| Bioactivity | LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally. | ||||||||||||
| In Vivo | With oral administration of LX-1031 in mice, the average 5-HT reductions in the jejunum relative to control are appr 33, 51, and 66% with the 15, 45 and 135 mg/kg/day doses respectively. In a preliminary report, the effects of LX-1031, 100 mg/kg daily, on 5-HT levels in jejunal mucosa are reversible within 2 days of discontinuation in mice[1]. LX-1031 dose-dependently reduces expression of 5-HT in the duodenum, jejunum and ileum, but has no effect on brain 5-HT levels in preclinical assay[2]. | ||||||||||||
| Name | LX-1031 | ||||||||||||
| CAS | 945976-76-1 | ||||||||||||
| Formula | C28H25F3N4O4 | ||||||||||||
| Molar Mass | 538.52 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Camilleri M. LX-1031, a tryptophan 5-hydroxylase inhibitor, and its potential in chronic diarrhea associated with increased serotonin. Neurogastroenterol Motil. 2011 Mar;23(3):193-200. [2]. Camilleri M. LX-1031, a tryptophan 5-hydroxylase inhibitor that reduces 5-HT levels for the potential treatment of irritable bowel syndrome. IDrugs. 2010 Dec;13(12):921-8. |