Page last updated: 2024-09-25

l 703606

Description

L 703606: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132629
CHEMBL ID24999
SCHEMBL ID15271416
MeSH IDM0206538

Synonyms (32)

Synonym
MLS002172464 ,
smr001254095
l-703,606
gtpl2104
(7r,8r)-7-[di(phenyl)methyl]-n-[(2-iodophenyl)methyl]-1-azabicyclo[2.2.2]octan-8-amine
l703606
l 703606
(cis)-n-(2-iodobenzyl)-2-benzhydrylquinuclidin-3-amine
bdbm50140771
((2r,3r)-2-benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(2-iodo-benzyl)-amine
CHEMBL24999 ,
(cis)-2-(diphenylmethyl)-n-((2-iodophenyl)methyl)-1-azabicyclo(2.2.2)octan-3-amine
2-(diphenylmethyl)-n-((2-iodophenyl)methyl)-1-azabicyclo(2.2.2)octan-3-amine
144425-84-3
2-(diphenylmethyl)-n-((2-iodophenyl)methyl)-3-quinuclidinamine
l-703606
(i125)l-703606
(2r,3r)-2-benzhydryl-n-[(2-iodophenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
1-azabicyclo(2.2.2)octan-3-amine, 2-(diphenylmethyl)-n-((2-iodophenyl)methyl)-, cis-
[(2r,3r)-2-benzhydrylquinuclidin-3-yl]-(2-iodobenzyl)amine;oxalic acid;hydrate
cid_25102597
(2r,3r)-2-benzhydryl-n-[(2-iodophenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine;oxalic acid;hydrate
(2r,3r)-2-(diphenylmethyl)-n-[(2-iodanylphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine;ethanedioic acid;hydrate
bdbm79212
(2r,3r)-2-(diphenylmethyl)-n-[(2-iodophenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine;oxalic acid;hydrate
SCHEMBL15271416
DTXSID10162704
MLS-0412840
Q27078408
(2r,3r)-2-benzhydryl-n-(2-iodobenzyl)quinuclidin-3-amine
rel-(2r,3r)-2-benzhydryl-n-(2-iodobenzyl)quinuclidin-3-amine
SDCCGMLS-0412840.P031

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Substance-P receptorHomo sapiens (human)IC50 (µMol)0.00160.00000.09526.8130AID208276
[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)
Substance-P receptorHomo sapiens (human)EC50 (µMol)0.02440.00010.00400.0244AID380505
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (38)

Processvia Protein(s)Taxonomy
aggressive behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of leukocyte migrationSubstance-P receptorHomo sapiens (human)
angiotensin-mediated drinking behaviorSubstance-P receptorHomo sapiens (human)
inflammatory responseSubstance-P receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
long-term memorySubstance-P receptorHomo sapiens (human)
associative learningSubstance-P receptorHomo sapiens (human)
detection of abiotic stimulusSubstance-P receptorHomo sapiens (human)
response to ozoneSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell migrationSubstance-P receptorHomo sapiens (human)
response to auditory stimulusSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell migrationSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, cholinergicSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicSubstance-P receptorHomo sapiens (human)
response to estradiolSubstance-P receptorHomo sapiens (human)
response to progesteroneSubstance-P receptorHomo sapiens (human)
response to nicotineSubstance-P receptorHomo sapiens (human)
operant conditioningSubstance-P receptorHomo sapiens (human)
sperm ejaculationSubstance-P receptorHomo sapiens (human)
eating behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-P receptorHomo sapiens (human)
response to ethanolSubstance-P receptorHomo sapiens (human)
positive regulation of action potentialSubstance-P receptorHomo sapiens (human)
positive regulation of blood pressureSubstance-P receptorHomo sapiens (human)
positive regulation of ossificationSubstance-P receptorHomo sapiens (human)
positive regulation of vasoconstrictionSubstance-P receptorHomo sapiens (human)
positive regulation of hormone secretionSubstance-P receptorHomo sapiens (human)
behavioral response to painSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of lymphocyte proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of stress fiber assemblySubstance-P receptorHomo sapiens (human)
response to electrical stimulusSubstance-P receptorHomo sapiens (human)
smooth muscle contraction involved in micturitionSubstance-P receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-P receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
tachykinin receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingSubstance-P receptorHomo sapiens (human)
substance P receptor activitySubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membraneSubstance-P receptorHomo sapiens (human)
cell surfaceSubstance-P receptorHomo sapiens (human)
dendriteSubstance-P receptorHomo sapiens (human)
sperm flagellumSubstance-P receptorHomo sapiens (human)
cell bodySubstance-P receptorHomo sapiens (human)
sperm headSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID208276Binding affinity against human Tachykinin receptor 1 expressed in astrocytoma UC11MG cells using [125I]- SP radioligand2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
A non-peptide NK1 receptor agonist showing subpicomolar affinity.
AID1628462Intrinsic antimalarial activity against intermediate chloroquine-resistant Plasmodium falciparum 7G8 isolate MRA-154 harboring CRT SVMNT haplotype mutant assessed as reduction in parasite viability at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628459Inhibition of CRT K76T mutant in chloroquine/artemisinin-resistant Plasmodium falciparum NHP4773 assessed as reversal of chloroquine resistance by measuring reduction in chloroquine IC50 at 500 nM relative to chloroquine alone2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628457Inhibition of CRT K76T mutant in chloroquine/artemisinin-resistant Plasmodium falciparum ARS272 assessed as reversal of chloroquine resistance by measuring reduction in chloroquine IC50 at 500 nM relative to chloroquine alone2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID208262Inhibition of labeled SP total binding to human Tachykinin receptor 1 expressed in astrocytoma UC11MG cells2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
A non-peptide NK1 receptor agonist showing subpicomolar affinity.
AID1628467Intrinsic antimalarial activity against chloroquine-resistant Plasmodium falciparum NHP4559 harboring CRT K76T mutant assessed as reduction in parasite viability at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628465Intrinsic antimalarial activity against chloroquine/artemisinin-resistant Plasmodium falciparum ARS233 harboring CRT K76T mutant assessed as reduction in parasite viability at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628460Intrinsic antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 isolate MRA-102 assessed as reduction in parasite viability at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628478Cytotoxicity against TAMH assessed as reduction in cell viability by CellTiter-Glo assay2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628463Intrinsic antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 isolate MRA-159 harboring CRT CVIET haplotype mutant assessed as reduction in parasite viability at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628479Cytotoxicity against human AC10 cells assessed as reduction in cell viability by CellTiter-Glo assay2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628453Inhibition of CRT SVMNT haplotype mutant in intermediate chloroquine-resistant Plasmodium falciparum 7G8 isolate MRA-154 t assessed as reversal of chloroquine resistance by measuring reduction in chloroquine IC50 at 500 nM relative to chloroquine alone2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628484Permeability of compound incubated for 16 hrs at pH 7.4 by PAMPA2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628485Inhibition of CRT CVIET haplotype mutant in Plasmodium falciparum K1 isolate MRA-159 infected in erythrocytes assessed as reversal of chloroquine resistance by measuring reduction in chloroquine IC50 by Hoechst 33342 staining based flow cytometry2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628449Inhibition of CRT CVIET haplotype mutant in Plasmodium falciparum K1 isolate MRA-159 infected in erythrocytes assessed as chloroquine-coumarin probe accumulation at 10 uM after 10 hrs by Hoechst 33342 staining based flow cytometry (Rvb = 35.57 +/- 3.84%)2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628458Inhibition of CRT K76T mutant in chloroquine-resistant Plasmodium falciparum NHP4559 assessed as reversal of chloroquine resistance by measuring reduction in chloroquine IC50 at 500 nM relative to chloroquine alone2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628475Cytotoxicity against TAMH assessed as chloroquine IC50 by measuring reduction in cell viability at 100 nM by CellTiter-Glo assay (Rvb = 85.26 +/- 3.01 uM)2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628481Therapeutic index, ratio of IC50 for human AC10 cells to EC50 for chloroquine-resistant Plasmodium falciparum K1 isolate MRA-159 CRT CVIET haplotype mutant2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628468Intrinsic antimalarial activity against chloroquine/artemisinin-resistant Plasmodium falciparum NHP4773 harboring CRT K76T mutant assessed as reduction in parasite viability at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628483Permeability of compound incubated for 6 hrs at pH 7.4 by PAMPA2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628470Resistance index, ratio of chloroquine IC50 for chloroquine-resistant Plasmodium falciparum K1 isolate MRA-159 CRT CVIET haplotype mutant to chloroquine IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 isolate MRA-102 at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628464Intrinsic antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 isolate MRA-156 harboring CRT K76T mutant assessed as reduction in parasite viability at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628476Cytotoxicity against TAMH assessed as chloroquine IC50 by measuring reduction in cell viability at 1 uM by CellTiter-Glo assay (Rvb = 85.26 +/- 3.01 uM)2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628482Aqueous kinetic solubility of compound in pH 7.4 solution incubated for 24 hrs2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628461Intrinsic antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB3 isolate MRA-155 assessed as reduction in parasite viability at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628455Inhibition of CRT K76T mutant in chloroquine-resistant Plasmodium falciparum Dd2 isolate MRA-156 assessed as reversal of chloroquine resistance by measuring reduction in chloroquine IC50 at 500 nM relative to chloroquine alone2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628451Potentiation of chloroquine-induced antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 isolate MRA-102 assessed as reduction in chloroquine IC50 at 500 nM relative to chloroquine alone2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628454Inhibition of CRT CVIET haplotype mutant in chloroquine-resistant Plasmodium falciparum K1 isolate MRA-159 assessed as reversal of chloroquine resistance by measuring reduction in chloroquine IC50 at 500 nM relative to chloroquine alone2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628456Inhibition of CRT K76T mutant in chloroquine/artemisinin-resistant Plasmodium falciparum ARS233 assessed as reversal of chloroquine resistance by measuring reduction in chloroquine IC50 at 500 nM relative to chloroquine alone2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID380505Displacement of [3H]SR140333 from human recombinant NK1 receptor expressed in CHO cells2006Journal of natural products, Mar, Volume: 69, Issue:3
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
AID1628466Intrinsic antimalarial activity against chloroquine/artemisinin-resistant Plasmodium falciparum ARS272 harboring CRT K76T mutant assessed as reduction in parasite viability at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628469Resistance index, ratio of chloroquine IC50 for intermediate chloroquine-resistant Plasmodium falciparum 7G8 isolate MRA-154 CRT SVMNT haplotype mutant to chloroquine IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 isolate MRA-102 at 500 nM2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628477Cytotoxicity against TAMH assessed as chloroquine IC50 by measuring reduction in cell viability at 10 uM by CellTiter-Glo assay (Rvb = 85.26 +/- 3.01 uM)2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628452Potentiation of chloroquine-induced antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB3 isolate MRA-155 assessed as reduction in chloroquine IC50 at 500 nM relative to chloroquine alone2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1628480Therapeutic index, ratio of IC50 for TAMH to EC50 for chloroquine-resistant Plasmodium falciparum K1 isolate MRA-159 CRT CVIET haplotype mutant2016European journal of medicinal chemistry, Aug-25, Volume: 119Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.
AID1346346Human NK1 receptor (Tachykinin receptors)1996The Journal of biological chemistry, Aug-23, Volume: 271, Issue:34
The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (74)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (18.92)18.2507
2000's44 (59.46)29.6817
2010's16 (21.62)24.3611
2020's0 (0.00)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%
Other74 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]