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- RB-101 abstract "RB-101 is a drug that acts as an enkephalinase inhibitor, which is used in scientific research.RB-101 is a prodrug which acts by splitting at the disulfide bond once inside the brain, to form two selective enzyme inhibitors and blocking both types of the zinc-metallopeptidase enkephalinase enzymes. This inhibits the breakdown of the endogenous opioid peptides known as enkephalins. These two enzymes, aminopeptidase N (APN) and neutral endopeptidase 24.11 (NEP), are responsible for the breakdown of both kinds of enkephalin naturally found in the body, and so RB-101 causes a buildup of both Met-enkephalin and Leu-enkephalin.These peptides act primarily at the delta opioid receptor, although they also stimulate the mu opioid receptor to some extent through a delta-opioid receptor mediated interaction with another peptide cholecystokinin, and the enzyme-inhibiting effects of RB-101 thus produce indirect stimulation of both of these opioid receptor subtypes. This causes RB-101 to be strongly synergistic with cholecystokinin antagonists.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. 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. Animal studies suggest that RB-101 is also likely to be useful in relieving the symptoms of acute opioid withdrawal and in the management of opioid dependence.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. Consequently even though RB-101 is able to produce potent analgesic effects via the opioid system, it is unlikely to be addictive.Unlike conventional opioid agonists, RB-101 also failed to produce respiratory depression, which suggests it might be a much safer drug than traditional opioid painkillers. RB-101 also powerfully potentiated the effects of traditional analgesics such as ibuprofen and morphine, suggesting that it could be used to boost the action of a low dose of normal opioids which would otherwise be ineffective.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.".
- RB-101 casNumber "135949-60-9".
- RB-101 iupacName "benzyl N-(3-{[(2S)-2-amino-4-(methylthio)butyl]dithio}-2-benzylpropanoyl)-(L)-phenylalaninate".
- RB-101 pubchem "119600".
- RB-101 thumbnail RB-1012DCSD.svg?width=300.
- RB-101 wikiPageID "16636681".
- RB-101 wikiPageLength "12573".
- RB-101 wikiPageOutDegree "28".
- RB-101 wikiPageRevisionID "679029194".
- RB-101 wikiPageWikiLink Alanine_aminopeptidase.
- RB-101 wikiPageWikiLink Aminopeptidase_N.
- RB-101 wikiPageWikiLink Analgesic.
- RB-101 wikiPageWikiLink Antidepressant.
- RB-101 wikiPageWikiLink Antidiarrheal.
- RB-101 wikiPageWikiLink Antidiarrhoeal.
- RB-101 wikiPageWikiLink Anxiolytic.
- RB-101 wikiPageWikiLink Category:Enkephalinase_inhibitors.
- RB-101 wikiPageWikiLink Category:Organic_disulfides.
- RB-101 wikiPageWikiLink Category:Propionamides.
- RB-101 wikiPageWikiLink Category:Propionates.
- RB-101 wikiPageWikiLink Cholecystokinin.
- RB-101 wikiPageWikiLink Cholecystokinin_antagonist.
- RB-101 wikiPageWikiLink Delta_opioid_receptor.
- RB-101 wikiPageWikiLink Disulfide.
- RB-101 wikiPageWikiLink Disulfide_bond.
- RB-101 wikiPageWikiLink Ecadotril.
- RB-101 wikiPageWikiLink Enkephalin.
- RB-101 wikiPageWikiLink Enkephalinase.
- RB-101 wikiPageWikiLink Enzyme_inhibitor.
- RB-101 wikiPageWikiLink Hypoventilation.
- RB-101 wikiPageWikiLink Ibuprofen.
- RB-101 wikiPageWikiLink Leu-enkephalin.
- RB-101 wikiPageWikiLink Met-enkephalin.
- RB-101 wikiPageWikiLink Morphine.
- RB-101 wikiPageWikiLink Mu_opioid_receptor.
- RB-101 wikiPageWikiLink Neprilysin.
- RB-101 wikiPageWikiLink Phenylalanine.
- RB-101 wikiPageWikiLink Prodrug.
- RB-101 wikiPageWikiLink Racecadotril.
- RB-101 wikiPageWikiLink Respiratory_depression.
- RB-101 wikiPageWikiLink Δ-opioid_receptor.
- RB-101 wikiPageWikiLink Μ-opioid_receptor.
- RB-101 wikiPageWikiLinkText "RB-101".
- RB-101 c "31".
- RB-101 casNumber "135949".
- RB-101 h "38".
- RB-101 hasPhotoCollection RB-101.
- RB-101 image "RB-1013DanJ.gif".
- RB-101 iupacName "benzyl N--(L)-phenylalaninate".
- RB-101 molecularWeight "582.84".
- RB-101 n "2".
- RB-101 o "3".
- RB-101 pubchem "119600".
- RB-101 s "3".
- RB-101 synonyms "(RB-101; phenylmethyl -2-[amino]-3-phenylpropanoate)".
- RB-101 verifiedrevid "448079539".
- RB-101 width "300".
- RB-101 wikiPageUsesTemplate Template:Drugbox.
- RB-101 wikiPageUsesTemplate Template:Opioidergics.
- RB-101 wikiPageUsesTemplate Template:Reflist.
- RB-101 subject Category:Enkephalinase_inhibitors.
- RB-101 subject Category:Organic_disulfides.
- RB-101 subject Category:Propionamides.
- RB-101 subject Category:Propionates.
- RB-101 hypernym Drug.
- RB-101 type Article.
- RB-101 type ChemicalSubstance.
- RB-101 type Drug.
- RB-101 type Amide.
- RB-101 type Article.
- RB-101 type Chemical.
- RB-101 type Inhibitor.
- RB-101 type ChemicalObject.
- RB-101 type Thing.
- RB-101 type Q8386.
- RB-101 comment "RB-101 is a drug that acts as an enkephalinase inhibitor, which is used in scientific research.RB-101 is a prodrug which acts by splitting at the disulfide bond once inside the brain, to form two selective enzyme inhibitors and blocking both types of the zinc-metallopeptidase enkephalinase enzymes. This inhibits the breakdown of the endogenous opioid peptides known as enkephalins.".
- RB-101 label "RB-101".
- RB-101 sameAs m.03yhx3l.
- RB-101 sameAs RB-101.
- RB-101 sameAs RB-101.
- RB-101 sameAs Q7275904.
- RB-101 sameAs Q7275904.
- RB-101 wasDerivedFrom RB-101?oldid=679029194.
- RB-101 depiction RB-1012DCSD.svg.
- RB-101 isPrimaryTopicOf RB-101.