| Identification | Back Directory | [Name]
(2S,4S)-4-Fluoro-1-[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]-2-pyrrolidinecarboxamide | [CAS]
2376198-66-0 | [Synonyms]
(2S,4S)-4-Fluoro-1-[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]-2-pyrrolidinecarboxamide | [Molecular Formula]
C19H20F2N2O2 | [MOL File]
2376198-66-0.mol | [Molecular Weight]
346.37 |
| Hazard Information | Back Directory | [Uses]
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 μM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD)[1]. | [in vivo]
MAO-B-IN-6 (1 mg/kg, i.v.; 5 mg/kg, p.o.) shows oral bioavailability in rats (F=55.2%) and monkeys (F=107.1%)[1].
MAO-B-IN-6 (0.08, 0.4, 2 mg/kg; i.p.) diaplays stronger MAO-B inhibitory activity[1].
MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) increases the rearing activity in a dose-dependent manner[1].
MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) shows a potential efficacy for alleviating dopamine (DA) deficits in the MPTP-induced Parkinson's disease (PD) mouse model[1].
MAO-B-IN-6 (0.156, 0.312, 0.625, 1.25 mg/kg; i.p.) increases the effect of levodopa on dopamine concentration in the striatum[1].
MAO-B-IN-6 (0.156, 0.312, 0.625, 1.25 mg/kg; i.p.) shows a significant reduction in galantamine-induced tremulous jaw movements[1].
Pharmacokinetic Parameters of MAO-B-IN-6 in SD rats and cynomolgus monkeys[1].
| Compound | Route | Dose (mg/kg) | Cmax (ng/mL) | AUCt (ng·h/mL) | T1/2 (h) | Vss (h) | Cl (mL/min/kg) | F (%) | | D5 (Rats) | iv | 1 | 690 | 505 | 0.67 | 1.37 | 32.9 | / | | D5 (Rats) | po | 5 | 1000 | 1400 | 0.57 | / | / | 55.2 | | D5 (Monkeys) | iv | 1 | 924 | 2120 | 1.77 | 1.06 | 7.54 | / | | D5 (Monkeys) | po | 5 | 2280 | 11,300 | 2.80 | / | / | 107.1 |
SD rats; 1 mg/kg, i.v.; 5 mg/kg, p.o.; Cynomolgus monkeys; 1 mg/kg, i.v.; 5 mg/kg, p.o. [1].
| Animal Model: | SD rats[1] | | Dosage: | 1, 5 mg/kg | | Administration: | 1 mg/kg, i.v.; 5 mg/kg, p.o. | | Result: | Showed oral bioavailability in rats (F=55.2%). |
| Animal Model: | cynomolgus monkeys[1] | | Dosage: | 1, 5 mg/kg | | Administration: | 1 mg/kg, i.v.; 5 mg/kg, p.o. | | Result: | Showed oral bioavailability in monkeys (F=107.1%). |
| Animal Model: | mice[1] | | Dosage: | 0.08, 0.4, 2 mg/kg | | Administration: | i.p. | | Result: | Displayed stronger MAO-B inhibitory activity. |
| Animal Model: | PD mouse mode[1] | | Dosage: | 0.625, 1.25, 2.5 mg/kg | | Administration: | i.p. | | Result: | Increased the rearing activity in a dose-dependent manner. |
| Animal Model: | C57BL/6 mice[1] | | Dosage: | 0.156, 0.312, 0.625, 1.25 mg/kg | | Administration: | i.p. | | Result: | Increased the effect of levodopa on dopamine concentration in the striatum. |
| Animal Model: | SD rats[1] | | Dosage: | 0.156, 0.312, 0.625, 1.25 (3.0 mg/kg galantamine, i.p.) | | Administration: | i.p. | | Result: | Showed a significant reduction in galantamine-induced tremulous jaw movements. |
| [IC 50]
MAO-B: 0.019 μM (IC50); MAO-A: 46.365 μM (IC50) | [References]
[1] Wang Z,et al. Enhancing monoamine oxidase B inhibitory activity via chiral fluorination: Structure-activity relationship, biological evaluation, and molecular docking study. Eur J Med Chem. 2022; 228:114025. DOI:10.1016/j.ejmech.2021.114025 |
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