4-Ethynyl-L-phenylalanine hydrochloride

4-Ethynyl-L-phenylalanine hydrochloride is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine hydrochloride is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine hydrochloride selectively and reversibly inhibits the biosynthesis of serotonin[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Tryptophan Hydroxylase

Research Areas >> Neurological Disease

Ki: 32.6 μM (TPH)[1]

4-Ethynyl-L-phenylalanine hydrochloride (30 mg/kg; i.p.) decreases in 5-HT and 5-HIAA levels in the rat midbrain but not in tissue[1]. 4-Ethynyl-L-phenylalanine hydrochloride is not inhibiting the aromatic amino acid decarboxylase[1]. 4-Ethynyl-L-phenylalanine hydrochloride has a low affinity for various recombinant 5-HT receptors[1]. Animal Model: Male Sprague-Dawley rats (200 g)[1] Dosage: 30 mg/kg Administration: Intraperitoneal injection Result: Decreased in 5-HT and 5-HIAA levels in the rat midbrain.

[1]. Stokes AH, et al. p-ethynylphenylalanine: a potent inhibitor of tryptophan hydroxylase. J Neurochem. 2000 May;74(5):2067-73.