Page last updated: 2024-11-11

ssr180711

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Description

SSR180711: a selective alpha7 acetylcholine nicotinic receptor (n-AChRs) partial agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9797360
CHEMBL ID559478
SCHEMBL ID1427769
MeSH IDM0506352

Synonyms (28)

Synonym
ssr-180711
j2.849.107g ,
ssr-180,711
ssr180711c
ssr180711
CHEMBL559478 ,
(4-bromophenyl) 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate
bdbm50296742
1,4-diazabicyclo[3.2.2]nonane-(4-bromo)-phenyl carbamate
NCGC00247961-01
tox21_300241
cas-298198-52-4
dtxsid2047359 ,
dtxcid0027359
NCGC00254110-01
298198-52-4
1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid, 4-bromophenyl ester
1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester
4-bromophenyl 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate
RXLOZRCLQMJJLC-UHFFFAOYSA-N
SCHEMBL1427769
1,4-diaza-bicyclo[3.2.2]nonane-4-carboxylic acid 4-bromo-phenyl ester
unii-qf4p1u1666
1,4-diazabicyclo(3.2.2)nonane-4-carboxylic acid, 4-bromophenyl ester
QF4P1U1666 ,
4-bromophenyl 1,4-diazabicyclo(3.2.2)nonane-4-carboxylate
1,4-diazabicyclo(3,2,2)nonane-4-carboxylic acid 4-bromophenyl ester
Q27287229

Research Excerpts

Overview

SSR180711 is a recently described α7 nAChR agonist. It has shown antidepressant-like activity in the rat forced swim test.

ExcerptReferenceRelevance
"SSR180711 is a recently described α7 nAChR agonist that has shown antidepressant-like activity in the rat forced swim test."( Combined α7 nicotinic acetylcholine receptor agonism and partial serotonin transporter inhibition produce antidepressant-like effects in the mouse forced swim and tail suspension tests: a comparison of SSR180711 and PNU-282987.
Andreasen, JT; Nielsen, EØ; Redrobe, JP, 2012
)
1.29

Actions

ExcerptReferenceRelevance
"SSR180711 displays high affinity for rat and human alpha7 n-AChRs (K(i) of 22+/-4 and 14+/-1 nM, respectively)."( SSR180711, a novel selective alpha7 nicotinic receptor partial agonist: (1) binding and functional profile.
Avenet, P; Bergis, OE; Besnard, F; Biton, B; Bohme, GA; Chesney, F; Coste, A; Curet, O; Debono, MW; Françon, D; Galli, F; George, P; Godet, D; Graham, D; Granger, P; Griebel, G; Gueudet, C; Jegham, S; Lanneau, C; Léonardon, J; Lochead, AW; Nedelec, A; Oblin, A; Oury-Donat, F; Rouquier, L; Santamaria, R; Santucci, V; Scatton, B; Sgard, F; Souilhac, J; Steinberg, R; Vigé, X; Voltz, C, 2007
)
2.5
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency27.30600.000221.22318,912.5098AID743042
estrogen nuclear receptor alphaHomo sapiens (human)Potency32.17350.000229.305416,493.5996AID1259244; AID1259248; AID743080; AID743091
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency4.85580.001723.839378.1014AID743083
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency63.70930.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency30.63790.000627.21521,122.0200AID743202
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency48.55770.001557.789015,848.9004AID1259244
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency48.55770.001551.739315,848.9004AID1259244
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)IC50 (µMol)6.48000.00181.31326.5000AID431144
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)Ki0.01400.00221.742710.0000AID580944; AID690414; AID746041
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC50 (µMol)3.16000.00011.07899.0000AID431148
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)Ki0.03000.00000.73078.0000AID431140; AID690426
[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)
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)EC50 (µMol)3.23330.12802.80188.9000AID580948; AID690429; AID690430
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (50)

Processvia Protein(s)Taxonomy
monoatomic ion transportNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of smooth muscle contractionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
nervous system developmentNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
locomotory behaviorNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of acetylcholine secretion, neurotransmissionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of membrane potentialNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of dendrite morphogenesisNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
synaptic transmission involved in micturitionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
response to acetylcholineNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
negative regulation of tumor necrosis factor productionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to hypoxiaNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of protein phosphorylationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium ion transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
intracellular calcium ion homeostasisNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
learning or memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
short-term memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of cell population proliferationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
negative regulation of tumor necrosis factor productionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of MAPK cascadeNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of angiogenesisNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synapse organizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
cognitionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
sensory processingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of protein metabolic processNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
dendritic spine organizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
modulation of excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
dendrite arborizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of long-term synaptic potentiationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of amyloid-beta formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
negative regulation of amyloid-beta formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of amyloid precursor protein catabolic processNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to amyloid-betaNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to acetylcholineNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of amyloid fibril formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of CoA-transferase activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of membrane potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit alpha-7Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
protein bindingNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
amyloid-beta bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
toxic substance bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
chloride channel regulator activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein homodimerization activityNeuronal acetylcholine receptor subunit alpha-7Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
endoplasmic reticulumNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
Golgi apparatusNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
postsynaptic densityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
nuclear speckNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
dendriteNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
neuronal cell bodyNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membrane raftNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membrane raftNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
postsynapseNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-7Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (125)

Assay IDTitleYearJournalArticle
AID746111Biodistribution in CD1 mouse adrenal at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746120Biodistribution in CD1 mouse small intestine at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID580948Partial agonist activity at human alpha7 nAChR expressed in Xenopus oocyte assessed as evoked ACh-induced current by voltage clamp method2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Exploring α7-Nicotinic Receptor Ligand Diversity by Scaffold Enumeration from the Chemical Universe Database GDB.
AID746115Biodistribution in CD1 mouse bladder at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746080Biodistribution in CD1 mouse liver at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746081Biodistribution in CD1 mouse small intestine at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746113Biodistribution in CD1 mouse thymus at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746100Biodistribution in CD1 mouse large intestine at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746122Biodistribution in CD1 mouse lung at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746156Biodistribution in CD1 mouse liver at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746162Biodistribution in CD1 mouse heart at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746088Plasma concentration in CD1 mouse at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746091Biodistribution in CD1 mouse skin at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746089Biodistribution in CD1 mouse muscle at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746116Biodistribution in CD1 mouse urine at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746135Biodistribution in CD1 mouse kidney at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746123Biodistribution in CD1 mouse heart at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431142Displacement of L-[3H]Nicotine from alpha4beta2 nAChR in rat brain homogenate by rapid filtration method2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID431141Agonist activity at rat alpha7 nAChR expressed in Xenopus oocytes at 32 uM by two-electrode voltage clamp technique relative to nicotine2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746138Biodistribution in CD1 mouse large intestine at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746073Biodistribution in CD1 mouse thymus at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID690414Binding affinity to human alpha7 nAchR2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID746097Biodistribution in CD1 mouse urine at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746074Biodistribution in CD1 mouse pancreas at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746104Biodistribution in CD1 mouse heart at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746119Biodistribution in CD1 mouse large intestine at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID1460122In vivo agonist activity at alpha7 nAChR in Wistar rat assessed as induction of c-fos gene expression in medial prefrontal cortex at 10 mg/kg, sc after 2 hrs by qPCR method relative to control2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Development of spiroguanidine-derived α7 neuronal nicotinic receptor partial agonists.
AID746147Biodistribution in CD1 mouse femur at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746076Biodistribution in CD1 mouse bladder at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746114Biodistribution in CD1 mouse spleen at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746127Biodistribution in CD1 mouse femur at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746132Biodistribution in CD1 mouse thymus at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746105Biodistribution in CD1 mouse brain at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431153Drug concentration in Sprague-Dawley rat CSF at 5 mg/kg, sc after 1 hr2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID1336491Reversal of MK-801 induced cognitive deficits in Sprague-Dawley rat assessed as reduction in number of trials to reach set shift at 10 mg/kg, po administered immediately prior to MK-801
AID690429Partial agonist activity at human alpha7 nAChR expressed in Xenopus oocytes relative to acetylcholine2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID746077Biodistribution in CD1 mouse urine at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746106Plasma concentration in CD1 mouse at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746163Plasma concentration in CD1 mouse at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431140Displacement of [125I]BTX from rat alpha7 nAChR expressed in rat GH4C1 cells2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746072Biodistribution in CD1 mouse adrenal at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746144Plasma concentration in CD1 mouse at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746131Biodistribution in CD1 mouse pancreas at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746164Biodistribution in CD1 mouse blood at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746099Biodistribution in CD1 mouse liver at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746140Biodistribution in CD1 mouse stomach at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746107Biodistribution in CD1 mouse blood at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID1460128Effect on beta2-microglobulin gene expression in Wistar rat medial prefrontal cortex at 10 mg/kg, sc after 2 hrs by qPCR method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Development of spiroguanidine-derived α7 neuronal nicotinic receptor partial agonists.
AID746130Biodistribution in CD1 mouse adrenal at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID675874Partial agonist activity at human alpha7 nAChR expressed in Xenopus oocyte assessed as stimulation of ACh-induced current after 30 secs by electrophysiological assay2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Synthesis and nicotinic receptor activity of chemical space analogues of N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester (SSR180711).
AID746041Displacement of [3H]alpha-BTX from human alpha7 nAChR expressed in rat GH4C1 cells after 60 mins2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746141Biodistribution in CD1 mouse lung at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746133Biodistribution in CD1 mouse spleen at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746137Biodistribution in CD1 mouse liver at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746134Biodistribution in CD1 mouse bladder at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746136Biodistribution in CD1 mouse urine at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746158Biodistribution in CD1 mouse stomach at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746148Biodistribution in CD1 mouse skin at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746090Biodistribution in CD1 mouse femur at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431147Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells at 10 uM2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746117Biodistribution in CD1 mouse kidney at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID580944Binding affinity to human alpha7 nAChR2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Exploring α7-Nicotinic Receptor Ligand Diversity by Scaffold Enumeration from the Chemical Universe Database GDB.
AID690426Binding affinity to rat alpha7 nAchR2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID746151Biodistribution in CD1 mouse spleen at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746071Biodistribution in CD1 mouse skin at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746161Biodistribution in CD1 mouse brain at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746149Biodistribution in CD1 mouse adrenal at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746160Biodistribution in CD1 mouse lung at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746109Biodistribution in CD1 mouse skin at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746126Plasma concentration in CD1 mouse at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746129Biodistribution in CD1 mouse skin at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746159Biodistribution in CD1 mouse small intestine at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746082Biodistribution in CD1 mouse stomach at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID690430Partial agonist activity at human alpha7 nAChR expressed in GH4C1 cells relative to acetylcholine2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID746152Biodistribution in CD1 mouse thymus at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746095Biodistribution in CD1 mouse bladder at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746153Biodistribution in CD1 mouse bladder at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID690427Intrinsic activity at human alpha7 nAChR expressed in Xenopus oocytes relative to acetylcholine2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID746142Biodistribution in CD1 mouse heart at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431151Plasma concentration in Sprague-Dawley rat at 5 mg/kg, sc after 1 hr2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID1460126In vivo agonist activity at alpha7 nAChR in Wistar rat assessed as induction of Arc gene expression in medial prefrontal cortex at 10 mg/kg, sc after 2 hrs by qPCR method relative to control2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Development of spiroguanidine-derived α7 neuronal nicotinic receptor partial agonists.
AID690428Intrinsic activity at human alpha7 nAChR expressed in GH4C1 cells relative to acetylcholine2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID746154Biodistribution in CD1 mouse kidney at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431148Displacement of [3H]LY278584 from human 5HT3 receptor expressed in HEK293 cells2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746143Biodistribution in CD1 mouse brain at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431144Displacement of [3H]epibatidine from alpha3 nAChR in human IMR32 cells2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746085Biodistribution in CD1 mouse brain at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431146Aqueous solubility of the compound2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746118Biodistribution in CD1 mouse liver at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746096Biodistribution in CD1 mouse spleen at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746108Biodistribution in CD1 mouse femur at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID1278549Displacement of [3H]methyllycaconitine from Sprague-Dawley rat brain alpha7* nAChR incubated for 2.5 hrs by liquid scintillation counting analysis2016European journal of medicinal chemistry, Mar-03, Volume: 110New quinoline derivatives as nicotinic receptor modulators.
AID746121Biodistribution in CD1 mouse stomach at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746157Biodistribution in CD1 mouse large intestine at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746079Biodistribution in CD1 mouse large intestine at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746083Biodistribution in CD1 mouse lung at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746070Biodistribution in CD1 mouse femur at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746124Biodistribution in CD1 mouse brain at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746103Biodistribution in CD1 mouse lung at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746139Biodistribution in CD1 mouse small intestine at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746110Biodistribution in CD1 mouse muscle at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746075Biodistribution in CD1 mouse spleen at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746146Biodistribution in CD1 mouse muscle at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746093Biodistribution in CD1 mouse adrenal at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746128Biodistribution in CD1 mouse muscle at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746101Biodistribution in CD1 mouse stomach at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746094Biodistribution in CD1 mouse thymus at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746112Biodistribution in CD1 mouse pancreas at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746069Biodistribution in CD1 mouse muscle at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431149Intrinsic clearance in human liver microsomes at 1 uM at pH 7.4 after 30 mins2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746098Biodistribution in CD1 mouse kidney at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746155Biodistribution in CD1 mouse urine at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746150Biodistribution in CD1 mouse pancreas at 200 to 300 kBq, iv measured at 5 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431150Drug concentration in Sprague-Dawley rat brain at 5 mg/kg, sc after 1 hr2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746087Biodistribution in CD1 mouse blood at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431145Octanol-aqueous buffer partition coefficient, log D at pH 7.42009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746092Biodistribution in CD1 mouse pancreas at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746078Biodistribution in CD1 mouse kidney at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431143Selectivity ratio of IC50 for alpha4beta2 nAChR in rat brain homogenate to Ki for rat alpha7 nAChR2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746084Biodistribution in CD1 mouse heart at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis in presence of SSR1807112013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID431152Ratio of drug level in brain to plasma in Sprague-Dawley rat at 5 mg/kg, sc after 1 hr2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
AID746102Biodistribution in CD1 mouse small intestine at 200 to 300 kBq, iv measured at 60 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID746145Biodistribution in CD1 mouse blood at 200 to 300 kBq, iv measured at 15 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
AID690279Binding affinity to human 5HT3 receptor at 10 uM by radioligand binding assay2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID746125Biodistribution in CD1 mouse blood at 200 to 300 kBq, iv measured at 30 mins by gamma counting analysis2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging of α7 nicotinic acetylcholine receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's9 (29.03)29.6817
2010's22 (70.97)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.05

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 Index11.05 (24.57)
Research Supply Index3.50 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.13%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other31 (96.88%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]