Fenclonine (4-Chloro-DL-phenylalanine) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine (4-Chloro-DL-phenylalanine) acts pharmacologically to deplete endogenous levels of serotonin. Fenclonine (4-Chloro-DL-phenylalanine; PCPA) markedly attenuates MCT(monocrotaline)-induced pulmonary vascular remodeling and lung inflammation, inhibits the expression of Tph-1 and SERT and suppresses the expression of MMP-2/-9, TIMP-1/-2, interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α) and intercellular adhesion molecule-1 (ICAM-1). Fenclonine inhibits 5-HT by suppressing Tph-1, regulating SERT and the serotonin downstream signaling pathway.
| Molecular Weight | 199.63 |
| Formula | C9H10ClNO2 |
| CAS Number | 7424-00-2 |
| Form | Solid |
| Solubility (25°C) | DMSO >60 mg/mL (ultrasonic and adjust pH to 2 with HCl) Water 4 mg/mL (ultrasonic and warming and adjust pH to 2 with HCl) |
| 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.
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