Page last updated: 2024-12-07

senktide

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

Senktide is a synthetic peptide analog of the C-terminal portion of the naturally occurring peptide substance P. It has been shown to have potent anti-inflammatory and analgesic effects. Senktide is a selective agonist of the neurokinin-1 receptor (NK-1R), which is a member of the tachykinin receptor family. NK-1R is widely expressed in the central and peripheral nervous systems, and its activation has been implicated in a variety of physiological and pathophysiological processes. Senktide is being studied as a potential therapeutic agent for the treatment of inflammatory pain, migraine headaches, and other conditions. It is also being investigated for its potential to modulate neurotransmission and promote wound healing. The synthesis of Senktide involves the solid-phase peptide synthesis method, where amino acids are sequentially added to a growing peptide chain on a solid support. The resulting peptide is then cleaved from the support and purified. Senktide is a valuable research tool for investigating the role of NK-1R in various biological processes. It is also a promising therapeutic candidate for a variety of conditions.'

Cross-References

ID SourceID
PubMed CID108147
CHEMBL ID106124
SCHEMBL ID5238634
MeSH IDM0154353

Synonyms (26)

Synonym
bdbm50052524
(s)-n-((s)-1-{[(s)-1-({[(s)-1-((s)-1-carbamoyl-3-methylsulfanyl-propylcarbamoyl)-3-methyl-butylcarbamoyl]-methyl}-carbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl}-2-phenyl-ethyl)-3-(3-carboxy-propionylamino)-succinamic acid
gtpl2127
suc[asp6,mephe3]sp(6-11))
suc[asp6,mephe3]sp(6-11)
n-(3-carboxy-1-oxopropyl)-6-(n-methyl-l-phenylalanine)-7-de-l-valine-4-10-neuromedin b (swine spinal cord)
succinyl-6-asp-8-me-phe-substance p (6-11)
substance p (6-11), succinyl-aspartyl(6)-methylphenylalanine(8)-
4-10-neuromedin b (swine spinal cord), n-(3-carboxy-1-oxopropyl)-6-(n-methyl-l-phenylalanine)-7-de-l-valine-
substance p (6-11), succinyl-asp(6)-me-phe(8)-
senktide
l-methioninamide, n-(3-carboxy-1-oxopropyl)-l-alpha-aspartyl-l-phenylalanyl-n-methyl-l-phenylalanylglycyl-l-leucyl-
106128-89-6
CHEMBL106124 ,
(3s)-4-[[(2s)-1-[[(2s)-1-[[2-[[(2s)-1-[[(2s)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]-methylamino]-1-oxo-3-phenylpropan-2-yl]amino]-3-[(4-hydroxy-4-oxobutanoyl)amino]-4-o
SCHEMBL5238634
CS-8091
HY-P0187
J-001543
Q27088780
A16945
(5s,8s,14s,17s,20s)-14,17-dibenzyl-5-carbamoyl-20-(carboxymethyl)-8-isobutyl-15-methyl-7,10,13,16,19,22-hexaoxo-2-thia-6,9,12,15,18,21-hexaazapentacosan-25-oic acid
MS-31559
4-({14-benzyl-7,10,13-trihydroxy-5-[hydroxy(imino)methyl]-15-methyl-8-(2-methylpropyl)-16-oxo-18-phenyl-2-thia-6,9,12,15-tetraazaoctadeca-6,9,12-trien-17-yl}imino)-3-[(3-carboxy-1-hydroxypropylidene)amino]-4-hydroxybutanoic acid
DTXSID80909926
(3s)-4-[[(2s)-1-[[(2s)-1-[[2-[[(2s)-1-[[(2s)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]-methylamino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(3-carboxypropanoylamino)-4-oxobutan

Research Excerpts

Overview

Senktide is a highly specific and potent analog of neurokinin B. It is the natural ligand of the tachykinin receptor NK-3.

ExcerptReferenceRelevance
"Senktide is a highly specific and potent analog of neurokinin B, the natural ligand of the tachykinin receptor NK-3. "( 1H nuclear magnetic resonance determination of the membrane-bound conformation of senktide, a highly selective neurokinin B agonist.
Bersch, B; Koehl, P; Milon, A; Nakatani, Y; Ourisson, G, 1993
)
1.95

Actions

ExcerptReferenceRelevance
"Senktide tended to increase this frequency, but its effect was not statistically significant."( Chronic peripheral administration of kappa-opioid receptor antagonist advances puberty onset associated with acceleration of pulsatile luteinizing hormone secretion in female rats.
Deura, C; Fujii, N; Iwase, A; Kikkawa, F; Maeda, K; Minabe, S; Nakahara, T; Nakamura, S; Noguchi, T; Oishi, S; Tsukamura, H; Uenoyama, Y; Watanabe, Y, 2013
)
1.11

Treatment

Senktide treatment recovered components of ELM (memory for place and object) compared with vehicle-treated animals. Pretreatment with senktide potentiated this effect to 666 (core) and 869% (shell) of baseline.

ExcerptReferenceRelevance
"Senktide treatment seemed to suppress the increase in ovarian temperature from 2 h after the beginning of administration, although the difference between groups was not statistically significant."( Neurokinin 3 receptor-selective agonist, senktide, decreases core temperature in Japanese Black cattle.
Matsuyama, S; Miwa, M; Morita, Y; Nakamura, S; Ohkura, S; Wakabayashi, Y; Yamamura, T, 2021
)
1.61
"Senktide treatment recovered components of ELM (memory for place and object) compared with vehicle-treated animals."( The neurokinin-3 receptor agonist senktide facilitates the integration of memories for object, place and temporal order into episodic memory.
Chao, OY; de Souza Silva, MA; Huston, JP; Nikolaus, S, 2014
)
1.4
"Pretreatment with senktide at a dose of 0.2 mg/kg potentiated this effect to 666 (core) and 869% (shell) of baseline, without having any effect on dopamine when given alone."( Neurokinin 3 receptor activation potentiates the psychomotor and nucleus accumbens dopamine response to cocaine, but not its place conditioning effects.
de Souza Silva, MA; Huston, JP; Jocham, G; Lauber, AC; Müller, CP, 2007
)
0.66

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic evaluation of SB 223412 in rat and dog indicated low plasma clearance, oral bioavailability and high and sustained plasma concentrations after 4 to 8 mg/kg oral dosages."( Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Brawner, ME; Elshourbagy, NA; Foley, JJ; Giardina, GA; Griswold, DE; Hay, DW; Martin, LD; Medhurst, AD; Potts, W; Sarau, HM; Schmidt, DB; Webb, EF, 1997
)
0.3
"The pharmacological and pharmacokinetic profile of SB-222200 [(S)-(-)-N-(alpha-ethylbenzyl)-3-methyl-2-phenylquinoline-4-car boxami de], a human NK-3 receptor (hNK-3R) antagonist, was determined."( Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist.
Barone, FC; Bush, B; Foley, JJ; Giardina, GA; Griswold, DE; Hay, DW; Legos, JJ; Lundberg, D; Luttmann, MA; Martin, LD; Medhurst, AD; Potts, W; Sandhu, P; Sarau, HM; Schmidt, DB; Webb, EF; Whitmore, RG, 2000
)
0.31

Bioavailability

ExcerptReferenceRelevance
" Pharmacokinetic evaluation of SB 223412 in rat and dog indicated low plasma clearance, oral bioavailability and high and sustained plasma concentrations after 4 to 8 mg/kg oral dosages."( Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Brawner, ME; Elshourbagy, NA; Foley, JJ; Giardina, GA; Griswold, DE; Hay, DW; Martin, LD; Medhurst, AD; Potts, W; Sarau, HM; Schmidt, DB; Webb, EF, 1997
)
0.3
" Pharmacokinetic evaluation of SB-222200 in rat after oral administration (8 mg/kg) indicated sustained plasma concentrations (C(max) = about 400 ng/ml) and bioavailability of 46%."( Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist.
Barone, FC; Bush, B; Foley, JJ; Giardina, GA; Griswold, DE; Hay, DW; Legos, JJ; Lundberg, D; Luttmann, MA; Martin, LD; Medhurst, AD; Potts, W; Sandhu, P; Sarau, HM; Schmidt, DB; Webb, EF; Whitmore, RG, 2000
)
0.31
" Pharmacokinetic evaluation in the mouse and rat revealed that oral SB 235375 was well absorbed systemically but did not effectively cross the blood-brain barrier."( Nonpeptide tachykinin receptor antagonists. III. SB 235375, a low central nervous system-penetrant, potent and selective neurokinin-3 receptor antagonist, inhibits citric acid-induced cough and airways hyper-reactivity in guinea pigs.
Barone, FC; Bush, B; Foley, JJ; Giardina, GA; Griswold, DE; Grugni, M; Hay, DW; Kilian, D; Kotzer, CJ; Legos, JJ; Lundberg, D; Luttmann, MA; Martin, LD; Potts, W; Raveglia, LF; Sandhu, P; Sarau, HM; Schmidt, DB; Underwood, DC, 2002
)
0.31

Dosage Studied

ExcerptRelevanceReference
" In the ventral tegmental area, senktide induced locomotion and wet dog shakes with bell-shaped dose-response curves which were unaffected by age."( Effects of ageing on tachykinin function in the basal ganglia.
Frydryszak, H; Polanski, E; Stoessl, AJ, 1993
)
0.57
" After the perivascular preinjection of 1 nmol/l L-668,169 or 1 nmol/l L-733,060 (NK1 receptor antagonists), the SP dose-response curve was shifted to the right."( Effects of neuropeptides on the sumatriptan-disturbed circulation in the optic nerve head of rabbits.
Cunha-Vaz, JG; Gaspar, MN; Macedo, TR; Ribeiro, CA, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuromedin-K receptorRattus norvegicus (Norway rat)IC50 (µMol)0.01100.01100.01100.0110AID212386
Substance-K receptorHomo sapiens (human)Ki10.00000.00011.92429.7930AID1203262
Substance-P receptorHomo sapiens (human)IC50 (µMol)10.00000.00000.09526.8130AID208430
Substance-P receptorHomo sapiens (human)Ki10.00000.00000.79368.7470AID1203183
Neuromedin-K receptorHomo sapiens (human)IC50 (µMol)0.02630.00100.28822.9900AID1165549; AID145629; AID212234
Neuromedin-K receptorHomo sapiens (human)Ki0.00320.00020.05430.9250AID1203261
Neuromedin-K receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.01200.00200.00700.0120AID212218
[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)
Neuromedin-K receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00680.00051.61667.5000AID1165554; AID212381
Substance-K receptorRattus norvegicus (Norway rat)EC50 (µMol)200.00000.00050.49643.1300AID211907
Neuromedin-K receptorHomo sapiens (human)EC50 (µMol)0.00700.00020.08960.7930AID1165553; AID145627; AID276405
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (49)

Processvia Protein(s)Taxonomy
muscle contractionSubstance-K receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-K receptorHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionSubstance-K receptorHomo sapiens (human)
intestine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
negative regulation of luteinizing hormone secretionSubstance-K receptorHomo sapiens (human)
operant conditioningSubstance-K receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-K receptorHomo sapiens (human)
positive regulation of monoatomic ion transportSubstance-K receptorHomo sapiens (human)
positive regulation of smooth muscle contractionSubstance-K receptorHomo sapiens (human)
response to electrical stimulusSubstance-K receptorHomo sapiens (human)
prolactin secretionSubstance-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-K receptorHomo sapiens (human)
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 (4)

Processvia Protein(s)Taxonomy
tachykinin receptor activitySubstance-K receptorHomo sapiens (human)
protein bindingSubstance-K receptorHomo sapiens (human)
substance K receptor activitySubstance-K receptorHomo sapiens (human)
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-K receptorHomo sapiens (human)
sperm flagellumSubstance-K receptorHomo sapiens (human)
sperm headSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
sperm midpieceSubstance-K receptorHomo sapiens (human)
plasma membraneSubstance-K receptorHomo sapiens (human)
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 (35)

Assay IDTitleYearJournalArticle
AID1346355Rat NK3 receptor (Tachykinin receptors)1992FEBS letters, Mar-24, Volume: 299, Issue:1
Molecular characterisation, expression and localisation of human neurokinin-3 receptor.
AID1346386Human NK3 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.
AID1346355Rat NK3 receptor (Tachykinin receptors)1986The Journal of biological chemistry, Aug-05, Volume: 261, Issue:22
Characterization of a neurokinin B receptor site in rat brain using a highly selective radioligand.
AID1346386Human NK3 receptor (Tachykinin receptors)2001European journal of pharmacology, Feb-16, Volume: 413, Issue:2-3
Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
AID1346386Human NK3 receptor (Tachykinin receptors)1997The Journal of pharmacology and experimental therapeutics, Jun, Volume: 281, Issue:3
Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
AID1346402Mouse NK3 receptor (Tachykinin receptors)2001European journal of pharmacology, Feb-16, Volume: 413, Issue:2-3
Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.
AID1165579Metabolic stability in cattle serum up to 24 hrs by HPLC analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID211907Effective concentration to activate Tachykinin receptor 2 in rat vas deferens (RVD)1996Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16
Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P.
AID1203261Displacement of [125I][MePhe7]NKB from human NK3R expressed in CHO cell membranes after 90 mins by scintillation counting analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
AID145629Compound was evaluated for its ability to displace [3H]NKB binding in hNK3 receptors expressed in CHO cells1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.
AID1165581Metabolic stability in goat serum up to 24 hrs by HPLC analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID1165584Drug metabolism assessed as NEP 24.11 (unknown origin)-mediated Succinyl-Asp-Phe-MePhe-Gly-OH up to 24 hrs by HPLC analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID1165553Agonist activity at human NK3R expressed in CHO cells assessed as potentiation of senktide-induced effect2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID1165549Displacement of [125I]His3, MePhe7 from human NK3R expressed in CHO cell membranes by scintillation counting2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID208097Effective concentration to activate Tachykinin receptor 1 in guinea pig ileum(GPI)1996Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16
Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P.
AID212218Inhibitory activity against Tachykinin receptor 3 in guinea pig cortical membranes labeled with [125I]-[MePhe7]1996Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
AID1203182Displacement of [3H]-SB222200 from rat NK3R after 90 mins by scintillation counting analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
AID276405Activity at human NK3 receptor expressed in CHO cells assessed as increase in inositol phosphate generation2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.
AID1165582Metabolic stability in pig hypothalamic extract by HPLC analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID1165580Metabolic stability in pig serum up to 24 hrs by HPLC analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID1203183Displacement of [3H]-Substance P from human NK1R after 90 mins by scintillation counting analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
AID1165556Agonist activity at goat NK3R2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID1165578Metabolic stability in rat serum up to 24 hrs by HPLC analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID1165583Drug metabolism assessed as NEP 24.11 (unknown origin)-mediated degradation up to 24 hrs by HPLC analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID212381Effective concentration to activate Tachykinin receptor 3 in rat portal vein (RPV)1996Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16
Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P.
AID1165555Agonist activity at cattle NK3R2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID1203181Displacement of [3H]-SB222200 from monkey NK3R after 90 mins by scintillation counting analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
AID1203262Displacement of [125I]NKA from human NK2R expressed in CHO cell membranes after 90 mins by scintillation counting analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
AID212386Inhibitory activity against cloned human Tachykinin receptor 3 in CHO cells labeled with [125I][MePhe7]-NKB1996Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
AID145627Compound was evaluated for concentration-dependent and oscillatory increase in [Ca2+], caused by activation of hNK3 receptors in CHO cells1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.
AID1165554Agonist activity at rat NK3R2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID1165557Induction of GnRH release in ovariectomized goat assessed as induction of multiple-unit activity volley measured as duration of effect at 200 nmol, iv as single dose2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID208430Inhibitory activity against Tachykinin receptor 1 in human lymphoma IM9 cells labeled with [125I]Bolton-Hunter substance P1996Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
AID1165585Drug metabolism assessed as NEP 24.11 (unknown origin)-mediated H-Leu-Met-NH2 up to 24 hrs by HPLC analysis2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
AID212234Inhibitory activity against Tachykinin receptor 3 in rat cortical membranes labeled with [125I][MePhe7]-NKB1996Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (289)

TimeframeStudies, This Drug (%)All Drugs %
pre-199012 (4.15)18.7374
1990's140 (48.44)18.2507
2000's80 (27.68)29.6817
2010's54 (18.69)24.3611
2020's3 (1.04)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.21

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index23.21 (24.57)
Research Supply Index5.68 (2.92)
Research Growth Index5.56 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.34%)5.53%
Reviews1 (0.34%)6.00%
Case Studies1 (0.34%)4.05%
Observational0 (0.00%)0.25%
Other289 (98.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]