BPR1M97具有双重活性的μ阿片受体（MOP）和孤啡肽FQ肽（NOP）受体激动剂。
Cas No.:2059904-66-2
Sample solution is provided at 25 µL, 10mM.
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BPR1M97 is a novel, dual-activity agonist of the mu-opioid receptor (MOP) and the nociceptin/orphanin FQ peptide (NOP) receptor. BPR1M97 produces potent analgesic effects by simultaneously activating both MOP and NOP receptors, while exhibiting fewer adverse reactions compared to morphine. BPR1M97 is used for pain management and related research[1].
In vitro, cells expressing the human mu-opioid receptor (MOP) and/or the nociceptin/orphanin FQ peptide (NOP) receptor (e.g., HEK-MOP, CHO-K1-NOP, U2OS-MOP) were treated with BPR1M97 (0.6nM – 1.9µM) for 0.5 to 1.5 hours. BPR1M97 significantly inhibited intracellular cAMP levels, activated GIRK channels, and induced β-arrestin-2 recruitment and receptor internalization[1].
In vivo, normal ICR mice or mice with neuropathic pain models were subcutaneously administered a single dose of BPR1M97 (0.2-9mg/kg). BPR1M97 produced a dose-dependent and potent analgesic effect. At high doses, the respiratory depression it induced was significantly less severe than that caused by equi-analgesic doses of morphine[1].
References:
[1] Chao PK, Chang HF, Chang WT, et al. BPR1M97, a dual mu opioid receptor/nociceptin-orphanin FQ peptide receptor agonist, produces potent antinociceptive effects with safer properties than morphine. Neuropharmacology. 2020 Apr;166:107678.
BPR1M97具有双重活性的μ阿片受体（MOP）和孤啡肽FQ肽（NOP）受体激动剂。BPR1M97通过同时激活MOP和NOP受体产生强效镇痛作用，且相比吗啡具有更少的不良反应。BPR1M97可用于疼痛管理及相关研究[1]。
在体外，BPR1M97（0.6nM–1.9μM）处理表达人μ阿片受体（MOP）和/或孤啡肽FQ肽（NOP）受体的细胞（如HEK-MOP、CHO-K1-NOP、U2OS-MOP）0.5-1.5小时。BPR1M97显著抑制细胞内cAMP水平、激活GIRK通道、诱导β-arrestin-2招募及受体内化[1]。
在体内，BPR1M97（0.2-9mg/kg；单次给药）皮下注射于正常ICR小鼠或神经病理性疼痛模型小鼠。BPR1M97能够剂量依赖性地产生强效镇痛作用，且在高剂量下诱导的呼吸抑制显著轻于等镇痛剂量的吗啡[1]。
| Cell experiment [1]: | |
Cell lines | HEK-MOP cells (human embryonic kidney 293 cells constitutively expressing the human mu opioid receptor), CHO-K1-NOP cells (Chinese hamster ovary cells expressing the human nociceptin-orphanin FQ peptide receptor), U2OS-MOP cells (human osteosarcoma cells expressing human MOP), and myc-MOP-expressing mouse pituitary AtT-20 cells |
Preparation Method | HEK-MOP cells were cultured in high-glucose DMEM supplemented with 10% fetal bovine serum (FBS). CHO-K1-NOP cells were cultured in F12 medium containing 10% FBS. U2OS-MOP cells were cultured in McCoy's 5A medium with 10% FBS. AtT-20 cells were cultured in DMEM with 10% FBS. Cells were treated with BPR1M97 at concentrations ranging from 0.6nM to 1.9µM. Incubation times varied by assay: 30 minutes for the cAMP assay, 1.5 hours for the β-arrestin-2 recruitment and receptor internalization assays, and 0.5 hours of pre-treatment with dye followed by real-time monitoring for the membrane potential assay. |
Reaction Conditions | 0.6nM–1.9μM; 0.5-1.5h. |
Applications | In MOP-expressing cells, BPR1M97 acted as a full agonist, significantly inhibiting cAMP production, activating GIRK channels, recruiting β-arrestin-2, and inducing receptor internalization. In NOP-expressing cells, BPR1M97 acted as a G protein-biased full agonist, inhibiting cAMP production but failing to recruit β-arrestin-2. |
| Animal experiment [1]: | |
Animal models | ICR mice, formalin-induced inflammatory pain model in ICR mice, and chronic constriction injury (CCI)-induced neuropathic pain model in ICR mice. |
Preparation Method | Mice were subcutaneously (s.c.) administered a single dose of BPR1M97. For thermal and mechanical nociception tests, behavioral responses were recorded at specified time points post-injection. For tolerance and dependence studies, mice received twice-daily injections for 5 days. |
Dosage form | 0.2-9mg/kg; s.c.; Single or twice-daily injections for 5 days |
Applications | BPR1M97 produced potent, dose-dependent antinociception in acute thermal, acute mechanical with efficacy comparable or superior to morphine. BPR1M97 caused significantly less respiratory depression, cardiovascular inhibition. BPR1M97 also induced conditioned place preference (reward effect) but with lower hyperlocomotor activity. |
References: | |
| Cas No. | 2059904-66-2 | SDF | |
| Canonical SMILES | O=C(NCC1N(C)CCC2=C1C=CC=C2)C3=CC=C(Cl)C(Cl)=C3 | ||
| 分子式 | C18H18Cl2N2O | 分子量 | 349.25 |
| 溶解度 | DMSO: 250 mg/mL (715.82 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8633 mL | 14.3164 mL | 28.6328 mL |
| 5 mM | 572.7 μL | 2.8633 mL | 5.7266 mL |
| 10 mM | 286.3 μL | 1.4316 mL | 2.8633 mL |
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