Page last updated: 2024-12-10

bibp 3226

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Description

BIBP 3226: a selective non-peptide neuropeptide Y Y1 receptor antagonist; structure given in first source; BIBP-3435 is the S-enantiomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311023
CHEMBL ID332347
SCHEMBL ID650331
MeSH IDM0245205

Synonyms (27)

Synonym
gtpl1485
(2r)-5-(diaminomethylideneamino)-2-[[2,2-di(phenyl)acetyl]amino]-n-[(4-hydroxyphenyl)methyl]pentanamide
bibp3226
bibp 3226
CHEMBL332347 ,
bibp-3226
(2r)-5-(diaminomethylideneamino)-2-[(2,2-diphenylacetyl)amino]-n-[(4-hydroxyphenyl)methyl]pentanamide
(r)-2-diphenylacetylamino-5-guanidino-pentanoic acid 4-hydroxy-benzylamide
(r)-5-(diaminomethyleneamino)-2-(2,2-diphenylacetamido)-n-(4-hydroxybenzyl)pentanamide
bdbm50060728
(r)-2-(2,2-diphenylacetamido)-5-guanidino-n-(4-hydroxybenzyl)pentanamide
159013-54-4
[3h]bibp3226
[3h]-bibp3226
gtpl3474
SCHEMBL650331
n-[(1r)]-4-[(aminoiminomethyl)amino-1-[[[(4-hydroxyphenyl)methyl]amino]carbonyl]butyl-?-phenylbenzeneacetamide
DTXSID30415502
n-[(1r)]-4-[(aminoiminomethyl)amino-1-[[[(4-hydroxyphenyl)methyl]amino]carbonyl]butyl-alpha-phenylbenzeneacetamide trifluoroacetate
Q4835633
AKOS034831590
(2r)-5-carbamimidamido-2-(2,2-diphenylethanoylamino)-n-((4-hydroxyphenyl)methyl)pentanamide
rg9766ugz8 ,
HY-107726A
CS-0078220
n-[(1r)-4-[(aminoiminomethyl)amino]-1-[[[(4-hydroxyphenyl)methyl]amino]carbonyl]butyl]-alpha-phenylbenzeneacetamide
benzeneacetamide, n-[(1r)-4-[(aminoiminomethyl)amino]-1-[[[(4-hydroxyphenyl)methyl]amino]carbonyl]butyl]-alpha-phenyl-

Research Excerpts

Effects

ExcerptReferenceRelevance
"BIBP 3226 has a similar effect on nicotinic receptor-stimulated 45Ca2+ influx."( BIBP 3226 inhibition of nicotinic receptor mediated chromaffin cell secretion.
Hexum, TD; Zhang, P; Zheng, J, 1998
)
2.46
"BIBP 3226 has a similar effect on nicotinic receptor-stimulated 45Ca2+ influx."( BIBP 3226 inhibition of nicotinic receptor mediated chromaffin cell secretion.
Hexum, TD; Zhang, P; Zheng, J, 1998
)
2.46

Actions

ExcerptReferenceRelevance
"BIBP 3226 does not inhibit [3H]norepinephrine release induced by high K+ and its effect is not pertussis toxin-sensitive."( BIBP 3226 inhibition of nicotinic receptor mediated chromaffin cell secretion.
Hexum, TD; Zhang, P; Zheng, J, 1998
)
2.46

Treatment

ExcerptReferenceRelevance
"Both BIBP 3226 and BIIE 0246 treatment reversed the elevated total cholesterol (TC) and low density lipoprotein (LDL-C) level, and reduced high density lipoprotein (HDL-C) level in DM rats. "( Blockage of peripheral NPY Y1 and Y2 receptors modulates barorefex sensitivity of diabetic rats.
Ai, J; Cai, BZ; Chen, QX; Liu, J; Sun, LH; Wang, N; Xie, F; Yang, BF; Ye, JH, 2013
)
0.9

Compound-Compound Interactions

ExcerptReferenceRelevance
"Folic acid is antidepressant, either alone or combined with several antidepressant drugs."( Fluoxetine, 17-β estradiol or folic acid combined with intra-lateral septal infusions of neuropeptide Y produced antidepressant-like actions in ovariectomized rats forced to swim.
Molina-Hernández, M; Téllez-Alcántara, NP, 2011
)
0.37

Dosage Studied

increasing concentrations (10(-9)-10(-6) M) of the Y1 receptor antagonist, BIBP 3226, to human cerebral vessels caused a parallel and rightward shift in the NPY dose-response curves. There was no significant change in the maximal contractile response.

ExcerptRelevanceReference
" Increasing concentrations (10(-9)-10(-6) M) of the Y1 receptor antagonist, BIBP 3226, to human cerebral vessels caused a parallel and rightward shift in the NPY dose-response curves without any significant change in the maximal contractile response."( Characterization of neuropeptide Y (NPY) receptors in human cerebral arteries with selective agonists and the new Y1 antagonist BIBP 3226.
Abounader, R; Hamel, E; Villemure, JG, 1995
)
0.73
" Increasing concentrations (10(-9) - 10(-6) M) of BIBP 3226 caused a parallel and rightward shift in the neuropeptide Y dose-response curve but did not significantly change the effect of noradrenaline."( Neuropeptide Y accounts for sympathetic vasoconstriction in guinea-pig vena cava: evidence using BIBP 3226 and 3435.
Lundberg, JM; Malmstrom, RE, 1995
)
0.76
" The dose-response curves obtained with neuropeptide Y, peptide YY and with C-terminal fragments such as neuropeptide Y-(2-26), neuropeptide Y-(13-36) and peptide YY-(3-36) have similar slopes and maxima."( The dog saphenous vein: a sensitive and selective preparation for the Y2 receptor of neuropeptide Y.
Dumont, Y; Fournier, A; Pheng, LH; Quirion, R; Regoli, D, 1997
)
0.3
" Furthermore, 5 microM BIBP-3226, a Y1-receptor antagonist, shifted both dose-response curves to the right in a similar fashion for both peptides."( Human syncytiotrophoblast NPY receptors are located on BBM and activate PLC-to-PKC axis.
Ech-Chadli, H; Lafond, J; Robidoux, J; Simoneau, L; St-Pierre, S, 1998
)
0.3
" However, in renovascular Goldblatt hypertensive rats, the dose-response curves for both NPY and NA were significantly displaced to the left, approximately threefold."( Increased neuropeptide Y pressor activity in Goldblatt hypertensive rats: in vivo studies with BIBP 3226.
Capurro, D; Donoso, V; Huidobro-Toro, JP; Mezzano, V, 1998
)
0.52
" [Leu31 Pro34]-rNPY (agonist potency: Y1 > Y5 > Y4 = y6) and human pancreatic polypeptide (hPP) produced flatter dose-response curves, suggesting partial agonism at the receptor(s)."( Characterisation of the neuropeptide Y receptor that mediates feeding in the rat: a role for the Y5 receptor?
Arch, JR; Buckingham, RE; Haynes, AC; McClue, S; Wilson, S, 1998
)
0.3
"5 fold rightward the pressor dose-response curve elicited by exogenous neuropeptide Y, without altering the norepinephrine curve."( The involvement of neuropeptide Y Y1 receptors in the blood pressure baroreflex: studies with BIBP 3226 and BIBO 3304.
Capurro, D; Huidobro-Toro, JP, 1999
)
0.52
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki10.00000.00000.12345.5000AID146605
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki10.00000.00000.10825.5000AID146605
Neuropeptide Y receptor type 1Homo sapiens (human)IC50 (µMol)0.00910.00020.70318.3700AID1266459; AID1266462; AID1266463; AID1266496; AID414235; AID468183
Neuropeptide Y receptor type 1Homo sapiens (human)Ki0.19560.00010.22952.3150AID1266456; AID1266471; AID1266474; AID146581; AID146583; AID389949; AID414234; AID414235; AID502229; AID597409; AID597411; AID779933
Neuropeptide Y receptor type 2Homo sapiens (human)Ki10.00000.00010.00260.0050AID146605
Neuropeptide Y receptor type 4Homo sapiens (human)Ki7.50000.00040.00040.0004AID146737; AID779932
Neuropeptide Y receptor type 5Homo sapiens (human)Ki10.00000.00151.66775.0000AID146882
Neuropeptide FF receptor 1Homo sapiens (human)Ki0.01500.00010.02070.0580AID1266467; AID1266479
Neuropeptide FF receptor 2Homo sapiens (human)Ki0.16700.00000.05970.2500AID1266468; AID1266480
[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)
Neuropeptide Y receptor type 1Homo sapiens (human)Kd0.00210.00210.00210.0021AID1266454
Neuropeptide FF receptor 1Homo sapiens (human)Kd0.02090.00110.01100.0209AID698092
Neuropeptide FF receptor 2Homo sapiens (human)EC50 (µMol)0.17300.00270.19260.6120AID697926; AID698097
[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)
Neuropeptide Y receptor type 1Homo sapiens (human)Kb0.00150.00150.00210.0045AID389948; AID502228; AID597410; AID779930
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (27)

Processvia Protein(s)Taxonomy
outflow tract morphogenesisNeuropeptide Y receptor type 1Homo sapiens (human)
glucose metabolic processNeuropeptide Y receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerNeuropeptide Y receptor type 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide Y receptor type 1Homo sapiens (human)
locomotory behaviorNeuropeptide Y receptor type 1Homo sapiens (human)
feeding behaviorNeuropeptide Y receptor type 1Homo sapiens (human)
regulation of blood pressureNeuropeptide Y receptor type 1Homo sapiens (human)
sensory perception of painNeuropeptide Y receptor type 1Homo sapiens (human)
regulation of multicellular organism growthNeuropeptide Y receptor type 1Homo sapiens (human)
outflow tract morphogenesisNeuropeptide Y receptor type 2Homo sapiens (human)
cardiac left ventricle morphogenesisNeuropeptide Y receptor type 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayNeuropeptide Y receptor type 2Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide Y receptor type 2Homo sapiens (human)
locomotory behaviorNeuropeptide Y receptor type 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuropeptide Y receptor type 4Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide Y receptor type 4Homo sapiens (human)
positive regulation of acute inflammatory responseNeuropeptide Y receptor type 5Homo sapiens (human)
negative regulation of acute inflammatory response to antigenic stimulusNeuropeptide Y receptor type 5Homo sapiens (human)
outflow tract morphogenesisNeuropeptide Y receptor type 5Homo sapiens (human)
cardiac left ventricle morphogenesisNeuropeptide Y receptor type 5Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide Y receptor type 5Homo sapiens (human)
negative regulation of glutamate secretionNeuropeptide Y receptor type 5Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicNeuropeptide Y receptor type 5Homo sapiens (human)
eating behaviorNeuropeptide Y receptor type 5Homo sapiens (human)
negative regulation of apoptotic processNeuropeptide Y receptor type 5Homo sapiens (human)
positive regulation of smooth muscle cell proliferationNeuropeptide Y receptor type 5Homo sapiens (human)
generation of ovulation cycle rhythmNeuropeptide Y receptor type 5Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeNeuropeptide Y receptor type 5Homo sapiens (human)
synaptic signaling via neuropeptideNeuropeptide Y receptor type 5Homo sapiens (human)
chemical synaptic transmissionNeuropeptide Y receptor type 5Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuropeptide Y receptor type 5Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide FF receptor 1Homo sapiens (human)
biological_processNeuropeptide FF receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuropeptide FF receptor 1Homo sapiens (human)
cellular response to hormone stimulusNeuropeptide FF receptor 1Homo sapiens (human)
neuropeptide signaling pathwayNeuropeptide FF receptor 2Homo sapiens (human)
detection of abiotic stimulusNeuropeptide FF receptor 2Homo sapiens (human)
regulation of MAPK cascadeNeuropeptide FF receptor 2Homo sapiens (human)
cellular response to hormone stimulusNeuropeptide FF receptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayNeuropeptide FF receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
peptide YY receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
pancreatic polypeptide receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide Y receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
protein bindingNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide receptor activityNeuropeptide Y receptor type 1Homo sapiens (human)
neuropeptide bindingNeuropeptide Y receptor type 1Homo sapiens (human)
peptide YY receptor activityNeuropeptide Y receptor type 2Homo sapiens (human)
neuropeptide Y receptor activityNeuropeptide Y receptor type 2Homo sapiens (human)
calcium channel regulator activityNeuropeptide Y receptor type 2Homo sapiens (human)
protein bindingNeuropeptide Y receptor type 2Homo sapiens (human)
signaling receptor activityNeuropeptide Y receptor type 2Homo sapiens (human)
pancreatic polypeptide receptor activityNeuropeptide Y receptor type 4Homo sapiens (human)
G protein-coupled receptor activityNeuropeptide Y receptor type 4Homo sapiens (human)
peptide hormone bindingNeuropeptide Y receptor type 4Homo sapiens (human)
neuropeptide bindingNeuropeptide Y receptor type 4Homo sapiens (human)
neuropeptide Y receptor activityNeuropeptide Y receptor type 5Homo sapiens (human)
pancreatic polypeptide receptor activityNeuropeptide Y receptor type 5Homo sapiens (human)
peptide YY receptor activityNeuropeptide Y receptor type 5Homo sapiens (human)
neuropeptide bindingNeuropeptide Y receptor type 5Homo sapiens (human)
G protein-coupled receptor activityNeuropeptide FF receptor 1Homo sapiens (human)
protein bindingNeuropeptide FF receptor 1Homo sapiens (human)
neuropeptide receptor activityNeuropeptide FF receptor 1Homo sapiens (human)
peptide bindingNeuropeptide FF receptor 1Homo sapiens (human)
G protein-coupled receptor activityNeuropeptide FF receptor 2Homo sapiens (human)
neuropeptide receptor activityNeuropeptide FF receptor 2Homo sapiens (human)
opioid receptor bindingNeuropeptide FF receptor 2Homo sapiens (human)
peptide bindingNeuropeptide FF receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
plasma membraneNeuropeptide Y receptor type 1Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 1Homo sapiens (human)
neuron projectionNeuropeptide Y receptor type 1Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 2Homo sapiens (human)
ciliumNeuropeptide Y receptor type 2Homo sapiens (human)
non-motile ciliumNeuropeptide Y receptor type 2Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 4Homo sapiens (human)
membraneNeuropeptide Y receptor type 4Homo sapiens (human)
neuron projectionNeuropeptide Y receptor type 4Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 4Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 5Homo sapiens (human)
presynapseNeuropeptide Y receptor type 5Homo sapiens (human)
GABA-ergic synapseNeuropeptide Y receptor type 5Homo sapiens (human)
plasma membraneNeuropeptide Y receptor type 5Homo sapiens (human)
neuron projectionNeuropeptide Y receptor type 5Homo sapiens (human)
plasma membraneNeuropeptide FF receptor 1Homo sapiens (human)
ciliumNeuropeptide FF receptor 1Homo sapiens (human)
plasma membraneNeuropeptide FF receptor 1Homo sapiens (human)
plasma membraneNeuropeptide FF receptor 2Homo sapiens (human)
actin cytoskeletonNeuropeptide FF receptor 2Homo sapiens (human)
plasma membraneNeuropeptide FF receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (58)

Assay IDTitleYearJournalArticle
AID1266478Displacement of Cy5-pNPY from human NPY5R expressed in HEC cells by flow cytometric analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID1266454Binding affinity to NPY1R in human SK-N-MC cells after 2 hrs by liquid scintillation counting assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID1266495Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 300 nM pNPY-induced Ca+2 response preincubated for 15 mins by Fura-2 dye based spectrofluorimetric analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID779931Binding affinity to human neuropeptide Y receptor type 5 receptor expressed in HEC-1B cells using Cy5-pNPY by flow cytometric analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Dimeric argininamide-type neuropeptide Y receptor antagonists: chiral discrimination between Y1 and Y4 receptors.
AID779934Binding affinity to human neuropeptide Y receptor type 2 receptor expressed in CHO cells using Cy5-pNPY by flow cytometric analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Dimeric argininamide-type neuropeptide Y receptor antagonists: chiral discrimination between Y1 and Y4 receptors.
AID698096Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation at 10 uM after 2 hrs by liquid scintillation counting relative to NPFF2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
AID1266458Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response by Fura-2 dye based spectrofluorimetric analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID1266468Binding affinity to human NPFF2 receptor expressed in CHO cells2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID779929Antagonist activity at human neuropeptide Y receptor type 4 expressed in CHO cells co-expressing Gqi5-mtAEQ assessed as inhibition of hPP-induced calcium mobilization by Aequorin assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Dimeric argininamide-type neuropeptide Y receptor antagonists: chiral discrimination between Y1 and Y4 receptors.
AID597410Antagonist activity at Y1R in human HEL cells assessed as inhibition of pNPY induced [Ca2+] mobilisation2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Red-fluorescent argininamide-type NPY Y1 receptor antagonists as pharmacological tools.
AID779932Binding affinity to human neuropeptide Y receptor type 4 receptor expressed in CHO cells using Cy5-[K4]-hPP by flow cytometric analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Dimeric argininamide-type neuropeptide Y receptor antagonists: chiral discrimination between Y1 and Y4 receptors.
AID698094Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as fold decrease in NPVF-induced [3H]inositol phosphate accumulation at 1 uM after 2 hrs by liquid scintillation counting relative to control2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
AID697926Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
AID698093Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as fold decrease in NPVF-induced [3H]inositol phosphate accumulation at 10 uM after 2 hrs by liquid scintillation counting relative to control2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
AID1266474Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells by radioligand binding assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID502230Distribution coefficient, log D of the compound2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
N(G)-Acyl-argininamides as NPY Y(1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity.
AID698097Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
AID1266471Displacement of [3H]UR-MK136 from NPY1R in human SK-N-MC cells by radioligand binding assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID697919Partial agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation at 10 uM after 2 hrs by liquid scintillation counting relative to NPFF2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
AID468183Inhibition of neuropeptide Y1 receptor in human SK-N-MC cells after 60 mins by scintillation counting2009Journal of natural products, Dec, Volume: 72, Issue:12
5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor.
AID1266459Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 secs by Fura-2 dye based spectrofluorimetric analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID597411Displacement of [3H]-UR-MK114 from Y1R in human SK-N-MC cells2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Red-fluorescent argininamide-type NPY Y1 receptor antagonists as pharmacological tools.
AID414234Displacement of [3H]propionyl-pNPY from neuropeptide Y1 receptor in human SK-N-MC cells2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist.
AID1266480Displacement of [3H]EYF from human NPFF2 expressed in CHO cells by radioligand binding assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID1266496Displacement of (R)-Na-Diphenylacetyl-Nomega[2-([2,3-3H]-propionylamino)ethyl]aminocarbonyl (4-hydroxybenzyl)-argininamide from NPY1R in human SK-N-MC cells2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID779930Antagonist activity at neuropeptide Y receptor type 1 in HEL assessed as inhibition of pNPY-induced calcium mobilization by Fura-2 calcium assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Dimeric argininamide-type neuropeptide Y receptor antagonists: chiral discrimination between Y1 and Y4 receptors.
AID1266462Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 5 mins by Fura-2 dye based spectrofluorimetric analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID414235Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist.
AID597409Displacement of radiolabeled NPY from human Y1R expressed in human SK-N-MC cells2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
Red-fluorescent argininamide-type NPY Y1 receptor antagonists as pharmacological tools.
AID698095Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as fold decrease in NPVF-induced [3H]inositol phosphate accumulation at 0.1 uM after 2 hrs by liquid scintillation counting relative to control2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
AID698092Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
AID1266463Antagonist activity at NPY1R in human HEL cells assessed as inhibition of 10 nM pNPY-induced Ca+2 response preincubated for 10 mins by Fura-2 dye based spectrofluorimetric analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID1266477Displacement of Cy5-[K4]hPP from human NPY4R expressed in CHO cells by flow cytometric analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID146581Inhibition of binding of [125I]PYY radioligand to human neuropeptide Y1 receptor in SK-N-MC cell membrane2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
AID146605Affinity for human Neuropeptide Y receptor type 21997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists.
AID1266456Displacement of [3H]propionyl-pNPY from NPY1R in HEL cells after 60 to 90 mins by flow cytometric analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID779933Displacement of [3H]UR-MK114 from human neuropeptide Y receptor type 1 expressed in human SK-N-MC cells2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Dimeric argininamide-type neuropeptide Y receptor antagonists: chiral discrimination between Y1 and Y4 receptors.
AID502228Antagonist activity at NPY1 receptor in human HEL cells assessed as inhibition of NPY-induced calcium mobilization by Fura-2 assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
N(G)-Acyl-argininamides as NPY Y(1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity.
AID1266467Binding affinity to human NPFF1 receptor expressed in CHO cells2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID389948Antagonist activity at NPY Y1 receptor in HEL cells assessed as inhibition of NPY-induced increase in intracellular calcium mobilization by Fura-2 assay2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists.
AID146882Affinity for human Neuropeptide Y receptor type 51997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists.
AID1266479Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID502229Displacement of [3H]UR-MK114 from NPY1 receptor in human SK-N-MC cells2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
N(G)-Acyl-argininamides as NPY Y(1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity.
AID698099Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation up to 10 uM after 2 hrs by liquid scintillation counting2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Selective mode of action of guanidine-containing non-peptides at human NPFF receptors.
AID146737Affinity for human Neuropeptide Y receptor type 41997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists.
AID389949Displacement of NG-([2,3-3H]propionyl)-BIBP-3226 from NPY Y1 receptor in human SK-N-MC cells2008Bioorganic & medicinal chemistry, Nov-15, Volume: 16, Issue:22
Modular synthesis of non-peptidic bivalent NPY Y1 receptor antagonists.
AID146583Binding affinity for Neuropeptide Y receptor type 1 expressed in AV-12 cells1997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists.
AID1266476Displacement of Cy5-pNPY from human NPY2R expressed in CHO cells by flow cytometric analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
N(ω)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.
AID1346317Rat Y1 receptor (Neuropeptide Y receptors)1996British journal of pharmacology, Sep, Volume: 119, Issue:2
The functional investigation of a human adenocarcinoma cell line, stably transfected with the neuropeptide Y Y1 receptor.
AID1346421Human NPFF1 receptor (Neuropeptide FF/neuropeptide AF receptors)2002European journal of pharmacology, Sep-20, Volume: 451, Issue:3
Pharmacological characterization of human NPFF(1) and NPFF(2) receptors expressed in CHO cells by using NPY Y(1) receptor antagonists.
AID1346349Human NPFF2 receptor (Neuropeptide FF/neuropeptide AF receptors)2001British journal of pharmacology, May, Volume: 133, Issue:1
Agonist and antagonist activities on human NPFF(2) receptors of the NPY ligands GR231118 and BIBP3226.
AID1346421Human NPFF1 receptor (Neuropeptide FF/neuropeptide AF receptors)2002Neuroscience, , Volume: 115, Issue:2
Quantitative autoradiographic distribution of NPFF1 neuropeptide FF receptor in the rat brain and comparison with NPFF2 receptor by using [125I]YVP and [(125I]EYF as selective radioligands.
AID1346317Rat Y1 receptor (Neuropeptide Y receptors)1995The Journal of pharmacology and experimental therapeutics, Oct, Volume: 275, Issue:1
Pharmacological characterization of the selective nonpeptide neuropeptide Y Y1 receptor antagonist BIBP 3226.
AID1346423Human Y1 receptor (Neuropeptide Y receptors)1995The Journal of pharmacology and experimental therapeutics, Oct, Volume: 275, Issue:1
Pharmacological characterization of the selective nonpeptide neuropeptide Y Y1 receptor antagonist BIBP 3226.
AID1346317Rat Y1 receptor (Neuropeptide Y receptors)1997Peptides, , Volume: 18, Issue:3
[125I]Leu31, Pro34-PYY is a high affinity radioligand for rat PP1/Y4 and Y1 receptors: evidence for heterogeneity in pancreatic polypeptide receptors.
AID1346421Human NPFF1 receptor (Neuropeptide FF/neuropeptide AF receptors)2000The Journal of biological chemistry, Dec-15, Volume: 275, Issue:50
Identification and characterization of two G protein-coupled receptors for neuropeptide FF.
AID1346423Human Y1 receptor (Neuropeptide Y receptors)1995The Journal of pharmacology and experimental therapeutics, Oct, Volume: 275, Issue:1
Subtype selectivity and antagonistic profile of the nonpeptide Y1 receptor antagonist BIBP 3226.
AID1346349Human NPFF2 receptor (Neuropeptide FF/neuropeptide AF receptors)2000The Journal of biological chemistry, Dec-15, Volume: 275, Issue:50
Identification and characterization of two G protein-coupled receptors for neuropeptide FF.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (245)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's84 (34.29)18.2507
2000's100 (40.82)29.6817
2010's59 (24.08)24.3611
2020's2 (0.82)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.15

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 Index18.15 (24.57)
Research Supply Index5.52 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.15)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (1.61%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other244 (98.39%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]