145084-28-2 Usage
Uses
Used in Pharmaceutical Industry:
YM 022 is used as a pharmacological agent for targeting the gastrin/cholecystokinin (CCK)-B receptor. Its high selectivity and potency make it a valuable tool in the development of drugs aimed at treating conditions related to the overactivation of the CCK-B receptor, such as certain gastrointestinal disorders and potentially cancer-related conditions.
Used in Research Applications:
In the field of research, YM 022 serves as a valuable compound for studying the role of the CCK-B receptor in various physiological processes and disease states. Its use as a selective antagonist allows researchers to investigate the specific functions and pathways associated with the CCK-B receptor, contributing to a deeper understanding of its role in health and disease.
Used in Drug Development:
YM 022 is utilized in the development of new drugs targeting the CCK-B receptor. Its high affinity and selectivity make it an attractive starting point for the design and synthesis of novel therapeutic agents. These drugs may have potential applications in treating a range of conditions, including gastrointestinal disorders and possibly certain types of cancer.
Biological Activity
Extremely potent and highly selective non-peptide CCK 2 silent antagonist (K i values are 68 pM and 63 nM at CCK 2 and CCK 1 receptors respectively). Acts in vivo to potently inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation with a long duration of action.
Check Digit Verification of cas no
The CAS Registry Mumber 145084-28-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,4,5,0,8 and 4 respectively; the second part has 2 digits, 2 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 145084-28:
(8*1)+(7*4)+(6*5)+(5*0)+(4*8)+(3*4)+(2*2)+(1*8)=122
122 % 10 = 2
So 145084-28-2 is a valid CAS Registry Number.
145084-28-2Relevant academic research and scientific papers
Benzodiazepine aryl urea derivatives
-
, (2008/06/13)
This invention relates to novel benzodiazepine derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof, STR1 (wherein R 1 is an aryl group, or an aromatic heterocyclic radical of 5-membered monocyclic, 6-m
New 1,4-benzodiazepin-2-one derivatives as gastrin/cholecystokinin-B antagonists
Satoh,Kondoh,Okamoto,Nishida,Miyata,Ohta,Mase,Murase
, p. 2159 - 2167 (2007/10/03)
A novel series of 1-aroylmethyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one derivatives was prepared and evaluated for activity as gastrin/cholecystokinin (CCK)-B receptor antagonists. In vitro binding studies showed that some derivatives exhibited potent affinity for gastrin/CCK-B receptor and high selectivity over peripheral CCK (CCK-A) receptor. Furthermore, these compounds potently inhibited pentagastrin- induced gastric acid secretion upon intravenous administration in an in vivo model in rats. Structure-activity relationship studies of this series suggested that 1-[(R)-2,3-dihydro-1-(2-methylphenacyl)-2-oxo-5-phenyl-1H- 1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (35b, YM022) was the optimal compound with IC50 values of 0.17, 0.11 and 150 nM for gastrin, CCK-B and CCK-A receptors, respectively, and an ED50 value of 9.5 nmol/kg (i.v.) in rats. The absolute configuration of the precursor of YM022, an (R)-3-amino- 1,3-dihydro-2H-1,4-benzodiazepin-2-one derivative ((R)-25), was determined by X-ray crystallographic analysis of its (S)-mandelate. It would be expected thai YM022, a potent and selective gastrin/CCK-B receptor antagonist, inhibits gastric acid secretion without inducing gastrin-mediated side- effects such as hypergastrinemia and hyperplasia of oxyntic mucosa.
