Page last updated: 2024-12-07

cp 96345

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Description

CP 96345: structure given in first source; potent nonpeptide antagonist of the substance P (NK1) receptor; CP 96344 is enantiomer of CP 96345 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID104943
CHEMBL ID95638
CHEMBL ID16192
SCHEMBL ID675159
MeSH IDM0183525

Synonyms (42)

Synonym
bdbm50030232
(s)-((s)-2-benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(2-methoxy-benzyl)-amine
chembl95638
cp-96345
132746-60-2
cp 96344
(2s,3s)-2-benzhydryl-n-[(2-methoxyphenyl)methyl]quinuclidin-3-amine
cp-96,345
(2s,3s)-cis-2-(diphenylmethyl)-n-[(2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
cp 96345
1-azabicyclo(2.2.2)octan-3-amine, 2-(diphenylmethyl)-n-((2-methoxyphenyl)methyl)-, (2s-cis)-
2-(diphenylmethyl)-n-((2-methoxyphenyl)methyl)-1-azabicyclo(2.2.2)octan-3-amine
cp 96,345
CHEMBL16192 ,
(2-benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(2-methoxy-benzyl)-amine
i(2-benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(2-methoxy-benzyl)-amine
(+)(2-benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(2-methoxy-benzyl)-amine
bdbm50000040
((s)-2-benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(2-methoxy-benzyl)-amine
((2s,3s)-2-benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(2-methoxy-benzyl)-amine
(-) (2-benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(2-methoxy-benzyl)-amine
(2s,3s)-2-benzhydryl-n-[(2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
w22ila2i52 ,
unii-w22ila2i52
(2s,3s)-2-(diphenylmethyl)-n-[(2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
1-azabicyclo(2.2.2)octan-3-amine, 2-(diphenylmethyl)-n-((2-methoxyphenyl)methyl)-, (2s,3s)-
SCHEMBL675159
FLNYLINBEZROPL-NSOVKSMOSA-N ,
(2s,3s)-n-(2-methoxyphenyl)methyl-2-diphenylmethyl-1-azabicyclo[2.2.2]octan-3-amine
cp96345
AKOS024457323
cp-96345, >=98% (hplc)
J-006217
NCGC00371069-01
2-(diphenylmethyl)-n-[(2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
DTXSID30927796
(2s,3s)-2-benzhydryl-n-(2-methoxybenzyl)quinuclidin-3-amine
129912-34-1
1-azabicyclo[2.2.2]octan-3-amine, 2-(diphenylmethyl)-n-[(2-methoxyphenyl)methyl]-, (2s,3s)-
Q27292206
CS-0028950
HY-108482

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" In the presence of FK 224, SP dose-response curves and NKA dose-response curves were shifted to the right in parallel with no depression of the maximal contraction."( FK 224, a novel cyclopeptide substance P antagonist with NK1 and NK2 receptor selectivity.
Fujii, T; Kiyotoh, S; Maeda, Y; Morimoto, H; Murai, M; Nishikawa, M; Yamaoka, M, 1992
)
0.28
" Atropine (10(-6) M) and tetrodotoxin (3 x 10(-7) M) did not affect NKA-induced contractions, but inhibited SP- and NKB-induced contractions; the dose-response curves for SP and NKB were rightwardly shifted by atropine."( Tachykinin-induced contractions in the circular muscle of guinea pig ileum.
Gomi, Y; Mizuno, K; Suzuki, N, 1994
)
0.29
" In the radio-ligand receptor binding assay using [125I]-Bolton-Hunter substance P to membranes from guinea pig ileum, the fragment exhibited a distinct dose-response curve (IC50 = 11 microM)."( Receptor-mediated specific biological activity of a beta-amyloid protein fragment for NK-1 substance P receptors.
Iwata, T; Kamiya, H; Matsumoto, H; Ohno, M; Saito, R; Shimohigashi, Y; Takano, Y, 1993
)
0.29
" The NK1 antagonist (+/-)-CP96345 was found to cause, at a maximally tolerated dose of 9 mumol/kg, an approximate 10-fold rightward shift of the dose-response curves for selective NK1 agonists substance P (SP), [Sar9,Met(O2)11]SP and Ac-[Arg6,Sar9,Met(O2)11]SP6-11 without altering responses to selective NK2 agonists neurokinin A (NKA), [Nle10]NKA4-10 or [beta-Ala8]NKA4-10."( Differential blockade by tachykinin NK1 and NK2 receptor antagonists of bronchoconstriction induced by direct-acting agonists and the indirect-acting mimetics capsaicin, serotonin and 2-methyl-serotonin in the anesthetized guinea pig.
Buckner, CK; Campbell, J; Dea, D; Krell, RD; Lengel, D; Liberati, N; Miller, S; Shenvi, A; Stinson-Fisher, C, 1993
)
0.29
" Conversely, SR-48,968 antagonized the bronchoconstrictor response to Nle10-NKA[4-10], right-shifting the dose-response curve by 2 log units, but had no effect on Sar9, Met(O2)11-SP-induced bronchoconstriction."( Tachykinin receptor antagonists inhibit hyperpnea-induced bronchoconstriction in guinea pigs.
Alger, LE; Garland, A; Gitter, B; Howbert, JJ; Jordan, JE; Kao, BM; Leff, AR; Necheles, J; Rodger, IW; Solway, J, 1993
)
0.29
" Twenty-four sheep were actively sensitized to Ascaris suum, then challenged with nebulized Ascaris extract in a dose-response fashion."( Tachykinins contribute to the acute airways response to allergen in sheep actively sensitized to Ascaris suum.
Holmes, MD; Reynolds, AM; Reynolds, PN; Rice, AJ; Scicchitano, R; Thornton, AT, 1997
)
0.3
" Based on dose-response data, dialysis of the NK-1 receptor antagonist CP-96,345 (5 mM for 2 h) into the L7 dorsal horn ipsilateral to the contracting muscle attenuated the pressor response to static contraction (75 +/- 15 vs."( Segmental effect of spinal NK-1 receptor blockade on the pressor reflex.
Hand, GA; Wilson, LB, 1998
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency11.98770.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency0.19000.00108.379861.1304AID1645840
[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)
Substance-P receptorHomo sapiens (human)IC50 (µMol)0.00280.00000.09526.8130AID144536; AID145783; AID145784; AID208267; AID208269; AID208271; AID208410; AID208417; AID208420; AID208429; AID208593; AID779964
Substance-P receptorHomo sapiens (human)Ki0.00110.00000.79368.7470AID208574; AID208577; AID715707; AID715708
Neuromedin-K receptorHomo sapiens (human)Ki10.00000.00020.05430.9250AID715706
Neuromedin-K receptorCavia porcellus (domestic guinea pig)IC50 (µMol)10.00000.00200.00700.0120AID212077
Substance-P receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.00040.00002.751810.0000AID208113
Substance-K receptorMesocricetus auratus (golden hamster)IC50 (µMol)10.00000.00100.03530.1480AID211536
[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 receptorRattus norvegicus (Norway rat)Kd0.00030.00030.00030.0003AID211329
Neuromedin-K receptorRattus norvegicus (Norway rat)Kd2.51192.51192.51192.5119AID212389
Substance-P receptorHomo sapiens (human)Kd0.00610.00000.00540.0166AID208092; AID211329; AID715902; AID715903
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

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)
tachykinin receptor signaling pathwayNeuromedin-K receptorHomo sapiens (human)
positive regulation of heart rateNeuromedin-K receptorHomo sapiens (human)
response to estradiolNeuromedin-K receptorHomo sapiens (human)
regulation of dopamine metabolic processNeuromedin-K receptorHomo sapiens (human)
response to cocaineNeuromedin-K receptorHomo sapiens (human)
positive regulation of blood pressureNeuromedin-K receptorHomo sapiens (human)
regulation of feeding behaviorNeuromedin-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionNeuromedin-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilityNeuromedin-K 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)
protein bindingNeuromedin-K receptorHomo sapiens (human)
tachykinin receptor activityNeuromedin-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

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)
plasma membraneNeuromedin-K receptorHomo sapiens (human)
dendrite membraneNeuromedin-K receptorHomo sapiens (human)
neuronal cell body membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
plasma membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (55)

Assay IDTitleYearJournalArticle
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID208420Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
AID72234Maximum change in the mean arterial blood pressure in the anesthetized ferret of substane P at 3 mg/Kg intravenous bolus1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID211899Inhibition of neurokinin A induced contraction of rabbit pulmonary artery (RPA) tissue expressing Tachykinin receptor 21996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
AID208593Binding affinity was measured against the Tachykinin receptor 1 in human IM-9 cells using [3H]SP as ligand.1998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.
AID211536Inhibitory activity against [125I]neurokinin binding to Tachykinin receptor 2 in hamster urinary bladder1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
AID214783In vitro inhibitory activity against P induced IL-6 secretion in U-373 MG Astrocytoma cells1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
AID715705Displacement of radioligand [3H]osanetant at human NK3 Y315F6.51 mutant expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID208574Binding affinity towards Tachykinin receptor 1 expressed in CHO cells using [3H][Pro9]-SP as radioligand2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Synthesis, modelling and NK1 antagonist evaluation of a non-rigid cyclopropane-containing analogue of CP-99,994.
AID211329Inhibition of substance P induced contraction of rabbit vena ceva (RVC) tissue expressing Tachykinin receptor 11996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
AID212077Inhibitory activity against Tachykinin receptor 3 in guinea pig cortex [125I]-BH-eledoisin as radioligand1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
AID208269Binding affinity against human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID194622Inhibition of SP-induced salvation after intraperitoneal administration of the durg at a concentration of 50 mg/kg in rats1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
AID72232Maximum change in the mean arterial blood pressure in the anesthetized ferret of substane P at 0.3 mg/Kg intravenous bolus1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID1378235Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and biological studies of a library of NK1-Receptor Ligands Based on a 5-arylthiosubstituted 2-amino-4,6-diaryl-3-cyano-4H-pyran core: Switch from antagonist to agonist effect by chemical modification.
AID71915Effect on heart rate of substance P antagonist was determined as change heart rate in the anesthetized ferret at 0.1 mg/Kg intravenous bolus1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID208602Inhibitory activity against NK-1 receptors in mouse brain using [125I]-labeled Boltan-Hunter substance P as radioligand1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
AID211346Inhibitory activity against Tachykinin receptor 1 in rat brain using [125I]-labeled Boltan-Hunter substance P as radioligand1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
AID715902Competitive inhibition of human NK1 F264Y6.51 mutant expressed in HEK293 cells assessed as decrease in SP1-induced [3H]IP accumulation after 20 mins2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID212389Inhibition of neurokinin B induced contraction of rat portal vein (RPV) tissue expressing Tachykinin receptor 31996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
AID208092Antagonist activity against Tachykinin receptor 1 in dog isolated carotid artery1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
AID208577In vitro binding affinity for the Tachykinin receptor 1 in human IM-9 cell using [125I]BH-SP of the compound.1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Discovery of a potent substance P antagonist: recognition of the key molecular determinant.
AID208113Inhibitory activity against Tachykinin receptor 1 in guinea pig brain using [125I]-labeled Boltan-Hunter substance P as radioligand1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
AID72231Maximum change in the mean arterial blood pressure in the anesthetized ferret of substane P at 0.1 mg/Kg intravenous bolus1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID222262Inhibition of SP-induced plasma extravasation in guinea pig after peroral administration at a dose 15 mg/kg1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
AID208271Binding affinity against wild type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID145784Binding affinity towards cloned neurokinin 1 receptor, based on the displacement of [125I]-labeled substance P1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
AID208429Inhibitory activity against Tachykinin receptor 1 in human IM-9 cells using [125I]-labeled Boltan-Hunter substance P as radioligand1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
AID145783Tested in vitro for the binding affinity towards NK1 receptor in human IM-9 cells using [125I]-labeled bolton-hunter substance P as ligand1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
Aza-tricyclic substance P antagonists.
AID1378233Antagonist activity at His6-tagged NK1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of substance-P-induced IP1 accumulation preincubated for 10 mins followed by substance-P addition measured after 30 mins by HTRF-FRET assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and biological studies of a library of NK1-Receptor Ligands Based on a 5-arylthiosubstituted 2-amino-4,6-diaryl-3-cyano-4H-pyran core: Switch from antagonist to agonist effect by chemical modification.
AID715704Selectivity ratio of Ki for wild type human NK3 receptor expressed in HEK293 cells to Ki for human NK3 Y315F6.51 mutant expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID72233Maximum change in the mean arterial blood pressure in the anesthetized ferret of substane P at 1 mg/Kg intravenous bolus1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID715903Competitive inhibition of wild type human NK1 receptor expressed in HEK293 cells assessed as decrease in SP1-induced [3H]IP accumulation after 20 mins2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID223050Ability to block SP-induced excitation of neurons in the locus coeruleus in guinea pig brain1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
AID1378236Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and biological studies of a library of NK1-Receptor Ligands Based on a 5-arylthiosubstituted 2-amino-4,6-diaryl-3-cyano-4H-pyran core: Switch from antagonist to agonist effect by chemical modification.
AID71917Effect on heart rate of substance P antagonist was determined as change heart rate in the anesthetized ferret at 1 mg/Kg intravenous bolus1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID779964Antagonist activity at NK1 receptor (unknown origin)2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
AID80770Inhibition of capsaicin-induced plasma extravasation in guinea pig ureter1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
Aza-tricyclic substance P antagonists.
AID229517Ratio of IC50 value against hNK1 receptor to that of Q165A receptor.1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID222263Inhibition of capsaicin-induced plasma extravasation in guinea pig ureter after intraperitoneal injection1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
AID208417Binding affinity towards Tachykinin receptor 1 in human IM-9 cells using [3H]-substance P as ligand1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
AID144536Tested against cloned human NK1 receptor by displacement of 125 I -labeled substance P expressed in CHO cells1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.
AID214785In vitro inhibitory activity against P induced phosphatidyl inositol turnover in UC-11 MG Astrocytoma cells1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
AID71918Effect on heart rate of substance P antagonist was determined as change heart rate in the anesthetized ferret at 3 mg/Kg intravenous bolus1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID208410Inhibition of binding of [125I]SP to the CHO cell line expressing human Tachykinin receptor 11995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.
AID715706Displacement of [3H]osanetant from wild type human NK3 receptor expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID1378230Antagonist activity at His6-tagged NK1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of substance-P-induced IP1 accumulation at 10'-7 M preincubated for 10 mins followed by substance-P addition measured after 30 mins by HTRF-FRET2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and biological studies of a library of NK1-Receptor Ligands Based on a 5-arylthiosubstituted 2-amino-4,6-diaryl-3-cyano-4H-pyran core: Switch from antagonist to agonist effect by chemical modification.
AID715707Displacement of radioligand [3H]SP from human NK1 F264Y6.51 mutant expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID208267Binding affinity against Gln165Ala mutant type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID71916Effect on heart rate of substance P antagonist was determined as change heart rate in the anesthetized ferret at 0.3 mg/Kg intravenous bolus1995Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6
Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
AID715708Displacement of radioligand [3H]SP from wild type human NK1 receptor expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (394)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's324 (82.23)18.2507
2000's53 (13.45)29.6817
2010's15 (3.81)24.3611
2020's2 (0.51)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 (%)
Trials1 (0.25%)5.53%
Reviews7 (1.74%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other395 (98.01%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]