Page last updated: 2024-12-10

neurotensin

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Description

neurotensin, Tyr(11)-: RN given refers to parent cpd & (D)-isomer; RN for cpd without isomeric designation not avail 5/91 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311318
CHEMBL ID415788
MeSH IDM0014773
PubMed CID14598781
MeSH IDM0014773
PubMed CID25077406
CHEMBL ID407196
CHEBI ID7542
MeSH IDM0014773

Synonyms (54)

Synonym
bdbm50048908
CHEMBL415788 ,
neurotensin(8-13)
(2s)-2-[[(2s,3s)-2-[[(2s)-2-[[(2s)-1-[(2s)-2-[[(2s)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid
neurotensin-(8-13)
gtpl7363
l-leucine,l-arginyl-l-arginyl-l-prolyl-l-tyrosyl-l-isoleucyl-
HY-P0251
l-arginyl-l-arginyl-l-prolyl-l-tyrosyl-l-isoleucyl-l-leucine
BS-17187
D80643
AKOS037649204
neurotensin (9-13)
gtpl1579
gtpl1574
[125i]neurotensin (human, mouse, rat)
[125i]nt
l-pyroglutamyl-l-leucyl-l-tyrosyl-l-alpha-glutamyl-l-asparagyl-l-lysyl-l-prolyl-l-arginyl-l-arginyl-l-prolyl-l-tyrosyl-l-isoleucyl-l-leucine
glp-leu-tyr-glu-asn-lys-pro-arg-arg-pro-tyr-ile-leu-oh
5-oxo-l-pro-l-leu-l-tyr-l-glu-l-asn-l-lys-l-pro-l-arg-l-arg-l-pro-l-tyr-l-ile-l-leu
CHEBI:7542
pyr-leu-tyr-glu-asn-lys-pro-arg-arg-pro-tyr-ile-leu
neurotensin (1-13)
neurotensin-(1-13)
5-oxo-l-prolyl-l-leucyl-l-tyrosyl-l-alpha-glutamyl-l-asparaginyl-l-lysyl-l-prolyl-l-arginyl-l-arginyl-l-prolyl-l-tyrosyl-l-isoleucyl-l-leucine
neurotensin 1-13
5-oxo-l-pro-l-leu-l-tyr-l-glu-l-asn-l-lys-l-pro-l-arg-l-arg-l-pro-l-tyr-l-ile-l-leu-oh
l-pyr-l-leu-l-tyr-l-glu-l-asn-l-lys-l-pro-l-arg-l-arg-l-pro-l-tyr-l-ile-l-leu
ccris 3327
39379-15-2
neurotensin ,
NCGC00167274-01
pglu-leu-tyr-glu-asn-lys-pro-arg-arg-pro-tyr-ile-leu-oh
pglu-leu-tyr-glu-asn-lys-pro-arg-arg-pro-tyr-ile-leu
nt(1-13)
bdbm50130880
CHEMBL407196 ,
xhb61lg5qs ,
unii-xhb61lg5qs
neurotensin (ox)
55508-42-4
neurotensin (ox), 11-d-tyrosine-
11-tyr-neurotensin
neurotensin, tyr(11)-
neurotensin, tyrosine(11)-
(d-tyr11)neurotensin
gtpl3830
[3h]-neurotensin
[3h]neurotensin (human, mouse, rat)
neurotensin, >=90% (hplc)
pglu(1)-leu(2)-tyr(3)-glu(4)-asn(5)-lys(6)-pro(7)-arg(8)-arg(9)-pro(10)-tyr(11)-ile(12)-leu(13)-oh
Q27087905
h-pyr-leu-tyr-glu-asn-lys-pro-arg-arg-pro-tyr-ile-leu-oh

Research Excerpts

Overview

Neurotensin is an endogenous tridecapeptide found in the central nervous system (CNS) and in peripheral tissues.

ExcerptReferenceRelevance
"Neurotensin (NT) is an endogenous tridecapeptide found in the central nervous system (CNS) and in peripheral tissues. "( The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).
Di Fruscia, P; He, Y; Kamenecka, TM; Koenig, M; McDonald, PH; Nieto, A; Tabrizifard, S, 2014
)
2.1

Toxicity

ExcerptReferenceRelevance
" Here, we thus hypothesized that the combined use of opioid and NT agonists would require lower doses to produce significant analgesic effects, hence decreasing opioid-induced adverse effects."( The combination of opioid and neurotensin receptor agonists improves their analgesic/adverse effect ratio.
Blais, V; Côté, J; Eiselt, E; Gendron, L; Longpré, JM; Sarret, P, 2019
)
0.51

Pharmacokinetics

ExcerptReferenceRelevance
" To assess its pharmacokinetic parameters in man the MCR and plasma half-life were estimated by the continuous infusion method."( Infusion of a novel peptide, calcitonin gene-related peptide (CGRP) in man. Pharmacokinetics and effects on gastric acid secretion and on gastrointestinal hormones.
Bloom, SR; Ch'ng, JL; Ghatei, MA; Kraenzlin, ME; Mulderry, PK, 1985
)
0.27
"A high-performance liquid chromatographic method to determine (Me)Arg-Lys-Pro-Trp-tert-Leu-Leu (NT-2) with neurotensin (NT) activity in rat plasma was developed and a pharmacokinetic study was performed in rats."( Pharmacokinetics of novel hexapeptides with neurotensin activity in rats.
Abe, K; Machida, R; Sasaki, A; Tokumura, T; Tsuchiya, Y, 1993
)
0.29
" Cerebrospinal fluid (CSF) and blood were collected for pharmacokinetic (PK) evaluation."( Phase IA Clinical Trial Evaluating the Tolerability, Pharmacokinetics, and Analgesic Efficacy of an Intrathecally Administered Neurotensin A Analogue in Central Neuropathic Pain Following Spinal Cord Injury.
Barnabe, KJ; Kern, SE; Sang, CN, 2016
)
0.43

Compound-Compound Interactions

ExcerptReferenceRelevance
"Microdialysis was combined with a highly sensitive sequential multiple antigen radioimmunoassay to simultaneously measure extracellular cholecystokinin and neurotensin fragments from discrete regions of the rat brain in vivo."( Dual determination of extracellular cholecystokinin and neurotensin fragments in rat forebrain: microdialysis combined with a sequential multiple antigen radioimmunoassay.
Erdelyi, E; Evans, CJ; Maidment, NT; Rudolph, VR; Siddall, BJ, 1991
)
0.28
"Allantoic endoderm of 3-day chick embryos was combined with pancreatic mesenchyme of 5-day embryos and cultured as chorio-allantoic grafts for a total of 14 days."( Differentiation of endocrine cells in chick allantoic epithelium combined with pancreatic mesenchyme.
Andrew, A; Stein, B, 1989
)
0.28
"The aim of this study is to evaluate the effect of the application of physical abrasion in combination with chemical peels."( A study of the effects of physical dermabrasion combined with chemical peeling in porcine skin.
Choi, JH; Jeong, KH; Kang, BK; Lee, SJ; Park, JM; Shin, MK; Suh, DH, 2015
)
0.42
"Three pigs were treated with physical abrasion using a water jet device in combination with an α-hydroxy acid solution, and the skin samples of the control received chemical peeling solution alone."( A study of the effects of physical dermabrasion combined with chemical peeling in porcine skin.
Choi, JH; Jeong, KH; Kang, BK; Lee, SJ; Park, JM; Shin, MK; Suh, DH, 2015
)
0.42
"Skin treated with physical dermabrasion combined with chemical peeling showed prominent detachment and swelling of the stratum corneum (SC), and fluid collection in the hair follicles."( A study of the effects of physical dermabrasion combined with chemical peeling in porcine skin.
Choi, JH; Jeong, KH; Kang, BK; Lee, SJ; Park, JM; Shin, MK; Suh, DH, 2015
)
0.42
"We concluded that physical dermabrasion combined with chemical peeling can be more effective than chemical peeling alone, for the approach through transfollicular routes."( A study of the effects of physical dermabrasion combined with chemical peeling in porcine skin.
Choi, JH; Jeong, KH; Kang, BK; Lee, SJ; Park, JM; Shin, MK; Suh, DH, 2015
)
0.42

Bioavailability

ExcerptReferenceRelevance
" NT also facilitated transcellular uptake of (3)H-glucose and (3)H-leucine and increased paracellular uptake to (51)Cr-EDTA and (3)H-mannitol, but did not alter the absorption rate for (14)C-antipyrine."( Enhancement of jejunal absorption of conjugated bile acid by neurotensin in rats.
Carraway, RE; Gui, X, 2001
)
0.31
" However, limited peptide stability and oral bioavailability have prevented these compounds from being developed as relevant pharmaceuticals."( Design, synthesis, and evaluation of the antipsychotic potential of orally bioavailable neurotensin (8-13) analogues containing non-natural arginine and lysine residues.
Dix, TA; Hadden, MK; Kokko, KP; Mazella, J; Orwig, KS, 2005
)
0.33
" In this case, the drug administration per os in the form of a tabletization mixture with poly(vinyl pyrrolidone) and lactose was more effective compared to a mixture of the parent substance with Tween-80, which can be explained by the favorable effect of additives on the bioavailability of dilept."( [Neurotensine dipeptide analog dilept decreases the deficiency of prestimulus startle reflex inhibition: a prognostic sign of antipsychotic activity].
Gudasheva, TA; Krupina, NA; Ostrovskaia, RU; Seredenin, SB; Voronina, TA,
)
0.13
" To transform these peptides into potential neurotherapeutics, their systemic bioavailability and metabolic stability must be improved."( Introduction of lipidization-cationization motifs affords systemically bioavailable neuropeptide Y and neurotensin analogs with anticonvulsant activities.
Bulaj, G; Green, BR; Klein, B; McDougle, DR; Pruess, TH; Scholl, EA; White, HS; White, KL; Zhang, L, 2010
)
0.36
"The identification of the novel, selective, orally bioavailable Sortilin inhibitor AF38469 is described."( The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
Andersen, JL; Biilmann Rønn, LC; Bundgaard, C; Christensen, S; David, L; de Jong, IE; Egebjerg, J; Eradi, P; Eskildsen, J; Jacobsen, J; Karlsson, JJ; Kasturi, SP; Langgård, M; Lindberg, S; Malik, IJ; Maltas, PJ; Pervaram, S; Sakumudi, DR; Schrøder, TJ; Simonsen, KB; Stavenhagen, JB; Strandbygård, D; Tagmose, L; Thirup, S; Uppalanchi, S; Watson, SP, 2014
)
0.4
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43

Dosage Studied

Dopaminergic autoreceptors of some neurones were less sensitive than in control conditions. The dose-response curve for the neurotensin effect was triphasic. Dose-response curves to the dopaminergic agonist BHT920 showed that, during the infusion of 10(-7) M neurotensins, dopaminergies were reduced.

ExcerptRelevanceReference
" A dose-response relationship was not observed."( Centrally administered neurotensin: activity in the Julou-Courvoisier muscle relaxation test in mice.
Manberg, PJ; Nemeroff, CB; Osbahr, AJ; Prange, AJ, 1979
)
0.26
" Because of the interaction between dopamine (DA) and neurotensin (NT) in the target areas of these systems, and in order to study if the different action of typical and atypical neuroleptic drugs could be related to a modification of the DA/NT balance, we investigated DA2 and NT receptor modifications--by means of quantitative receptor autoradiography--after chronic treatment with low dosage of haloperidol, chlorpromazine, thioridazine and clozapine."( DA2/NT receptor balance in the mesostriatal and mesolimbocortical systems after chronic treatment with typical and atypical neuroleptic drugs.
Amato, G; Calzà, L; Giardino, L; Piazza, PV; Zanni, M, 1990
)
0.28
" Single injections of neurotensin (1, 2, 4 and 8 micrograms/kg), somatostatin (5, 10 and 20 micrograms/kg) and substance P (1, 2, 4 and 8 micrograms/kg) induced relaxation followed by contraction, but their dose-response relations were obscure."( Effects of gastrointestinal hormones and their related compounds on gastric motility in the rat.
Muto, N; Tani, S, 1985
)
0.27
" Dose-response curves to the dopaminergic agonist BHT920 showed that, during the infusion of 10(-7) M neurotensin, dopaminergic autoreceptors of some neurones were less sensitive than in control conditions."( Electrophysiological effects of neurotensin on dopaminergic neurones of the ventral tegmental area of the rat in vitro.
Dresse, A; Massotte, L; Seutin, V, 1989
)
0.28
" The contractile responses to VIP were unchanged after beta-adrenergic blockade with nadolol at a concentration (10 microM) that shifted the ISO dose-response curve two to three orders of magnitude to the right."( Contractile effects of cardiac neuropeptides in isolated canine atrial and ventricular muscles.
Balasubramaniam, A; Grupp, G; Grupp, IL; Rigel, DF, 1989
)
0.28
" Neurotensin preincubation with intact N1E-115 cells for increasing lengths of time caused time-dependent shifts to the right of the dose-response curve and reductions in the maximum cyclic GMP response."( Desensitization of neurotensin receptor-mediated cyclic GMP formation in neuroblastoma clone N1E-115.
Gilbert, JA; Richelson, E; Strobel, TR, 1988
)
0.27
" The NTLI response to epinephrine was competitively inhibited by propranolol, producing a parallel rightward shift of the epinephrine dose-response curve."( Regulation of neurotensin release from canine enteric primary cell cultures.
Barber, DL; Buchan, AM; Soll, AH; Walsh, JH, 1986
)
0.27
" Dose-response curves for neurotensin-induced secretion revealed an EC50 of 1x10(-6)M, thereby being in the range of that for acetylcholine or nicotine."( Neurotensin affects metabolism of opioid peptides, catecholamines and inositol phospholipids in bovine chromaffin cells.
Bommer, M; Herz, A, 1989
)
0.28
" Pirenzepine, and M1 selective antagonist, produced a parallel shift in the oxotremorine dose-response curve, indicating that the enhanced hypnotic sensitivity to ethanol may be due to interaction of oxotremorine with M1 muscarinic receptors."( Central muscarinic cholinergic influences on ethanol sensitivity in long-sleep and short-sleep mice.
Erwin, VG; Jones, BC; Korte, A, 1988
)
0.27
" The dose-response curves were comparable with the two methods."( Neurotensin effects on evoked release of dopamine in slices from striatum, nucleus accumbens and prefrontal cortex in rat.
Blanchard, JC; Boireau, A; Dubédat, P; Hétier, E, 1988
)
0.27
" Blockade of prostaglandin (PG) synthesis by indomethacin or cortisone (5 X 10(-6) M) shifted to the right the dose-response curve for neurotensin (NT) and significantly reduced the NT maximum responses."( Mode of action of neurotensin on the spontaneous and electrically-induced contractions of gastric smooth muscle.
Bocheva, A; Milenov, K; Rakovska, A; Vassileva, M, 1987
)
0.27
" The dose-response curve for the neurotensin effect was triphasic: and initial gentle rise, a plateau (2."( Histamine release induced by neurotensin from rat peritoneal mast cells.
Kurose, M; Saeki, K, 1981
)
0.26
" Dose-response curves to AVP and to oCRF were obtained, and the response to a low dose of oCRF was potentiated by a low dose of AVP."( Effect of hypothalamic neuropeptides on corticotrophin release from quarters of rat anterior pituitary gland in vitro.
Adrian, TE; Bloom, SR; Gillham, B; Jones, MT; Nicholson, SA, 1984
)
0.27
" The microapplication of neurotensin in the same dosage into the posterior hypothalamus increased the stomach secretory function induced by histamine administration."( [Existence of neurotensin receptors in the caudate nucleus and posterior hypothalamus].
Barashkova, GM; Fokina, AA; Iakimovskii, AF; Klimov, PK; Suvorov, NF, 1982
)
0.26
" Experiments are performed on injection of antiserotonin serum of various dosage into the rat blood bed."( [Serotonin and neurotensin-containing cells in the mucosa of the alimentary tract].
Kazakov, VK; Kocherginskiĭ, EB; Solov'eva, IA, 1984
)
0.27
" In the radioimmunoassay toward NT they displayed dose-response curves parallel to standard and gave results indicating a competitive type of interaction with NT binding sites on antibody."( Bacterial peptides with C-terminal similarities to bovine neurotensin.
Bhatnagar, YM; Carraway, R, 1981
)
0.26
" However preinjection flow of a second dose-response curve of ET-1 was significantly higher in captopril-treated as compared with control animals."( Interference of angiotensin-converting enzyme inhibition with vasoactive peptides in the coronary circulation of dogs.
Bauer, B; Becker, HH; Dürr, R; Ertl, G; Neubauer, S; Spindler, M, 1995
)
0.29
" There was a dose-response relationship between the magnitude of the hyperpolarization and the concentration of the peptide (10(-10)-10(-7)M); 10(-10)M being the threshold concentration."( Autoradiographic and electrophysiological evidence for the existence of neurotensin receptors on cultured astrocytes.
Hösli, E; Hösli, L; Stauffer, S, 1995
)
0.29
" The pancreatic dose-response curve to 40-min venous infusions of neurotensin 1-13 (0."( Mechanism of neurotensin stimulation of external pancreatic secretion in the rat.
Chariot, J; Nagain, C; Rozé, C, 1993
)
0.29
" In Experiment 1, the dose-response and time course of neurotensin-induced hypothermia were evaluated (n = 5/dose)."( Neurotensin-induced hypothermia prevents hippocampal neuronal damage and increased locomotor activity in ischemic gerbils.
Babcock, AM; Baker, DA; Hallock, NL; Lovec, R; Lynch, WC; Peccia, JC, 1993
)
0.29
" In contrast, PHI was an effective stimulant in doses up to 15 nmol/rat but had no effect on either ACTH or CORT at a dose of 30 nmol/rat thus yielding a bell-shaped dose-response curve."( VIP antagonist demonstrates differences in VIP- and PHI-mediated stimulation and inhibition of ACTH and corticosterone secretion in rats.
Alexander, LD; Sander, LD, 1995
)
0.29
" Both, galanin and neurotensin (10(-9)-10(-5)) stimulated basal LH secretion in a dose-response manner."( Comparison of the effect of hypothalamic neuropeptides upon luteinizing hormone secretion by cultured rat anterior pituitary cells.
Croxatto, HB; Leiva, LA, 1994
)
0.29
" The ethanol activation slope provides a robust dose-response measure of ethanol activation, independent of both activity after saline and the inhibitory effects of ethanol on locomotor activity."( Common quantitative trait loci for alcohol-related behaviors and central nervous system neurotensin measures: locomotor activation.
Erwin, VG; Gehle, VM; Jones, BC; Radcliffe, RA, 1997
)
0.3
" Incubated with PC3 cells, NT exhibited a mitogenic effect with bell-shaped dose-response and maximum at 100 pM NT."( Neurotensin receptor expression in prostate cancer cell line and growth effect of NT at physiological concentrations.
Carraway, RE; Dobner, PR; Menon, M; Mitra, SP; Seethalakshmi, L, 1997
)
0.3
" Acute dosing with either vehicle, haloperidol, clozapine or zotepine produced no significant changes in NT binding from controls (naïve rats)."( Chronic, but not acute, dosing of antipsychotic drugs alters neurotensin binding in rat brain regions.
Aspley, S; Bennett, GW; Holtom, PE; Needham, PL, 2000
)
0.31
" We also provide evidence of deficient NT neurotransmission as well as a left-shifted antipsychotic drug dose-response curve in isolation-reared rats."( Enhanced neurotensin neurotransmission is involved in the clinically relevant behavioral effects of antipsychotic drugs: evidence from animal models of sensorimotor gating.
Binder, EB; Kilts, CD; Kinkead, B; Nemeroff, CB; Owens, MJ, 2001
)
0.31
" Thus, for example, NT69L after five daily injections at a fixed dosage was as effective at reversing cocaine-induced hyperactivity as after the first injection."( Selective tolerance to the hypothermic and anticataleptic effects of a neurotensin analog that crosses the blood-brain barrier.
Boules, M; Fauq, A; McCormick, D; McMahon, B; Richelson, E; Stewart, J; Wang, R; Warrington, L; Yerbury, S, 2003
)
0.32
" Chronic dosing (5mg/kg) of this compound over 5 consecutive days failed to induce hypothermic tolerance while the same dose failed to induce measurable catalepsy."( In vivo behavioral effects of stable, receptor-selective neurotensin[8-13] analogues that cross the blood-brain barrier.
Dix, TA; Hadden, MK; Kokko, KP; Orwig, KS; Price, KL; See, RE, 2005
)
0.33
" In a dose-response study (experiment 1) we used 3 different doses of neurotensin (25, 50 and 100microg) in a bolus icv infusion."( Effect of intracerebroventricular infusion of neurotensin in glucose-dependent insulinotropic peptide secretion in dogs.
Gotzamani-Psarakou, A; Kesisoglou, I; Kotsa, K; Yavropoulou, MP; Yovos, JG, 2010
)
0.36
" Dose-response curves revealed that two compounds were partial agonists with maximal responses below 75%, whereas all of the remaining compounds displayed a full response."( Systemically and topically active antinociceptive neurotensin compounds.
Barbut, D; Matulonis, JE; Pasternak, GW; Richelson, E; Rossi, GC, 2010
)
0.36
"01) satiety effect at high dosage (500 nmol/kg)."( Evaluation of the degradation and metabolic effects of the gut peptide xenin on insulin secretion, glycaemic control and satiety.
Flatt, PR; Gault, VA; Irwin, N; McKillop, AM; Patterson, S; Taylor, AI, 2010
)
0.36
" Four 25 mg/kg injections of mephedrone increased NT content in basal ganglia (striatum, substantia nigra and globus pallidus) and the limbic regions (nucleus accumbens core), while a lower dosage (5 mg/kg/injection) only increased striatal NT content."( Mephedrone alters basal ganglia and limbic neurotensin systems.
Fleckenstein, AE; German, CL; Hanson, GR; Hoonakker, AH, 2014
)
0.4
" Efficacy dosage with long-term treatment showed no obvious adverse events, while demonstrating improvement in the performance status."( Modulation of lung cancer cell plasticity and heterogeneity with the restoration of cisplatin sensitivity by neurotensin antibody.
Agopiantz, M; Alifano, M; Boullier, A; Djebrani-Oussedik, N; Duchatelle, V; Fléjou, JF; Forgez, P; Fournel, L; Gompel, A; Hoyeau, N; Liu, J; Melander, O; Ségal-Bendirdjian, E; Stadler, N; Trédaniel, J; Wu, Z, 2019
)
0.51
" To biologically evaluate these analogues, we determined their plasma stability and their binding affinities to type 1 NT receptor (NTS1), endogenously expressed in HT-29 cells, Among the fourteen NT analogues, compounds, NT5, NT6, and NT8, which have D-Tyr(Et) at position 11, bound to NTS1 in a dose-response manner and with relatively high affinity but still lower than that of the natural peptide."( Novel stable analogues of the neurotensin C-terminal hexapeptide containing unnatural amino acids.
Dermitzaki, E; Exarchakou, R; Karageorgos, V; Liapakis, G; Magafa, V; Margioris, AN; Matsoukas, MT; Pardalos, M; Spyroulias, GA; Stylos, EΚ; Tzakos, AG; Varvounis, G, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
mitogenA chemical substance that encourages a cell to commence cell division, triggering mitosis.
neurotransmitterAn endogenous compound that is used to transmit information across the synapse between a neuron and another cell.
vulneraryA drug used in treating and healing of wounds.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
peptide hormoneAny peptide with hormonal activity in animals, whether endocrine, neuroendocrine, or paracrine.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neurotensin receptor type 2Homo sapiens (human)IC50 (µMol)0.00750.00750.00750.0075AID1251024
Neurotensin receptor type 2Homo sapiens (human)Ki0.00190.00050.04710.4180AID1289949; AID1332008; AID1482087; AID1541740; AID1697037; AID1890925
Neurotensin receptor type 1Homo sapiens (human)IC50 (µMol)0.00070.00020.00730.0820AID1251023; AID1289937; AID1409813
Neurotensin receptor type 1Homo sapiens (human)Ki0.00050.00010.00100.0033AID1289937; AID1332007; AID1385376; AID1482086; AID1510626; AID1541732; AID1541735; AID1547790; AID1697036; AID1890924; AID1890926
Neurotensin receptor type 2Homo sapiens (human)Ki0.00460.00050.04710.4180AID1055239; AID1731235; AID593496
Neurotensin receptor type 1Rattus norvegicus (Norway rat)Ki0.00140.00110.00180.0026AID1161615; AID1176214
Neurotensin receptor type 1Homo sapiens (human)IC50 (µMol)0.00130.00020.00730.0820AID1285644; AID1336341; AID147045; AID268353; AID268354; AID340256; AID346439; AID349183; AID414520; AID751868; AID752198
Neurotensin receptor type 1Homo sapiens (human)Ki0.00170.00010.00100.0033AID1541732; AID1731234; AID346439; AID388349; AID414520; AID751868
Neurotensin receptor type 2Rattus norvegicus (Norway rat)IC50 (µMol)0.05820.01850.05820.1140AID1154141; AID1161614; AID1176213
Neurotensin receptor type 2Rattus norvegicus (Norway rat)Ki0.02260.00580.09170.6440AID1154142; AID1161616; AID1176215
SortilinHomo sapiens (human)IC50 (µMol)0.36000.23800.31110.3600AID1061981
[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)
Neurotensin receptor type 1Homo sapiens (human)EC50 (µMol)0.00080.00000.573610.0000AID1182263; AID1251025; AID1251026; AID1289935; AID1385378; AID1385379; AID1385380; AID1385381; AID1541730; AID1541731; AID1697048
Neurotensin receptor type 1Mus musculus (house mouse)EC50 (µMol)0.00200.00200.00200.0020AID414528
Neurotensin receptor type 2Homo sapiens (human)EC50 (µMol)0.11000.11000.11000.1100AID593500
Myelin basic proteinMus musculus (house mouse)Kd0.00060.00060.00060.0006AID593495
Neurotensin receptor type 1Rattus norvegicus (Norway rat)EC50 (µMol)0.00000.00000.00000.0000AID1154136
Neurotensin receptor type 1Homo sapiens (human)EC50 (µMol)0.06320.00000.573610.0000AID349181; AID414521; AID414527; AID418186; AID593498
Neurotensin receptor type 1Homo sapiens (human)Kd0.00050.00040.01300.0330AID1055241; AID593495
Neurotensin receptor type 2Rattus norvegicus (Norway rat)EC50 (µMol)0.10000.01800.07080.2170AID1176211
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neurotensin receptor type 2Homo sapiens (human)Activity0.00110.00110.00110.0011AID326478
Neurotensin receptor type 1Homo sapiens (human)Activity0.00020.00020.00020.0002AID326477
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (47)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathwayNeurotensin receptor type 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNeurotensin receptor type 2Homo sapiens (human)
sensory perceptionNeurotensin receptor type 2Homo sapiens (human)
regulation of membrane potentialNeurotensin receptor type 2Homo sapiens (human)
neuropeptide signaling pathwayNeurotensin receptor type 2Homo sapiens (human)
positive regulation of gene expressionNeurotensin receptor type 1Homo sapiens (human)
temperature homeostasisNeurotensin receptor type 1Homo sapiens (human)
negative regulation of systemic arterial blood pressureNeurotensin receptor type 1Homo sapiens (human)
regulation of membrane depolarizationNeurotensin receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeurotensin receptor type 1Homo sapiens (human)
neuropeptide signaling pathwayNeurotensin receptor type 1Homo sapiens (human)
chemical synaptic transmissionNeurotensin receptor type 1Homo sapiens (human)
learningNeurotensin receptor type 1Homo sapiens (human)
adult locomotory behaviorNeurotensin receptor type 1Homo sapiens (human)
positive regulation of glutamate secretionNeurotensin receptor type 1Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionNeurotensin receptor type 1Homo sapiens (human)
response to lipidNeurotensin receptor type 1Homo sapiens (human)
positive regulation of apoptotic processNeurotensin receptor type 1Homo sapiens (human)
negative regulation of apoptotic processNeurotensin receptor type 1Homo sapiens (human)
regulation of respiratory gaseous exchangeNeurotensin receptor type 1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painNeurotensin receptor type 1Homo sapiens (human)
negative regulation of release of sequestered calcium ion into cytosolNeurotensin receptor type 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolNeurotensin receptor type 1Homo sapiens (human)
positive regulation of inositol phosphate biosynthetic processNeurotensin receptor type 1Homo sapiens (human)
D-aspartate import across plasma membraneNeurotensin receptor type 1Homo sapiens (human)
inositol phosphate catabolic processNeurotensin receptor type 1Homo sapiens (human)
positive regulation of arachidonic acid secretionNeurotensin receptor type 1Homo sapiens (human)
positive regulation of inhibitory postsynaptic potentialNeurotensin receptor type 1Homo sapiens (human)
L-glutamate import across plasma membraneNeurotensin receptor type 1Homo sapiens (human)
cell surface receptor signaling pathwayNeurotensin receptor type 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNeurotensin receptor type 2Homo sapiens (human)
sensory perceptionNeurotensin receptor type 2Homo sapiens (human)
regulation of membrane potentialNeurotensin receptor type 2Homo sapiens (human)
neuropeptide signaling pathwayNeurotensin receptor type 2Homo sapiens (human)
positive regulation of gene expressionNeurotensin receptor type 1Homo sapiens (human)
temperature homeostasisNeurotensin receptor type 1Homo sapiens (human)
negative regulation of systemic arterial blood pressureNeurotensin receptor type 1Homo sapiens (human)
regulation of membrane depolarizationNeurotensin receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeurotensin receptor type 1Homo sapiens (human)
neuropeptide signaling pathwayNeurotensin receptor type 1Homo sapiens (human)
chemical synaptic transmissionNeurotensin receptor type 1Homo sapiens (human)
learningNeurotensin receptor type 1Homo sapiens (human)
adult locomotory behaviorNeurotensin receptor type 1Homo sapiens (human)
positive regulation of glutamate secretionNeurotensin receptor type 1Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionNeurotensin receptor type 1Homo sapiens (human)
response to lipidNeurotensin receptor type 1Homo sapiens (human)
positive regulation of apoptotic processNeurotensin receptor type 1Homo sapiens (human)
negative regulation of apoptotic processNeurotensin receptor type 1Homo sapiens (human)
regulation of respiratory gaseous exchangeNeurotensin receptor type 1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painNeurotensin receptor type 1Homo sapiens (human)
negative regulation of release of sequestered calcium ion into cytosolNeurotensin receptor type 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolNeurotensin receptor type 1Homo sapiens (human)
positive regulation of inositol phosphate biosynthetic processNeurotensin receptor type 1Homo sapiens (human)
D-aspartate import across plasma membraneNeurotensin receptor type 1Homo sapiens (human)
inositol phosphate catabolic processNeurotensin receptor type 1Homo sapiens (human)
positive regulation of arachidonic acid secretionNeurotensin receptor type 1Homo sapiens (human)
positive regulation of inhibitory postsynaptic potentialNeurotensin receptor type 1Homo sapiens (human)
L-glutamate import across plasma membraneNeurotensin receptor type 1Homo sapiens (human)
ossificationSortilinHomo sapiens (human)
protein targeting to lysosomeSortilinHomo sapiens (human)
Golgi to endosome transportSortilinHomo sapiens (human)
endocytosisSortilinHomo sapiens (human)
G protein-coupled receptor signaling pathwaySortilinHomo sapiens (human)
neuropeptide signaling pathwaySortilinHomo sapiens (human)
endosome to lysosome transportSortilinHomo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsSortilinHomo sapiens (human)
regulation of gene expressionSortilinHomo sapiens (human)
myotube differentiationSortilinHomo sapiens (human)
vesicle organizationSortilinHomo sapiens (human)
endosome transport via multivesicular body sorting pathwaySortilinHomo sapiens (human)
response to insulinSortilinHomo sapiens (human)
nerve growth factor signaling pathwaySortilinHomo sapiens (human)
negative regulation of fat cell differentiationSortilinHomo sapiens (human)
glucose importSortilinHomo sapiens (human)
neurotrophin TRK receptor signaling pathwaySortilinHomo sapiens (human)
plasma membrane to endosome transportSortilinHomo sapiens (human)
negative regulation of lipoprotein lipase activitySortilinHomo sapiens (human)
Golgi to lysosome transportSortilinHomo sapiens (human)
maintenance of synapse structureSortilinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityNeurotensin receptor type 2Homo sapiens (human)
G protein-coupled neurotensin receptor activityNeurotensin receptor type 2Homo sapiens (human)
G protein-coupled receptor activityNeurotensin receptor type 1Homo sapiens (human)
protein bindingNeurotensin receptor type 1Homo sapiens (human)
G protein-coupled neurotensin receptor activityNeurotensin receptor type 1Homo sapiens (human)
identical protein bindingNeurotensin receptor type 1Homo sapiens (human)
protein-containing complex bindingNeurotensin receptor type 1Homo sapiens (human)
G protein-coupled receptor activityNeurotensin receptor type 2Homo sapiens (human)
G protein-coupled neurotensin receptor activityNeurotensin receptor type 2Homo sapiens (human)
G protein-coupled receptor activityNeurotensin receptor type 1Homo sapiens (human)
protein bindingNeurotensin receptor type 1Homo sapiens (human)
G protein-coupled neurotensin receptor activityNeurotensin receptor type 1Homo sapiens (human)
identical protein bindingNeurotensin receptor type 1Homo sapiens (human)
protein-containing complex bindingNeurotensin receptor type 1Homo sapiens (human)
protein bindingSortilinHomo sapiens (human)
nerve growth factor receptor activitySortilinHomo sapiens (human)
enzyme bindingSortilinHomo sapiens (human)
neurotensin receptor activity, non-G protein-coupledSortilinHomo sapiens (human)
nerve growth factor bindingSortilinHomo sapiens (human)
retromer complex bindingSortilinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
plasma membraneNeurotensin receptor type 2Homo sapiens (human)
plasma membraneNeurotensin receptor type 2Homo sapiens (human)
endoplasmic reticulumNeurotensin receptor type 1Homo sapiens (human)
Golgi apparatusNeurotensin receptor type 1Homo sapiens (human)
plasma membraneNeurotensin receptor type 1Homo sapiens (human)
cytoplasmic side of plasma membraneNeurotensin receptor type 1Homo sapiens (human)
cell surfaceNeurotensin receptor type 1Homo sapiens (human)
symmetric synapseNeurotensin receptor type 1Homo sapiens (human)
terminal boutonNeurotensin receptor type 1Homo sapiens (human)
dendritic spineNeurotensin receptor type 1Homo sapiens (human)
dendritic shaftNeurotensin receptor type 1Homo sapiens (human)
perikaryonNeurotensin receptor type 1Homo sapiens (human)
membrane raftNeurotensin receptor type 1Homo sapiens (human)
plasma membraneNeurotensin receptor type 1Homo sapiens (human)
plasma membraneNeurotensin receptor type 2Homo sapiens (human)
plasma membraneNeurotensin receptor type 2Homo sapiens (human)
endoplasmic reticulumNeurotensin receptor type 1Homo sapiens (human)
Golgi apparatusNeurotensin receptor type 1Homo sapiens (human)
plasma membraneNeurotensin receptor type 1Homo sapiens (human)
cytoplasmic side of plasma membraneNeurotensin receptor type 1Homo sapiens (human)
cell surfaceNeurotensin receptor type 1Homo sapiens (human)
symmetric synapseNeurotensin receptor type 1Homo sapiens (human)
terminal boutonNeurotensin receptor type 1Homo sapiens (human)
dendritic spineNeurotensin receptor type 1Homo sapiens (human)
dendritic shaftNeurotensin receptor type 1Homo sapiens (human)
perikaryonNeurotensin receptor type 1Homo sapiens (human)
membrane raftNeurotensin receptor type 1Homo sapiens (human)
plasma membraneNeurotensin receptor type 1Homo sapiens (human)
lysosomeSortilinHomo sapiens (human)
lysosomal membraneSortilinHomo sapiens (human)
early endosomeSortilinHomo sapiens (human)
endoplasmic reticulum membraneSortilinHomo sapiens (human)
Golgi apparatusSortilinHomo sapiens (human)
cytosolSortilinHomo sapiens (human)
plasma membraneSortilinHomo sapiens (human)
clathrin-coated pitSortilinHomo sapiens (human)
cell surfaceSortilinHomo sapiens (human)
endosome membraneSortilinHomo sapiens (human)
membraneSortilinHomo sapiens (human)
clathrin-coated vesicleSortilinHomo sapiens (human)
trans-Golgi network transport vesicleSortilinHomo sapiens (human)
cytoplasmic vesicleSortilinHomo sapiens (human)
nuclear membraneSortilinHomo sapiens (human)
Golgi cisterna membraneSortilinHomo sapiens (human)
perinuclear region of cytoplasmSortilinHomo sapiens (human)
cerebellar climbing fiber to Purkinje cell synapseSortilinHomo sapiens (human)
membraneSortilinHomo sapiens (human)
Golgi apparatusSortilinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (120)

Assay IDTitleYearJournalArticle
AID1409816Half life in rat plasma by UPLC-MS analysis2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
In Search of the Optimal Macrocyclization Site for Neurotensin.
AID1510634Stability in human plasma assessed as half life at 100 uM by LC-HRMS analysis
AID1385377Half life in rat plasma by UPLC-MS analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13).
AID1385380Agonist activity at GFP10/beta-arrestin1-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin1 recruitment after 20 mins by BRET assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13).
AID1482088Selectivity ratio of Ki for human NTS1 receptor expressed in CHOK1 cell membrane to Ki for human NTS2 receptor expressed in human 1321N1 cell membranes
AID1890925Displacement of [3H]NT(8-13) from human NTSR2 expressed in HEK293 cell membranes by radioligand displacement assay2022Bioorganic & medicinal chemistry, 05-01, Volume: 61Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors.
AID1482086Displacement of 125I-[Tyr3]-NT from human NTS1 receptor expressed in CHOK1 cell membranes after 30 mins by gamma counting analysis
AID1289935Agonist activity at NTSR1 in human HT-29 cells assessed as induction of intracellular Ca2+ mobilization by fura-2 dye-based spectrofluorimetric analysis2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.
AID1482093Selectivity ratio of Ki for HA-tagged human NTS1 R212E mutant receptor expressed in HEK293 cell membranes to Ki for human NTS1 receptor expressed in CHOK1 cell membranes
AID1289933Drug degradation in human HT-29 cells at 50 uM after 2 hrs by reversed-phase HPLC analysis2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.
AID1289937Displacement of [3H]-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-Arg-ProTyr-Ile-Leu-OH Tris(hydrotrifluoroacetate) from NTSR1 in human HT-29 cells after 2 hrs by liquid scintillation counting2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.
AID1731237Stability of compound in rat plasma assessed as half life at 1 mM incubated for 1 to 20 mins by UPLC-MS analysis
AID1731260Cardiotoxicity in Sprague-Dawley rat assessed as decrease in mean arterial blood pressure at 0.1 mg/kg, iv measured up to 1000 seconds
AID1510628Stability in human plasma assessed as percentage intact peptide at 100 uM incubated for 30 mins by LC-HRMS analysis
AID1697049Agonist activity at human NTS1 expressed in HEK293 cells co-expressing Galphaq/RlucII/GFP10-Ggamma1/Gbeta1 assessed as increase in Gq activation incubated for 10 mins in presence of coelenterazine 400A by BRET assay relative to NT (8-13)2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
AID1541740Displacement of [3H] UR-MK300 from human neurotensin receptor 2 in HEK293 cells homogenate incubated in dark after 30 mins by liquid scintillation counter analysis2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.
AID1251024Displacement of [125I]-Tyr3-NT from human NTS2 receptor expressed in 1321N1 cell membranes incubated for 30 mins by gamma-counting based competitive radioligand binding assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.
AID1182263Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).
AID1697038Selectivity ratio of Ki for human recombinant NTS2 expressed in human 1321N1 cell membranes to Ki for human recombinant NTS1 expressed in CHO-K1 cell membranes incubated for 60 mins by gamma counter method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
AID1251026Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing hNTS1-GFP10/RlucII-beta-arrestin 2 assessed as beta-arrestin2 recruitment incubated for 15 mins by BRET assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.
AID1890924Displacement of [3H]neurotensin from human NTSR1 expressed in CHO cell membranes by radioligand depletion assay2022Bioorganic & medicinal chemistry, 05-01, Volume: 61Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors.
AID1541730Agonist activity at human neurotensin receptor 1 expressed in CHO cells assessed as increase in intracellular calcium by Fluo-4 dye based fluorescence assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.
AID1697037Displacement of [125I]-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
AID1510626Displacement of [3H]UR-MK300 from human NSTR1 in HT-29 cells incubated for 2 hrs by liquid scintillation counter
AID1541732Binding affinity to human neurotensin receptor 12020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.
AID1510629Stability in human plasma assessed as percentage intact peptide at 100 uM incubated for 1 hr by LC-HRMS analysis
AID1289949Displacement of [3H]NT(8 to 13 residues) from human NTSR2 expressed in HEK293 cell membranes2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Mimicking of Arginine by Functionalized N(ω)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.
AID1332007Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
NTS2-selective neurotensin mimetics with tetrahydrofuran amino acids.
AID1510631Stability in human plasma assessed as percentage intact peptide at 100 uM incubated for 6 hrs by LC-HRMS analysis
AID1385378Agonist activity at Galphaq-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galphaq activation after 5 mins by BRET assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13).
AID1731265Myorelaxant activity in Sprague-Dawley rat ileum assessed as reduction in carbachol-induced contractions by force transducer relaxation assay
AID1547790Binding affinity to human NTS1R2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
An Alkyne-functionalized Arginine for Solid-Phase Synthesis Enabling "Bioorthogonal" Peptide Conjugation.
AID1541736Displacement of [3H] UR-MK300 from human neurotensin receptor 1 stably expressed in CHO cells incubated in dark after 30 mins by liquid scintillation counter analysis2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.
AID1385381Agonist activity at GFP10/beta-arrestin2-Rluc2 fused human NTS1 expressed in CHO-K1 cell membranes assessed as beta-arrestin2 recruitment after 20 mins by BRET assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13).
AID1890926Displacement of [3H]NT(8-13) from human NTSR1 F2.65C mutant expressed in HEK293 cell membranes by radioligand displacement assay2022Bioorganic & medicinal chemistry, 05-01, Volume: 61Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors.
AID1332008Displacement of [leucine-3H]NT (8 to 13 residues) from human NTS2 receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
NTS2-selective neurotensin mimetics with tetrahydrofuran amino acids.
AID1510627Stability in human plasma assessed as percentage intact peptide at 100 uM incubated for 10 mins by LC-HRMS analysis
AID1385379Agonist activity at Galpha13-Rluc2/Gbeta1/GFP10-Ggamma1 fused human NTS1 expressed in CHO-K1 cell membranes assessed as Galpha13 activation after 5 mins by BRET assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13).
AID1251022Half life in rat plasma at 0.156 mM by UPLC/MS method2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.
AID1482091Displacement of 125I-[Tyr3]-NT from HA-tagged human NTS1 R212E mutant receptor expressed in HEK293 cell membranes after 30 mins by gamma counting analysis
AID1510632Stability in human plasma assessed as percentage intact peptide at 100 uM incubated for 24 hrs by LC-HRMS analysis
AID1409813Displacement of 125I-[Tyr3]-NT from human NTS1 receptor expressed in CHO-K1 cell membranes after 60 mins by gamma-counting method2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
In Search of the Optimal Macrocyclization Site for Neurotensin.
AID1890928Displacement of [3H]NT(8-13) from human NTSR1 F2.65C mutant expressed in HEK293 cell membranes assessed as amount of blocking at 10 nM incubated for 120 mins by radioligand depletion assay2022Bioorganic & medicinal chemistry, 05-01, Volume: 61Development of disulfide-functionalized peptides covalently binding G protein-coupled receptors.
AID1510630Stability in human plasma assessed as percentage intact peptide at 100 uM incubated for 2 hrs by LC-HRMS analysis
AID1482087Displacement of 125I-[Tyr3]-NT from human NTS2 receptor expressed in human 1321N1 cell membranes after 30 mins by gamma counting analysis
AID1385376Displacement of [125I]Tyr3-neurotensin from human NTS1 receptor expressed in CHOK1 cell membranes after 60 mins by gamma counting analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8-13).
AID1541735Displacement of [3H] UR-MK300 from human neurotensin receptor 1 expressed in HT-29 cells incubated in dark after 30 mins by liquid scintillation counter analysis2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.
AID1251025Agonist activity at human NTS1 receptor expressed in CHOK1 cells co-expressing Galphaq-RlucII(121)/Gbeta1/GFP10-Ggamma1 assessed as Galpha-q stimulation incubated for 15 mins by BRET assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.
AID1182264Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay relative to NT(8-13) peptide2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).
AID1251023Displacement of [125I]-Tyr3-NT from human NTS1 receptor expressed in CHOK1 cell membranes incubated for 30 mins by gamma-counting based competitive radioligand binding assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.
AID1731238Stability of compound in rat CSF assessed as half life at 1 mM incubated for 24 hrs by UPLC-MS analysis
AID1251028Reduction in arterial blood pressure in Sprague-Dawley rat at 0.1 mg/kg, iv measured over 4 mins2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.
AID1697048Agonist activity at human NTS1 expressed in HEK293 cells co-expressing Galphaq/RlucII/GFP10-Ggamma1/Gbeta1 assessed as increase in Galphaq activation incubated for 10 mins in presence of coelenterazine 400A by BRET assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
AID1541731Agonist activity at human neurotensin receptor 1 in HT-29 cells assessed as intracellular calcium mobilization by Fura-2 dye based spectrofluorimetry analysis2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.
AID1510633Stability in human plasma assessed as percentage intact peptide at 100 uM incubated for 48 hrs by LC-HRMS analysis
AID1697036Displacement of [125I]-neurotensin from human recombinant NTS1 stably expressed in CHO-K1 cell membranes incubated for 60 mins by gamma counter method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
AID1251027Agonist activity at human NTS1 in Sprague-Dawley rat ileum assessed as inhibition of carbachol-induced contraction2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.
AID1161613Agonist activity at rat NTS2 receptor expressed in CHO-K1 cells assessed as calcium mobilization by FLIPR assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.
AID1731236Selectivity index, ratio of Ki for displacement of [125I]Tyr3-neurotensin from human recombinant NTS2 to Ki for displacement of [125I]Tyr3-neurotensin from human recombinant NTS1
AID593495Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.
AID1154141Antagonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as inhibition of SR142948a-induced calcium release by FLIPR assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID1149941Retention time of the compound in 0.01 M NH4OAc buffer at pH 4.5 by HPLC analysis1977Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
Neurotensin analogues. Structure--activity relationships.
AID1176213Antagonist activity at rat neurotensin receptor type 2 expressed in CHOK1 cells assessed as inhibition of SR142948a-induced calcium release by FLIPR assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
AID1154139Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID414527Agonist activity at human NTR1 assessed as increase in intracellular calcium concentration2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.
AID326478Displacement of [125I]Tyr3NT from human NTS2 receptor expressed in COS7 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis and biological effects of c(Lys-Lys-Pro-Tyr-Ile-Leu-Lys-Lys-Pro-Tyr-Ile-Leu) (JMV2012), a new analogue of neurotensin that crosses the blood-brain barrier.
AID346439Displacement of radiolabeled neurotensin from human neurotensin receptor 12008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID1731234Displacement of [125I]Tyr3-neurotensin from human recombinant NTS1 stably expressed in CHO-K1 cell membranes incubated for 60 mins by gamma counter analysis
AID1161614Antagonist activity at rat NTS2 receptor expressed in CHO-K1 cells assessed as inhibition of SR142948a-induced calcium mobilization by FLIPR assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.
AID1176215Displacement of [125L]NT from rat neurotensin receptor type 2 expressed in CHOK1 cells by radioligand binding assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
AID268353Displacement of [125I]Tyr3-NT from human NTS1R expressed in HT29 cells2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Toward stable N4-modified neurotensins for NTS1-receptor-targeted tumor imaging with 99mTc.
AID418186Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.
AID1161616Displacement of [125I]neurotensin from rat NTS2 receptor expressed in CHO-K1 cells by competitive binding assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.
AID752198Binding affinity to NTS1 receptor (unknown origin) by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID1541732Binding affinity to human neurotensin receptor 12020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.
AID1154142Displacement of [125I]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma counting2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID1285644Displacement of [125I]Tyr3-neurotensin from human recombinant NT1 receptor expressed in CHO cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID349181Agonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as increase in intracellular calcium level by FLIPR assay2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
The identification of neurotensin NTS1 receptor partial agonists through a ligand-based virtual screening approach.
AID751868Binding affinity to human NTS1 receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID414521Agonist activity at NTR1 in human HT-29 cells assessed as increase in intracellular calcium concentration by FLIPR assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.
AID1176214Displacement of [125L]NT from rat neurotensin receptor type 1 expressed in CHOK1 cells by radioligand binding assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
AID593498Agonist activity at human NTS1 receptor expressed in HEK293 cells assessed as inhibition of constitutive activity on MAPK-mediated luciferase activity2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.
AID268354Displacement of [125I]Tyr3-NT from human NTS1R expressed in WiDr cells2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Toward stable N4-modified neurotensins for NTS1-receptor-targeted tumor imaging with 99mTc.
AID314665Agonist activity at NTR1 assessed as effect on intracellular calcium accumulation relative to neurotensin by cell based assay2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Peptide backbone modifications on the C-terminal hexapeptide of neurotensin.
AID340256Inhibition of human NTS1 receptor2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID147045Binding affinity towards neurotensin receptor in membranes prepared from HT-29 cell line, relative to [111In]-labeled neurotensin peptide2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Novel bioactive and stable neurotensin peptide analogues capable of delivering radiopharmaceuticals and molecular beacons to tumors.
AID414520Displacement of [125I]I-Tyr(3)NT from human NTR12009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.
AID349183Antagonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as inhibition of intracellular calcium elevation pretreated 30 mins before with SR-48692 by FLIPR assay2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
The identification of neurotensin NTS1 receptor partial agonists through a ligand-based virtual screening approach.
AID388349Displacement of [3H]NT(8-13) from wild type human NTR1 expressed in HEK293 cells2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensin receptor 1.
AID1061981Displacement of [3H]-neurotensin from human sortilin incubated 30 mins prior to [3H]-neurotensin addition measured after 6 hrs by scintillation proximity assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin.
AID414528Agonist activity at NTR1 in mouse N1E-115 cells assessed as increase in intracellular calcium concentration2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy.
AID326477Displacement of [125I]Tyr3NT from human NTS1 receptor expressed in COS7 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Synthesis and biological effects of c(Lys-Lys-Pro-Tyr-Ile-Leu-Lys-Lys-Pro-Tyr-Ile-Leu) (JMV2012), a new analogue of neurotensin that crosses the blood-brain barrier.
AID196904Relative potency expressed in percent to that of neurotensin was measured using perfused rat heart assay1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Synthesis of peptides by the solid-phase method. 6. Neurotensin, fragments, and analogues.
AID593500Agonist activity at human NTS2 receptor expressed in HEK293 cells assessed as inhibition of constitutive activity on MAPK-mediated luciferase activity2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.
AID349182Agonist activity at human NTS1 receptor expressed in CHOK1 cells assessed as increase in intracellular calcium level by FLIPR assay relative to neurotensin2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
The identification of neurotensin NTS1 receptor partial agonists through a ligand-based virtual screening approach.
AID1731235Displacement of [125I]Tyr3-neurotensin from human recombinant NTS2 stably expressed in human 1321N1 cell membranes incubated for 60 mins by gamma counter analysis
AID418187Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay relative to neurotensin2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.
AID314664Displacement of [3H]neurotensin from pig NTR12008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Peptide backbone modifications on the C-terminal hexapeptide of neurotensin.
AID1055239Displacement of [3H]NT(8 to 13) from human NTS2 receptor expressed in HEK293 cells2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors.
AID593497Selectivity ratio of Ki for human NTS1 to Ki for human NTS22011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.
AID196425Relative potency expressed in percent to that of neurotensin was measured using rat stomach strips assay1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Synthesis of peptides by the solid-phase method. 6. Neurotensin, fragments, and analogues.
AID1161615Displacement of [125I]neurotensin from rat NTS1 receptor expressed in CHO-K1 cells by competitive binding assay2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.
AID80754Relative potency expressed in percent to that of neurotensin was measured using guinea pig atria1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Synthesis of peptides by the solid-phase method. 6. Neurotensin, fragments, and analogues.
AID1176211Agonist activity at rat neurotensin receptor type 2 expressed in CHOK1 cells assessed as increase in calcium release by FLIPR assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
AID1336341Displacement of [125I]Tyr3-neurotensin from human recombinant NTS1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID1154137Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay relative to neurotensin2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID1055241Displacement of [3H]neurotensin from human NTS1 receptor expressed in CHO cells2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors.
AID593496Displacement of [3H]NT from human NTS2 receptor expressed in HEK293 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics.
AID1154136Agonist activity at rat NTS1 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.
AID1346344Human NTS1 receptor (Neurotensin receptors)2000Biochemical pharmacology, Sep-15, Volume: 60, Issue:6
A single amino acid of the human and rat neurotensin receptors (subtype 1) determining the pharmacological profile of a species-selective neurotensin agonist.
AID1346374Mouse NTS2 receptor (Neurotensin receptors)1998Biochemical and biophysical research communications, Feb-13, Volume: 243, Issue:2
Stable expression of the mouse levocabastine-sensitive neurotensin receptor in HEK 293 cell line: binding properties, photoaffinity labeling, and internalization mechanism.
AID1346325Human NTS2 receptor (Neurotensin receptors)2001Molecular pharmacology, Dec, Volume: 60, Issue:6
Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2.
AID1346344Human NTS1 receptor (Neurotensin receptors)2001Molecular pharmacology, Dec, Volume: 60, Issue:6
Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2.
AID1346391Rat NTS1 receptor (Neurotensin receptors)2000Biochemical pharmacology, Sep-15, Volume: 60, Issue:6
A single amino acid of the human and rat neurotensin receptors (subtype 1) determining the pharmacological profile of a species-selective neurotensin agonist.
AID1346315Rat NTS2 receptor (Neurotensin receptors)1999The Journal of biological chemistry, May-14, Volume: 274, Issue:20
Contulakin-G, an O-glycosylated invertebrate neurotensin.
AID1346391Rat NTS1 receptor (Neurotensin receptors)2003Molecular pharmacology, Aug, Volume: 64, Issue:2
Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: a molecular basis for agonist-directed trafficking of receptor stimulus.
AID1346391Rat NTS1 receptor (Neurotensin receptors)1998The Journal of biological chemistry, Jun-26, Volume: 273, Issue:26
Mutagenesis and modeling of the neurotensin receptor NTR1. Identification of residues that are critical for binding SR 48692, a nonpeptide neurotensin antagonist.
AID1346374Mouse NTS2 receptor (Neurotensin receptors)1996The Journal of neuroscience : the official journal of the Society for Neuroscience, Sep-15, Volume: 16, Issue:18
Structure, functional expression, and cerebral localization of the levocabastine-sensitive neurotensin/neuromedin N receptor from mouse brain.
AID1346315Rat NTS2 receptor (Neurotensin receptors)1996FEBS letters, May-20, Volume: 386, Issue:2-3
Molecular cloning of a levocabastine-sensitive neurotensin binding site.
AID1346391Rat NTS1 receptor (Neurotensin receptors)1995Molecular pharmacology, May, Volume: 47, Issue:5
[3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,824)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901433 (37.47)18.7374
1990's1174 (30.70)18.2507
2000's612 (16.00)29.6817
2010's475 (12.42)24.3611
2020's130 (3.40)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 49.09

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index49.09 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index72.23 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (49.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Trials45 (1.11%)5.53%
Reviews0 (0.00%)6.00%
Reviews0 (0.00%)6.00%
Reviews301 (7.42%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Case Studies28 (0.69%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Observational4 (0.10%)0.25%
Other13 (100.00%)84.16%
Other7 (100.00%)84.16%
Other3,676 (90.68%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]