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Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). 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]. | [in vivo]
Dosage of Taltirelin in non-salt form:
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]. | Animal Model: | MPTP (HY-15608) or Rotenone (HY-B1756) treated male C57/BL6 mice aged 8-9 weeks old[2] | | Dosage: | 0.2 mg/kg, 1 mg/kg, 5 mg/kg 14 days; 0.2 mg/kg, 1 mg/kg 56 days | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Improved the locomotor function and preserved dopaminergic neurons in the substantia nigra.
Down-regulated the levels of p-tau (S396), p-α-synuclein (S129) tau N368 and α-synuclein N103 fragments in substantia nigra and striatum.
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| Animal Model: | 5-FU (HY-90006) or radiation treated adult C57BL/6NCr mice aged 7-8 weeks;
Balb/cAnNCr mice aged 9 weeks old with colon 26 carcinoma[3] | | Dosage: | 1mg/kg;
10mg/kg | | Administration: | Intraperitoneal injection (i.p.);
Oral administration (p.o.);
Twice a day before the test and once again 30 minutes prior to the test.
| | Result: | Reversed the fatigue-like effect, caused mice to run nearer to the top of the treadmill during the test.
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| [References]
[1] Thirunarayanan N, et al. Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor. Front Endocrinol (Lausanne). 2012 Oct 9;3:120. DOI:10.3389/fendo.2012.00120
[2] Zheng C, et al. TRH Analog, Taltirelin Protects Dopaminergic Neurons From Neurotoxicity of MPTP and Rotenone. Front Cell Neurosci. 2018 Dec 20;12:485. DOI:10.3389/fncel.2018.00485
[3] Dougherty JP, et al. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue. Pharmacol Res. 2017 Oct;124:1-8. DOI:10.1016/j.phrs.2017.07.012 |
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