RB 101 hydrochloride
Based on 1 Customer Validation
RB 101 hydrochloride is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor. RB 101 hydrochloride blocks enkephalin breakdown, elevates extracellular enkephalin levels and activate δ-opioid receptor and dopamine D1 receptor. RB 101 hydrochloride can be used for the research of pain, depressive syndromes, and diabetic neuropathy.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C31H39ClN2O3S3
- Masse moléculaire:619.30
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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δ Opioid Receptor/DOR |
D1 Receptor |
In Vitro
In Vivo
RB 101 (5-20 mg/kg; i.v.; single administration) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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.) hydrochloride 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.
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Animal Model:Male albino mice (Depre, France; 20-22 g)[1]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:i.v.; single administration
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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.
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Animal Model:Male albino mice (Depre, France; 20-22 g; forced warm-water swim stress model)[1]
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Dosage:5 mg/kg; 20 mg/kg
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Administration:i.v.; single administration
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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.
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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]
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Dosage:1.25 mg/kg; 2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.v.; single slow injection
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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.).
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Animal Model:Swiss albino mice (male, ~30 g, 8 weeks old)[2]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.v.; single slow injection
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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.
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Animal Model:Swiss albino mice (male, 20-22 g)[2]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.v.; single slow injection
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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.).
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Animal Model:Sprague-Dawley (male, 300 g, Streptozocin-induced neuropathic pain)[3]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:i.v.
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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.
Chemical Information
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Appearance Solid-Liquid Mixture
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Masse moléculaire 619.30
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Formule C31H39ClN2O3S3
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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.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
Ethanol : 50 mg/mL (80.74 mM; Need ultrasonic)
DMSO : 1 mg/mL (1.61 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 0.5 mg/mL (0.81 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C
Pureté et documentation
Références
[1]. Ruiz-Gayo M, et al. In vivo occupation of mouse brain opioid receptors by endogenous enkephalins: blockade of enkephalin degrading enzymes by RB 101 inhibits [3H]diprenorphine binding. Brain Res. 1992;571(2):306-312. [Content Brief]
[2]. Baamonde A, et al. Antidepressant-type effects of endogenous enkephalins protected by systemic RB 101 are mediated by opioid delta and dopamine D1 receptor stimulation. Eur J Pharmacol. 1992;216(2):157-166. [Content Brief]
[3]. Coudoré-Civiale MA, et al. Enhancement of the effects of a complete inhibitor of enkephalin-catabolizing enzymes, RB 101, by a cholecystokinin-B receptor antagonist in diabetic rats. Br J Pharmacol. 2001;133(1):179-185. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 1.6147 mL | 8.0736 mL | 16.1473 mL | 40.3682 mL |
| Ethanol | 5 mM | 0.3229 mL | 1.6147 mL | 3.2295 mL | 8.0736 mL |
| 10 mM | 0.1615 mL | 0.8074 mL | 1.6147 mL | 4.0368 mL | |
| 15 mM | 0.1076 mL | 0.5382 mL | 1.0765 mL | 2.6912 mL | |
| 20 mM | 0.0807 mL | 0.4037 mL | 0.8074 mL | 2.0184 mL | |
| 25 mM | 0.0646 mL | 0.3229 mL | 0.6459 mL | 1.6147 mL | |
| 30 mM | 0.0538 mL | 0.2691 mL | 0.5382 mL | 1.3456 mL | |
| 40 mM | 0.0404 mL | 0.2018 mL | 0.4037 mL | 1.0092 mL | |
| 50 mM | 0.0323 mL | 0.1615 mL | 0.3229 mL | 0.8074 mL | |
| 60 mM | 0.0269 mL | 0.1346 mL | 0.2691 mL | 0.6728 mL | |
| 80 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5046 mL |
RB 101 hydrochloride Related Classifications
HY-117702A Related Classifications
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Keywords
- RB 101
- RB101
- RB-101
- Prolyl Endopeptidase (PREP)
- Aminopeptidase
- Opioid Receptor
- Dopamine Receptor
- Drug Intermediate
- streptozocin-induced diabetic rats
- rat spinal cord tissue
- aminopeptidase N
- neutral endopeptidase-24.11
- μ-opioid receptors
- mouse brain
- diabetic neuropathy
- dopamine D1 receptors
- δ opioid receptors
- enkephalin
- Inhibitor
- inhibitor
- inhibit