| Description | RP-72540 is a cholecystokinin B receptor antagonist. RP 72540 showed selectivity factors in express of 200 for CCKA versus CCKB receptors and also had high affinity for gastrin binding sites in the stomach. Administration of RP-72540 resulted in a dose-dependent inhibition of [3H]pCCK-8 binding in mouse brain homogenate. However, the relative penetration of RP-72540 into the forebrain after peripheral administration was below 0.01%. |
| Synonyms | RPR 102681, RPR-102681, RPR102681 |
| molecular weight | 518.56 |
| Molecular formula | C28H30N4O6 |
| CAS | 139088-45-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Bertrand P, Böhme GA, Durieux C, Guyon C, Capet M, Jeantaud B, Boudeau P, Ducos B, Pendley CE, Martin GE, et al. Pharmacological properties of ureido-acetamides, new potent and selective non-peptide CCKB/gastrin receptor antagonists. Eur J Pharmacol. 1994 Sep 12;262(3):233-45. PubMed PMID: 7813588. 2. Jensen RT. CCKB/gastrin receptor antagonists: recent advances and potential uses in gastric secretory disorders. Yale J Biol Med. 1996 May-Jun;69(3):245-59. Review. PubMed PMID: 9165693; PubMed Central PMCID: PMC2589015. 3. Bierkamp C, Kowalski-Chauvel A, Dehez S, Fourmy D, Pradayrol L, Seva C. Gastrin mediated cholecystokinin-2 receptor activation induces loss of cell adhesion and scattering in epithelial MDCK cells. Oncogene. 2002 Oct 31;21(50):7656-70. PubMed PMID: 12400008. |