Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.
Discov Med. 2017 Apr;23(127):221-234.
N-methyl-D-aspartate Receptors Mediate Epilepsy-Induced Axonal Impairment and Tau Phosphorylation via Activating Glycogen Synthase Kinase-3β and Cyclin-dependent Kinase 5
Ifenprodil Tartrate purchased from AbMole
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Source | Discov Med (2017). Figure 5. Ifenprodil (Abmole Bioscience, Houston, TX) |
| Method | Western blot | |
| Cell Lines | Sprague-Dawley rats | |
| Concentrations | 1 mg/kg | |
| Incubation Time | 24 h | |
| Results | PTZ-kindled rats had increased level of Cdk5 in white matters, memantine, ifenprodil, lithium chloride (LiCl), and roscovitine decreased Cdk5 in PTZ-kindled rats. |
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Source | Discov Med (2017). Figure 4. Ifenprodil (Abmole Bioscience, Houston, TX) |
| Method | Immunohistochemistry | |
| Cell Lines | Sprague-Dawley rats | |
| Concentrations | 1 mg/kg | |
| Incubation Time | 24 h | |
| Results | Representative immunohistochemical microphotographs showed increased accumulation of APP in corpus callosum in PTZ-kindled rats. Memantine, ifenprodil, lithium chloride (LiCl), and roscovitine alleviated the accumulation. |
 |
Source | Discov Med (2017). Figure 3. Ifenprodil (Abmole Bioscience, Houston, TX) |
| Method | Immunohistochemistry | |
| Cell Lines | Sprague-Dawley rats | |
| Concentrations | 1 mg/kg | |
| Incubation Time | 24 h | |
| Results | Memantine, ifenprodil, lithium chloride (LiCl), and roscovitine alleviated such reduction. |
 |
Source | Discov Med (2017). Figure 2. Ifenprodil (Abmole Bioscience, Houston, TX) |
| Method | Western Blot | |
| Cell Lines | Sprague-Dawley rats | |
| Concentrations | 1 mg/kg | |
| Incubation Time | 24 h | |
| Results | Memantine, ifenprodil, and LiCl increased tau in PTZ-kindled rats and decreased relative tau phosphorylation level, but failed to decrease p-tau S396 and p-tau T231. |
| Molecular Weight | 475.53 |
| Formula | C21H27NO2.1/2C4H6O6 |
| CAS Number | 23210-58-4 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL Water 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Takako Arii, et al. Nicergoline, ibudilast, ifenprodil tartrate
[4] O Irino, et al. Inhibitory mechanism of ifenprodil tartrate on rabbit platelet aggregation
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