Page last updated: 2024-12-11
yf 476
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
YF 476: gastrin and CCK-B receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9870520 |
| CHEMBL ID | 324547 |
| SCHEMBL ID | 1387611 |
| MeSH ID | M0272778 |
Synonyms (33)
| Synonym |
|---|
| 1-[(3r)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-pyridin-2-yl-3h-1,4-benzodiazepin-3-yl]-3-(3-methylaminophenyl)urea |
| gtpl887 |
| PDSP1_000895 |
| PDSP2_000881 |
| yf 476 |
| netazepide |
| yf-476 |
| yf476 |
| n-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1h-1,4-benzodiazepin-3-yl)-n'-(3-(methylamino)phenyl)urea |
| CHEMBL324547 , |
| sograzepide |
| (r)-1-(1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1h-benzo[e][1,4]diazepin-3-yl)-3-(3-(methylamino)phenyl)urea |
| 1-[(r)-1-(3,3-dimethyl-2-oxo-butyl)-2-oxo-5-pyridin-2-yl-2,3-dihydro-1h-benzo[e][1,4]diazepin-3-yl]-3-(3-methylamino-phenyl)-urea |
| bdbm50056102 |
| 155488-25-8 |
| 1-((3r)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1h-1,4-benzodiazepin-3-yl)-3-(3-(methylamino)phenyl)urea |
| netazepide [inn] |
| unii-hou4i0g29c |
| hou4i0g29c , |
| sograzepide [inn] |
| SCHEMBL1387611 |
| DTXSID00165906 |
| AKOS027322738 |
| YDZYKNJZCVIKPP-VWLOTQADSA-N |
| n-[(3r)-1-(3,3-dimethyl-2-oxobutyl)-2,3-dihydro-2-oxo-5-(2-pyridinyl)-1h-1,4-benzodiazepin-3-yl]-n'-[3-(methylamino)phenyl]urea |
| J-009200 |
| DB12355 |
| 1-[(3r)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-pyridin-2-yl-3h-1,4-benzodiazepin-3-yl]-3-[3-(methylamino)phenyl]urea |
| CS-0003594 |
| HY-14850 |
| Q2297773 |
| ym-220 |
| MS-29255 |
Research Excerpts
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " (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
| Excerpt | Relevance | Reference |
|---|---|---|
| " It produced a rightward shift of the gastrin dose-response curve, consistent with competitive inhibition." | ( Evaluation of three novel cholecystokinin-B/gastrin receptor antagonists: a study of their effects on rat stomach enterochromaffin-like cell activity. Ding, XQ; Håkanson, R; Lindström, E, 1997) | 0.3 |
| " In contrast, the increase in protein and enzyme output after the infusion of a supraphysiological dose of CCK-33 (130 pmol kg) to the general circulation was not affected by pretreatment with low dosage YF476, whereas high dosage YF476 completely inhibited the stimulated secretion." | ( CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Evilevitch, L; Pierzynowski, SG; Weström, BR, 2004) | 0.32 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (8)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 0.0288 | 0.0000 | 0.6518 | 10.0000 | AID290979 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 0.0288 | 0.0001 | 0.8363 | 10.0000 | AID290979 |
| Cholecystokinin receptor type A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.5020 | 0.0000 | 0.4362 | 4.3000 | AID53046 |
| Gastrin/cholecystokinin type B receptor | Canis lupus familiaris (dog) | Ki | 0.0288 | 0.0288 | 0.0288 | 0.0288 | AID290979 |
| Gastrin/cholecystokinin type B receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0001 | 0.0001 | 0.2480 | 1.4000 | AID51448 |
| Cholecystokinin receptor type A | Homo sapiens (human) | Ki | 0.0302 | 0.0000 | 0.3190 | 2.2760 | AID262761; AID290979; AID330894 |
| Gastrin/cholecystokinin type B receptor | Homo sapiens (human) | Ki | 0.0001 | 0.0001 | 0.0366 | 0.3450 | AID262760; AID290976; AID330893 |
| Cholecystokinin receptor type A | Cavia porcellus (domestic guinea pig) | Ki | 0.3981 | 0.0003 | 0.1377 | 0.6310 | AID312995 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (145)
Molecular Functions (18)
Ceullar Components (27)
Bioassays (25)
Research
Studies (43)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (11.63) | 18.2507 |
| 2000's | 20 (46.51) | 29.6817 |
| 2010's | 17 (39.53) | 24.3611 |
| 2020's | 1 (2.33) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 10.72
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.
| This Compound (10.72) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 9 (20.93%) | 5.53% |
| Reviews | 4 (9.30%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 30 (69.77%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||