Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C32H28N4O3 |
| Molecular Weight | 516.5897 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC(NC(=O)N[C@@H]2N=C(C3=CC=CC=C3)C4=CC=CC=C4N(CC(=O)C5=CC=CC=C5C)C2=O)=CC=C1
InChI
InChIKey=YCXFHPUBGMMWJQ-PMERELPUSA-N
InChI=1S/C32H28N4O3/c1-21-11-10-15-24(19-21)33-32(39)35-30-31(38)36(20-28(37)25-16-7-6-12-22(25)2)27-18-9-8-17-26(27)29(34-30)23-13-4-3-5-14-23/h3-19,30H,20H2,1-2H3,(H2,33,35,39)/t30-/m0/s1
| Molecular Formula | C32H28N4O3 |
| Molecular Weight | 516.5897 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
YM022 is an extremely potent and highly selective gastrin/cholecystokinin (CCK)-B receptor antagonist. It was discovered, that this compound possesses antisecretory and antiulcer activities in rats and that it represents a useful therapeutic agent in the treatment of peptic ulcer disease. However, research into this compound has subsequently been discontinued.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor. | 2002-01-15 |
|
| 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. | 1994-05 |
Sample Use Guides
YM022 replaced specific binding of [125I]CCK-8 to rat brain gastrin/cholecystokinin (CCK)-B receptors in a stereoselective and competitive manner. The Ki value of YM022 for gastrin/CCK-B receptors in brain were estimated to be 0.068 nM. The racemate, the S-form of YM022, L-365,260 and Cl-988 also replaced gastrin/CCK-B receptor binding, with Ki values of 0.11, 140, 19 and 6.3 nM, respectively. The affinity of YM022 for gastrin/CCK-B receptor was more than 2 orders of magnitude higher than that for rat pancreatic CCK-A receptor and various other receptors, such as benzodiazepine.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 19:08:03 GMT 2025
by
admin
on
Mon Mar 31 19:08:03 GMT 2025
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| Record UNII |
772CP7W12N
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| Record Status |
Validated (UNII)
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| Record Version |
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145084-28-2
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