2. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein Others
  3. Prolyl Endopeptidase (PREP) Aminopeptidase Opioid Receptor Dopamine Receptor Drug Intermediate
  4. RB 101

RB 101 is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor. RB 101 blocks enkephalin breakdown, elevates extracellular enkephalin levels and activate δ-opioid receptor and dopamine D1 receptor. RB 101 can be used for the research of pain, depressive syndromes, and diabetic neuropathy.

For research use only. We do not sell to patients.

RB 101

RB 101 Chemical Structure

CAS No. : 135949-60-9

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RB 101 Related Antibodies

Top Publications Citing Use of Products

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CD13 LTA4H

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • Biological Activity

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Description

RB 101 is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor. RB 101 blocks enkephalin breakdown, elevates extracellular enkephalin levels and activate δ-opioid receptor and dopamine D1 receptor. RB 101 can be used for the research of pain, depressive syndromes, and diabetic neuropathy[1][2][3].

IC50 & Target[2]

δ Opioid Receptor/DOR

 

D1 Receptor

 

In Vitro

RB 101 enhances spontaneous methionine-enkephalin-like material outflow from rat spinal cord tissue via inhibition of enkephalin degrading enzymes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RB 101 Related Antibodies
In Vivo

RB 101 (2.5-40 mg/kg; i.v.; single administration) dose-dependently inhibits [3H]diprenorphine binding to mouse brain opioid receptors under basal conditions[1].
RB 101 (5-20 mg/kg; i.v.; single administration) potentiates stress-induced analgesia in mice, reaching 85% analgesia at 5 mg/kg when combined with warm-water swim stress[1].
RB 101 (1.25-10 mg/kg; i.v.; single slow injection) induces a dose-dependent, long-lasting increase in spontaneous motor activity in mice via δ opioid and dopamine D1 receptor stimulation[2].
RB 101 (2.5-10 mg/kg; i.v.; single slow injection) dose-dependently attenuates conditioned suppression of motility in shocked mice and increases striatal dopamine turnover, via δ opioid and dopamine D1 receptor stimulation[2].
RB 101 (2.5-10 mg/kg; i.v.; single slow injection (20 s); 10 min before testing) significantly reduces immobility time in the mouse forced swim test via δ opioid and dopamine D1 receptor stimulation[2].
RB 101 (5-40 mg/kg; i.v.) produces dose-dependent, μ- and δ-opioid receptor-mediated antinociception in Streptozocin (HY-13753)-induced diabetic rats with neuropathic pain, completely suppressing mechanical hyperalgesia at doses of 20 and 40 mg/kg i.v.[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male albino mice (Depre, France; 20-22 g)[1]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: i.v.; single administration
Result: Induced a dose-dependent reduction in [3H]diprenorphine binding: 5 mg/kg caused 20% displacement, 10 mg/kg caused 30% displacement (plateau effect), with no additional displacement at 20 mg/kg.
Induced a non-significant increase in jump latency at 5 mg/kg.
Produced statistically significant analgesia relative to controls at 10 mg/kg, 20 mg/kg, and 40 mg/kg, with analgesia percentages increasing with dose.
Animal Model: Male albino mice (Depre, France; 20-22 g; forced warm-water swim stress model)[1]
Dosage: 5 mg/kg; 20 mg/kg
Administration: i.v.; single administration
Result: Combined with stress induced 85% analgesia at 5 mg/kg (vs. 48% analgesia from stress alone), and this combined analgesia was blocked by naloxone but not by naltrindole.
Combined with stress caused 45% displacement of [3H]diprenorphine relative to unstressed controls at 5 mg/kg, while 20 mg/kg combined with stress caused 43% displacement relative to unstressed controls.
Animal Model: Swiss albino mice (male, 20-22 g for spontaneous motor activity and forced swim tests; ~30 g, 8 weeks old for conditioned suppression of motility test)[2]
Dosage: 1.25 mg/kg; 2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.v.; single slow injection
Result: Induced a dose-dependent increase in locomotor activity, with effects peaking between 5-10 min post-injection.
Remained significant at 15 and 20 min post-injection at 10 mg/kg.
Produced a significant cumulative increase in motor activity (linear locomotion + rears) over 10 and 20 min at 5 mg/kg, which was antagonized by pre-treatment with naltrindole (0.1 mg/kg s.c.) and SCH 23390 (0.07 mg/kg s.c.), but not sulpiride (25 mg/kg i.p.).
Animal Model: Swiss albino mice (male, ~30 g, 8 weeks old)[2]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.v.; single slow injection
Result: Did not alter locomotor activity at 2.5 and 5 mg/kg, but increased activity at 10 mg/kg in non-shocked mice.
Dose-dependently reduced conditioned motility suppression at 5 and 10 mg/kg in shocked mice.
Effect of 5 mg/kg was antagonized by pre-treatment with naltrindole (0.1 mg/kg s.c.) and SCH 23390 (0.07 mg/kg s.c.), but not sulpiride (25 mg/kg i.p.).
Significantly increased striatal DOPAC/DA and HVA/DA ratios to 0.108 and 0.100, respectively, in shocked mice treated with 5 mg/kg, an effect blocked by naltrindole.
Animal Model: Swiss albino mice (male, 20-22 g)[2]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.v.; single slow injection
Result: Significantly shortened the duration of immobility in the forced swim test at 5 and 10 mg/kg.
Effect of 5 mg/kg was antagonized by pre-treatment with naltrindole (0.1 mg/kg s.c.) and SCH 23390 (0.07 mg/kg s.c.), but not sulpiride (25 mg/kg i.p.).
Animal Model: Sprague-Dawley (male, 300 g, Streptozocin-induced neuropathic pain)[3]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: i.v.
Result: Produced a dose-dependent antinociceptive effect on mechanical hyperalgesia, with 20 and 40 mg/kg doses completely suppressing diabetes-induced hyperalgesia (P<0.001).
Achieved a maximal vocalization threshold elevation of +294 g (+178% of predrug score) at 20 minutes with 40 mg/kg dose, which was not significantly different from the maximal effect of 20 mg/kg.
Had a short duration of action (20 minutes) with 5 mg/kg dose, while 10, 20, and 40 mg/kg doses lasted 60 minutes.
Showed a ceiling effect at 40 mg/kg confirmed by AUC values.
Produced a significant increase in withdrawal threshold for mechanical allodynia only with 40 mg/kg dose, with a maximal increase of +8.3 g at 20 minutes (P<0.01), lasting 20 minutes.
Did not significantly affect tail immersion reaction time for thermal allodynia at any dose.
Had its antinociceptive effect at 20 mg/kg completely abolished by pretreatment with 0.5 mg/kg i.v. naloxone or 1 μg/rat i.t. naltrindole.
Molecular Weight

582.84

Formula

C31H38N2O3S3
CAS No.
SMILES

CSCC[C@H](N)CSSCC(CC1=CC=CC=C1)C(N[C@H](C(OCC2=CC=CC=C2)=O)CC3=CC=CC=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RB 101 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RB 101135949-60-9RB101RB-101Prolyl Endopeptidase (PREP)AminopeptidaseOpioid ReceptorDopamine ReceptorDrug Intermediateprolyl oligopeptidasePOPDrug Iintermediatestreptozocin-induced diabetic ratsrat spinal cord tissueaminopeptidase Nneutral endopeptidase-24.11μ-opioid receptorsmouse braindiabetic neuropathydopamine D1 receptorsδ opioid receptorsenkephalinInhibitorinhibitorinhibit

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