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^[1][2][3]. In Vitro:RB 101 enhances spontaneous methionine-enkephalin-like material outflow from rat spinal cord tissue via inhibition of enkephalin degrading enzymes^[1]. 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].