Page last updated: 2024-12-11

f 13640

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

Description

befiradol: a selective serotonin 5-HT1A receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9865384
CHEMBL ID45305
SCHEMBL ID678174
MeSH IDM0449474

Synonyms (33)

Synonym
nlx-112
CHEMBL45305 ,
befiradol
f-13640
f13640 ,
L001676
((3-chloro-4-fluoro-phenyl)-(4-fluoro-4-((5-methyl-pyridin-2-ylmethyl)-amino)-methyl)piperidin-1-yl)-methadone
f 13640
bdbm50328639
(3-chloro-4-fluorophenyl)(4-fluoro-4-(((5-methylpyridin-2-yl)methylamino)methyl)piperidin-1-yl)methanone
(3-chloro-4-fluoro-phenyl)-(4-fluoro-4-{[(5-methyl-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl)-methanone
befiradol [inn]
208110-64-9
rat9oha1yh ,
unii-rat9oha1yh
[3h]nlx-112
gtpl3925
(3-chloro-4-fluorophenyl)-[4-fluoro-4-[[(5-methylpyridin-2-yl)methylamino]methyl]piperidin-1-yl]methanone
[3h]f13640
SCHEMBL678174
befiradol [who-dd]
(3-chloro-4-fluorophenyl)(4-fluoro-4-((((5-methylpyridin-2-yl)methyl)amino)methyl)piperidin-1-yl)methanone
AKOS032954037
CS-0003559
HY-14785
Q4880242
nlx-112 hydrochloride
DTXSID90943058
f-13640; f13640; f 13640; nlx-112; nlx112; nlx 112
BCP31302
nlx-112; f13640
befiradol (free base)
GLXC-15037

Research Excerpts

Overview

F 13640 is a newly discovered high-efficacy 5-HT(1A) receptor agonist. It produces exceptional analgesia in animal models of tonic and chronic, nociceptive and neuropathic pains.

ExcerptReferenceRelevance
"F 13640 is a newly discovered high-efficacy 5-HT(1A) receptor agonist that produces exceptional analgesia in animal models of tonic and chronic, nociceptive and neuropathic pains by novel molecular and neuroadaptive mechanisms. "( The novel analgesic, F 13640, produces intra- and postoperative analgesia in a rat model of surgical pain.
Bardin, L; Colpaert, FC; Degryse, AD; Gomez de Segura, IA; Kiss, I, 2005
)
2.09
"F 13640 is a recently discovered high-efficacy 5-HT1A receptor agonist that has demonstrated robust anti-allodynic efficacy in a rat model of trigeminal neuropathic pain upon acute and continuous administration. "( Effects of the combined continuous administration of morphine and the high-efficacy 5-HT1A agonist, F 13640 in a rat model of trigeminal neuropathic pain.
Adriaensen, HF; Colpaert, FC; Deseure, KR, 2004
)
1.98

Bioavailability

ExcerptReferenceRelevance
"The aim of this work was to improve the oral bioavailability of a recently discovered, novel structural class of 5-HT1A receptor agonists: aryl-{[4-(6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1 -yl-metha none."( Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
AssiƩ, MB; Bonnaud, B; Cosi, C; Funes, P; Jubault, N; Kleven, M; Koek, W; Vacher, B, 1999
)
0.3

Dosage Studied

ExcerptRelevanceReference
" Dose-response studies indicated that c-Fos protein expression was induced at doses (0."( The novel analgesic and high-efficacy 5-HT1A receptor agonist, F 13640 induces c-Fos protein expression in spinal cord dorsal horn neurons.
Besson, JM; Buritova, J; Colpaert, F; Tarayre, JP, 2003
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.00100.00010.532610.0000AID1854986
D(2) dopamine receptorHomo sapiens (human)Ki30.50000.00000.651810.0000AID517902; AID517903
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.00090.00010.739610.0000AID4413
D(4) dopamine receptorHomo sapiens (human)Ki2.00000.00000.436210.0000AID517905
D(3) dopamine receptorHomo sapiens (human)Ki10.00000.00000.602010.0000AID517904
Cannabinoid receptor 2Mus musculus (house mouse)Ki26.00000.00020.07970.7943AID517901
5-hydroxytryptamine receptor 2ASus scrofa (pig)Ki23.00000.03000.42700.9000AID517900
D(1A) dopamine receptorSus scrofa (pig)Ki26.00000.00051.22238.8000AID517901
[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)
Cytochrome P450 1A1Rattus norvegicus (Norway rat)EC50 (µMol)0.02570.00152.205710.0000AID3907
5-hydroxytryptamine receptor 1AHomo sapiens (human)EC50 (µMol)0.02460.00010.25718.0000AID298093; AID3907
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (133)

Processvia Protein(s)Taxonomy
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)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
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)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
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)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID298095Induction of forepaw treading in orally dosed rat after 60 mins2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID517897Displacement of [3H]WAY-100635 from 5-HT1A receptor in pig cortex membranes2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID298101Half life in human plasma2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID517902Displacement of [3H]Spiperone from human dopamine D2 long receptor2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID298100Bioavailability in dog2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID176228Effective intraperitoneal dose in vivo in rat after 15 mins to induce lower lip retraction1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
AID298103Lipophilicity, log D of the compound2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID517899Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in pig cortex membranes2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID517906Displacement of [3H]Prazosin from adrenergic alpha1 receptor in pig cortex membranes2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID298093Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID4413Binding affinity towards 5-hydroxytryptamine 1A receptor in rat cortex using [3H]8-OH-DPAT as a radioligand1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
AID298099Bioavailability in rat2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID517907Displacement of [3H]Prazosin from adrenergic alpha2 receptor in pig cortex membranes2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID517905Displacement of [3H]Spiperone from human dopamine D4.4 receptor2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID517904Displacement of [3H]Spiperone from human dopamine D3 receptor2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID298102Dissociation constant, pKa of the compound2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID176232Induction of lower lip retraction in rat 60 min after administration, effective peroral dose determined in vivo1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
AID517900Displacement of [3H]Ketanserin from 5-HT2 receptor in pig cortex membranes2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID298098Antidepressant like activity in orally dosed rat after 60 mins by forced swimming test2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID298092Binding affinity to 5HT1A receptor in rat cortex membrane2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID517901Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID298094Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTP-gamma-S binding relative to 5-hydroxytryptamine2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID298097Ratio of ED50 for forepaw treading induction in rat to ED50 for flat body posture induction in rat2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID1854986Binding affinity to 5-HT1A 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.
AID298096Induction of flat body posture in orally dosed rat as after 60 mins2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
AID3907In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
AID517903Displacement of [3H]Spiperone from human dopamine D2 short receptor2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)2010Naunyn-Schmiedeberg's archives of pharmacology, Oct, Volume: 382, Issue:4
[(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (42)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (2.38)18.2507
2000's18 (42.86)29.6817
2010's11 (26.19)24.3611
2020's12 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.21

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 Index12.21 (24.57)
Research Supply Index3.76 (2.92)
Research Growth Index5.98 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (4.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other40 (95.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]