Tryptamine

Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models^[1][2][3]. In Vitro:Tryptamine (100 μM; 48 h) significantly inhibits MOG35-55-specific CD4+ T cell proliferation and RORγT+ cell differentiation in T cell proliferation assay^[2].
Tryptamine (1 mM; 1 h) significantly increases intracellular cAMP levels in colon organoid cAMP assay, revealing activation of 5-HT4R signaling pathway^[3].
Tryptamine (1 mM; 30 min) significantly increases the surface area of ??colon organoids from GF and HM mice in colon organoid swelling assay, demonstrating promotion of fluid secretion^[3]. In Vivo:Tryptamine (0.5 mg/kg, 12 mg/kg; intravenous injection; single dose) induces elevated body temperature and enhances spinal reflex activity in rabbit models^[1].
Tryptamine (12.5 mg/kg; intraperitoneal injection; once every 2 days; 13 days) significantly alleviates paralysis symptoms, reduces CD4+ T cell infiltration in the central nervous system and promotes Treg differentiation in a chronic progressive EAE model in C57BL/6 mice^[2].