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RPR 102681
- Development stage
- Phase 1
- Lead developer
- Sanofi
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
RPR 102681 is a selective small molecule antagonist of the cholecystokinin B (CCK-B) receptor, also known as the gastrin receptor. Originally developed by Rhône-Poulenc Rorer, the compound was primarily investigated for its potential in treating cocaine-related disorders and addiction. The therapeutic rationale was based on preclinical findings that CCK-B receptor modulation could influence dopamine release and reduce cocaine self-administration. In Phase I clinical trials, RPR 102681 was found to be safe and well-tolerated when co-administered with cocaine; however, it appeared to reduce rather than increase intrasynaptic dopamine in the striatum of humans, contrasting with animal data. Beyond its psychiatric investigations, RPR 102681 has been used extensively in research as a tool to block gastrin-mediated effects on gastric acid secretion and gastroprotection.
- Other names
- RPR102681RPR-102681RPR 102681
02
Targets
CCK2R (Cholecystokinin 2 Receptor)
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