1B) receptor/G-protein stoichiometry.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (36.36)18.2507
2000's6 (54.55)29.6817
2010's0 (0.00)24.3611
2020's1 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]