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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.
Experiment: influence of AM251 or fenclonine pretreatment on the behavioral effects of paracetamol, AM404, or fluoxetine
In one set of groups, each mouse first received i.p. injections of AM251 (2mg/kg) or vehicle (Tween 80 : DMSO : saline, 10ml/kg), whereas in another set, mice were treated with fenclonine (300mg/kg×3 days) or vehicle (10ml/kg×3 days) for 3 consecutive days. Thirty minutes after AM251 injection or 24h after the last fenclonine injection, individual mice from each set of groups received a second i.p. injection of either vehicle (Tocrisolve 100 or 0.9% saline, 10 ml/kg), paracetamol (50 or 400mg/kg), or fluoxetine (20mg/kg), or AM404 (20 mg/kg). Thirty minutes later, mice were individually subjected to FST, TST, MBB, or locomotor activity. Separate groups of mice were used for each combined treatment and test (n=7/group). Doses of AM251 (2mg/ kg, i.p.) or fenclonine were determined in a preliminary study. Fenclonine was dissolved in 0.1 N NaOH, and then neutralized with 0.1 N HCl and finally adjusted with 0.9% saline.
https://pubmed.ncbi.nlm.nih.gov/25340977/
| 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 |
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