Taltirelin

Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC₅₀ at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca²⁺ concentration (Ca²⁺ release) with an EC₅₀ value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue^[1][2][3]. IC50 & Target:IC₅₀: 910 nM (Thyrotropin-releasing hormone receptor)^[1] In Vitro:Taltirelin (5 μM; 2 h) improves cell viability, reducess ROS production and apoptosis in MPP+ (HY-W008719) or Rotenone (HY-B1756) treated SH-SY5Y cells and primary rat midbrain neurons^[2].
Taltirelin (5 μM; 2 h) exerts neuroprotective effects by inhibiting tau phosphorylation and AEP activation in SH-SY5Y cells treated with MPP+ (HY-W008719) or rotenone (HY-B1756)^[2]. In Vivo:Taltirelin (0.2-5 mg/kg; Intraperitoneal injection; 14-56 days) has a neuroprotective effect in mouse models of MPTP (HY-15608) and chronic rotenone (HY-B1756) -induced PD, and improves locomotor function in mice ^[2].
Taltirelin (1 mg/kg Intraperitoneal injection; 10 mg/kg Oral administration; 1 day) alleviates the fatigue-like behavior caused by chemotherapy treatment, tumor burden and irradiation in mouse models ^[3].