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| | TCN 238 Basic information |
| | TCN 238 Chemical Properties |
| Boiling point | 414.883±43.00 °C(Press: 760.00 Torr)(predicted) | | density | 1.222±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | storage temp. | Store at -20°C | | solubility | DMF: 25 mg/ml; DMSO: 25 mg/ml; DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml; Ethanol: 5 mg/ml | | form | Powder | | pka | 4.055±0.10(predicted) | | color | White to off-white |
| | TCN 238 Usage And Synthesis |
| Uses | TCN 238 allosteric modulator of the mGlu4 receptor. TCN 238 may be useful in the treatment of motor dysfunction and in the treatment of Parkinson’s disease. TCN 238 is orally bioavailable. | | Uses | TCN 238 allosteric modulator of the mGlu4 receptor (1). TCN 238 may be useful in the treatment of motor dysfunction and in the treatment of Parkinson’s disease. TCN 238 is orally bioavailable. | | in vivo | TCN238 is highly CNS penetrant with a concentration of 33.8 μM in the brain. The plasma protein binding in rats is measured as 90% bound. The metabolic stability of TCN238 is assessed in rat and human microsomes and found to be 62% and 83% hepatic blood flow. The limited stability translated into a high in vivo clearance in rats of 75 mL/min/kg and TCN238 has a moderate volume of distribution (2.7 L/kg) with a short mean residence time (0.6 h) when dosed at 2 mg/kg via intravenous injection. TCN238 is orally bioavailable and 30 min following administration of a30 mg/kg dose, the plasma concentration is found to be 11.6 μM[1]. TCN 238 does not affect the performance of the learned task. However, the expression level of GRM4 in the hippocampus is reliable down-regulated five days after treatment with TCN 238. In addition, the expression level of GABRA1, encoding GABAA α-subunit is downregulated five days after the treatment in the frontal cortex[2]. | | IC 50 | mGlu4 Receptor: 1 μM (EC50) |
| | TCN 238 Preparation Products And Raw materials |
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