RB-101
Clinical data | |
---|---|
Other names | RB-101; phenylmethyl (2S)-2-[(2-([(2S)-2-amino-4-methylsulfanylbutyl]disulfanylmethyl)-3-phenylpropanoyl)amino]-3-phenylpropanoate |
Identifiers | |
| |
JSmol) | |
| |
| |
(verify) |
RB-101 is a drug that acts as an enkephalinase inhibitor, which is used in scientific research.
RB-101 is a
These peptides act primarily at the
Unlike the more commonly used enkephalinase inhibitor racecadotril, which only acts peripherally and has antidiarrheal effects, RB-101 is able to enter the brain, and thus produces a range of effects, acting as an analgesic, anxiolytic and antidepressant.[7] The antidepressant and anxiolytic actions are thought to be mediated through the delta opioid receptor, while the analgesic effects most likely result from a mix of mu and delta activity.[8] Animal studies suggest that RB-101 is also likely to be useful in relieving the symptoms of acute opioid withdrawal[9] and in the management of opioid dependence.[10][11][12]
A significant advantage of inhibiting the breakdown of endogenous opioid peptides rather than stimulating opioid receptors with exogenous drugs is that the levels of opioid peptides are only increased slightly from natural levels, thus avoiding overstimulation and downregulation of the opioid receptors. This means that even when RB-101 is used in high doses for extended periods of time, there is no development of dependence on the drug or tolerance to its analgesic effects.[13][14] Consequently, even though RB-101 is able to produce potent analgesic effects via the opioid system, it is unlikely to be addictive.[15][16]
Unlike conventional opioid agonists, RB-101 also failed to produce
RB-101 itself is not orally active and so has not been developed for medical use in humans, however modification of the drug has led to newer orally acting compounds such as RB-120 and RB-3007, which may be more likely to be adopted for medical use if clinical trials are successful.[19][20][21][22][23]
See also
References
- PMID 1320419.
- PMID 1560364.
- PMID 1352352.
- PMID 7996417.
- PMID 8035345.
- PMID 9103499.
- PMID 16442521.
- PMID 17627672.
- PMID 7780637.
- PMID 8872371.
- PMID 8947930.
- PMID 17351659.
- PMID 1478260.
- PMID 8200422.
- PMID 8422896.
- ISBN 978-0521622691.
- PMID 11166965.
- PMID 11543770.
- PMID 9469529.
- PMID 12855323.
- PMID 12855323.
- PMID 17227231.
- PMID 18855623.