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5-HTP is rapidly absorbed with a t max of ≈1.5 h, and rapidly eliminated with a half-life of ≈1.5 – 2 h. Co-administration of a decarboxylase inhibitor (e.g., carbidopa, benserazide ) doubles the half-life of 5-HTP to ≈ 3 – 4 h , [ 37 ] [ 34 ] and enhances exposure several-fold, depending on the dosing regimen.
5-HTP is produced from the amino acid tryptophan through the action of the enzyme tryptophan hydroxylase. Tryptophan hydroxylase is one of the biopterin-dependent aromatic amino acid hydroxylases. Production of 5-HTP is the rate-limiting step in 5-HT (serotonin) synthesis. 5-HTP is normally rapidly converted to 5-HT by amino acid decarboxylase. [1]
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α-Methyl-5-hydroxytryptophan (α-Me-5-HTP) is a synthetic tryptamine derivative, an artificial amino acid, and a prodrug of α-methylserotonin. [ 1 ] [ 2 ] It is the α- methylated derivative of 5-hydroxytryptophan (5-HTP), while αMS is the α-methylated analogue of serotonin .
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Carbidopa/oxitriptan (developmental code name EVX-101), or carbidopa/5-hydroxytryptophan (carbidopa/5-HTP), is a combination of 5-hydroxytryptophan (oxitriptan), a serotonin precursor, and carbidopa, a peripherally selective aromatic L-amino acid decarboxylase inhibitor, which is under development as an antidepressant for the treatment of depressive disorders. [1]