Page last updated: 2024-11-07

ym 022

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

Description

YM 022: a potent and selective gastrin/cholecystokinin-B receptor antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID122130
CHEMBL ID115121
SCHEMBL ID2870373
MeSH IDM0231168

Synonyms (35)

Synonym
3-(3-methylphenyl)-1-[(3r)-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-3h-1,4-benzodiazepin-3-yl]urea
gtpl888
PDSP1_000902
ym022
PDSP2_000888
NCGC00092280-01
1-(2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl-1h-1,4-benzodiazepin-3-yl)-3-(3-methylphenyl)urea
urea, n-(2,3-dihydro-1-(2-(2-methylphenyl)-2-oxoethyl)-2-oxo-5-phenyl-1h-1,4-benzodiazepin-3-yl)-n'-(3-methylphenyl)-, (r)-
ym 022
ym-022
CHEMBL115121 ,
bdbm50056101
ym022 racemate
1-[(r)-2-oxo-1-(2-oxo-2-o-tolyl-ethyl)-5-phenyl-2,3-dihydro-1h-benzo[e][1,4]diazepin-3-yl]-3-m-tolyl-urea
772cp7w12n ,
unii-772cp7w12n
145084-28-2
(r)-n-[2,3-dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1h-1,4-benzodiazepin-3-yl]-n'-(3-methylphenyl)-urea
SCHEMBL2870373
urea, n-((3r)-2,3-dihydro-1-(2-(2-methylphenyl)-2-oxoethyl)-2-oxo-5-phenyl-1h-1,4-benzodiazepin-3-yl)-n'-(3-methylphenyl)-
AKOS027378207
r-1-(2,3-dihydro-1-(2-methylphenacyl)-2-oxo-5-phenyl-1h-1,4-benzodiazepin-3-yl)-3(3-methylphenyl)urea
YCXFHPUBGMMWJQ-PMERELPUSA-N
ym 022, >=98% (hplc)
J-008051
(r,z)-1-(2-oxo-1-(2-oxo-2-o-tolylethyl)-5-phenyl-2,3-dihydro-1h-benzo[e][1,4]diazepin-3-yl)-3-m-tolylurea
(r)-1-(2-oxo-1-(2-oxo-2-(o-tolyl)ethyl)-5-phenyl-2,3-dihydro-1h-benzo[e][1,4]diazepin-3-yl)-3-(m-tolyl)urea
CS-0027718
HY-103355
n'-(3-methylphenyl)-n-{1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-2,3-dihydro-1h-1,4-benzodiazepin-3-yl}carbamimidic acid
DTXSID40932492
Q27089258
urea, n-[(3r)-2,3-dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-1h-1,4-benzodiazepin-3-yl]-n'-(3-methylphenyl)-
MS-29592
VFA08428

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" (3R)-N-[1-[(tert-butylcarbonyl)methyl]-2,3-dihydro-2-oxo-5-(2-pyri dyl) -1H-1,4-benzodiazepin-3-yl]-N'-[3-(methylamino)phenyl]urea, 15c (YF476), and (3R)-N-[1-[(tert-Butylcarbonyl)methyl]-2,3-dihydro-2-oxo-5- (2-pyridyl)-1H-1,4-benzodiazepin-3-yl]-N'-[3-(dimethylamino)phenyl ]urea hydrochloride, 15d, showed potent dose-dependent effects in both models with the former showing excellent oral bioavailability and an ED50 of 21nmol/kg po in dogs."( (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
Akuzawa, S; Batt, AR; Kendrick, DA; Miyata, K; Nishida, A; Ohta, M; Rooker, DP; Ryder, H; Satoh, M; Semple, G; Szelke, M, 1997
)
0.3
" PAPPA2 is a metalloproteinase that increases the bioavailability of insulin-like growth factor (IGF) by cleaving IGF binding proteins (IGFBPs)."( Netazepide Inhibits Expression of Pappalysin 2 in Type 1 Gastric Neuroendocrine Tumors.
Boyce, M; Burkitt, MD; Dodd, S; Duckworth, CA; Exarchou, K; Fang, Y; Hall, N; Howes, N; Lloyd, KA; Moore, AR; Oxvig, C; Papoutsopoulou, S; Parsons, BN; Pritchard, DM; Rainbow, L; Varro, A, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
" The YM022 dosage required in this model was much greater than that required in the inhibition of gastric acid."( YM022 [(R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl- 1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea], a potent and selective gastrin/cholecystokinin-B receptor antagonist, prevents gastric and duodenal lesions in rats.
Akuzawa, S; Ito, H; Kamato, T; Kobayashi, A; Miyata, K; Nagakura, Y; Nishida, A; Takinami, Y; Yamano, M; Yuki, H, 1994
)
0.29
" The YM022 dosage required to inhibit basal acid secretion is consistent with that required to suppress pentagastrin-induced acid secretion."( Comparative evaluation of the role of endogenous gastrin in basal acid secretion in conscious rats provided with chronic fistula and pylorus ligation.
Akuzawa, S; Miyata, K; Nishida, A; Takemoto, Y; Uchida-Kobayashi, A, 1996
)
0.29
" In a follow-up study, YM022 and RP73870 were found to produce a rightward shift of the gastrin dose-response curve, which is consistent with competitive inhibition."( Evaluation of the specificity and potency of a series of cholecystokinin-B/gastrin receptor antagonists in vivo.
Ding, XQ; HÃ¥kanson, R, 1996
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pathways (1)

PathwayProteinsCompounds
Cell-type dependent selectivity of CCK2R signaling06

Protein Targets (23)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, CruzipainTrypanosoma cruziPotency31.62280.002014.677939.8107AID1476
Microtubule-associated protein tauHomo sapiens (human)Potency44.66840.180013.557439.8107AID1468
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.81070.001318.074339.8107AID926; AID938
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency6.30960.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.58930.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC50 (µMol)0.14600.00000.43624.3000AID53046
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00010.00010.24801.4000AID51448
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID51448Inhibitory concentration against radioligand [125I]CCK-8 binding to gastrin/Cholecystokinin type B receptor from rat brain1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
AID59643Concentration required to inhibit pentagastrin-induced gastric acid secretion in heidenhain pouch dogs upon intravenous administration1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
AID178225Inhibition of pentagastrin-induced gastric acid secretion in anathesized rats upon intravenous administration1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
AID60212Compound at an peroral dose of 1 umol/kg was tested for the inhibition of pentagastrin-induced gastric acid secretion in heidenhain pouch dogs1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
AID229347Ratio of inhibitory concentration; CCK-A receptor to CCK-B receptor1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
AID59644Concentration required to inhibit pentagastrin-induced gastric acid secretion in heidenhain pouch dogs upon peroral administration1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
AID60213Compound at an peroral dose of 3 uM/Kg was tested for the inhibition of pentagastrin-induced gastric acid secretion in heidenhain pouch dogs1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
AID178226Inhibition of pentagastrin-induced gastric acid secretion in Dawley rats following intravenous administration1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
AID53046Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
AID1346883Human CCK2 receptor (Cholecystokinin receptors)2002Regulatory peptides, Jan-15, Volume: 103, Issue:1
Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor.
AID1346809Rat CCK1 receptor (Cholecystokinin receptors)1994The Journal of pharmacology and experimental therapeutics, May, Volume: 269, Issue:2
Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (63)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's36 (57.14)18.2507
2000's18 (28.57)29.6817
2010's7 (11.11)24.3611
2020's2 (3.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.09

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

MetricThis Compound (vs All)
Research Demand Index10.09 (24.57)
Research Supply Index4.20 (2.92)
Research Growth Index4.29 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.54%)5.53%
Reviews3 (4.62%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other61 (93.85%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]