| Bioactivity | Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease[1]. |
| Invitro | 在功能测定中，Fipamezole (JP-1730) 的强效拮抗剂特性表现为它能够降低肾上腺素诱导的 35S-GTPγS 结合，KB 值分别为 8.4 nM、16 nM、4.7 nM（在人类 α2A、α2B 和 α2C 受体上）。Fipamezole 对组胺 H1 和 H3 受体以及血清素 (5-HT) 转运体也具有中等亲和力（IC50 为 100 nM-1 μM）[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Fipamezole 相关抗体: |
| In Vivo | 在 MPTP 损伤的狨猴中，Fipamezole (1-10 mg/kg；口服；单次) 显著减轻了 L-DOPA (HY-N0304) 引起的运动障碍，同时又不影响 L-DOPA 的抗帕金森病作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 150586-58-6 |
| Formula | C14H15FN2 |
| Molar Mass | 230.28 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Juha-Matti Savola, et al. Fipamezole (JP-1730) is a potent alpha2 adrenergic receptor antagonist that reduces levodopa-induced dyskinesia in the MPTP-lesioned primate model of Parkinson's disease. Mov Disord. 2003 Aug;18(8):872-83. |